Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

Can the pharmaceutical industry reduce attrition rates?

Kola, I., & Landis, J. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1470 · Cited by 4,167 · see citing works

PHARMACOLOGY AND FUNCTIONS OF METABOTROPIC GLUTAMATE RECEPTORS

Conn, P. J., & Pin, J. (1997) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.37.1.205 · Cited by 3,083 · see citing works

The Ecology of Freshwater Phytoplankton.

Jones, R. I., & REYNOLDS, C. S. (1985) · Journal of Ecology · doi:10.2307/2260522 · Cited by 2,852 · see citing works

The mGluR theory of fragile X mental retardation

Bear, M. F., Huber, K. M., & Warren, S. T. (2004) · Trends in Neurosciences · doi:10.1016/j.tins.2004.04.009 · Cited by 1,580 · see citing works

G Protein-coupled Receptors

Ji, T. H., Grossmann, M., & Ji, I. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.28.17299 · Cited by 1,291 · see citing works

Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity

Dorr, P. K., Westby, M., Dobbs, S., Griffin, P., Irvine, B., Macartney, M. J., Mori, J., Rickett, G., Smith‐Burchnell, C., Napier, C. M., et al. (2005) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.49.11.4721-4732.2005 · Cited by 1,154 · see citing works

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B. K., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M., et al. (2006) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.106.104463 · Cited by 1,119 · see citing works

Operational models of pharmacological agonism

Black, J. W., & Leff, P. (1983) · Proceedings of the Royal Society B Biological Sciences · doi:10.1098/rspb.1983.0093 · Cited by 1,111 · see citing works

Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial

Patil, S. T., Zhang, L., Martenyi, F., Lowe, S. L., Jackson, K. A., Andreev, B. V., Avedisova, A. S., Bardenstein, L. M., Gurovich, I. Y., Morozova, M. A., et al. (2007) · Nature Medicine · doi:10.1038/nm1632 · Cited by 1,040 · see citing works

Reversal of Phencyclidine Effects by a Group II Metabotropic Glutamate Receptor Agonist in Rats

Moghaddam, B., & Adams, B. W. (1998) · Science · doi:10.1126/science.281.5381.1349 · Cited by 1,006 · see citing works

G Protein-Coupled Receptor Allosterism and Complexing

Christopoulos, A., & Kenakin, T. (2002) · Pharmacological Reviews · doi:10.1124/pr.54.2.323 · Cited by 934 · see citing works

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

Gasparini, F., Lingenhöhl, K., Stoehr, N., Flor, P. J., Heinrich, M., Vranesic, I., Biollaz, M., Allgeier, H., Heckendorn, R., Urwyler, S., et al. (1999) · Neuropharmacology · doi:10.1016/s0028-3908(99)00082-9 · Cited by 725 · see citing works

A new benzodiazepine pharmacology

Möhler, H., Fritschy, J. M., & Rudolph, U. (2002) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.300.1.2 · Cited by 716 · see citing works

Allosteric Modulation of G Protein–Coupled Receptors

May, L. T., Leach, K., Sexton, P. M., & Christopoulos, A. (2006) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.47.120505.105159 · Cited by 698 · see citing works

Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain

Romano, C., Sesma, M. A., McDonald, C. T., O’Malley, K. L., van den Pol, A. N., & Olney, J. W. (1995) · The Journal of Comparative Neurology · doi:10.1002/cne.903550310 · Cited by 671 · see citing works

Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

Christopoulos, A. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd746 · Cited by 665 · see citing works

Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development

Wess, J., Eglen, R. M., & Gautam, D. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2379 · Cited by 637 · see citing works

Metabotropic glutamate receptors as novel targets for anxiety and stress disorders

Swanson, C. J., Bures, M., Johnson, M. P., Linden, A.-M., Monn, J. A., & Schoepp, D. D. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1630 · Cited by 607 · see citing works

G-Protein-coupled receptor oligomerization and its potential for drug discovery

George, S. R., O’Dowd, B. F., & Lee, S. P. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd913 · Cited by 590 · see citing works

G Protein-coupled Receptors

Gether, U., & Kobilka, B. K. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.29.17979 · Cited by 585 · see citing works

Selective Muscarinic Receptor Agonist Xanomeline as a Novel Treatment Approach for Schizophrenia

Shekhar, A., Potter, W. Z., Lightfoot, J., Lienemann, J., Dubé, S., Mallinckrodt, C. H., Bymaster, F. P., McKinzie, D. L., & Felder, C. C. (2008) · American Journal of Psychiatry · doi:10.1176/appi.ajp.2008.06091591 · Cited by 563 · see citing works

Metabotropic Glutamate Receptors 1 and 5 Differentially Regulate CA1 Pyramidal Cell Function

Mannaioni, G., Marino, M. J., Valenti, O., Traynelis, S. F., & Conn, P. J. (2001) · Journal of Neuroscience · doi:10.1523/jneurosci.21-16-05925.2001 · Cited by 441 · see citing works

Effects of ketamine and n-methyl-d-aspartate on glutamate and dopamine release in the rat prefrontal cortex: modulation by a group II selective metabotropic glutamate receptor agonist LY379268

Lorrain, D. S., Baccei, C. S., Bristow, L. J., Anderson, J. J., & Varney, M. A. (2003) · Neuroscience · doi:10.1016/s0306-4522(02)00652-8 · Cited by 432 · see citing works

A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5

Dragic, T., Trkola, A., Thompson, D. A. D., Cormier, E. G., Kajumo, F., Maxwell, E., Lin, S. W., Ying, W., Smith, S. O., Sakmar, T. P., et al. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.090576697 · Cited by 427 · see citing works

3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity

Cosford, N. D. P., Tehrani, L. R., Roppe, J. R., Schweiger, E. J., Smith, N. D., Anderson, J., Bristow, L. J., Brodkin, J. D., Jiang, X., McDonald, I. A., et al. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm025570j · Cited by 397 · see citing works

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

Leach, K., Sexton, P. M., & Christopoulos, A. (2007) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2007.06.004 · Cited by 362 · see citing works

Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods.

Ehlert, F. J. (1988) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)13145-3 · Cited by 356 · see citing works

Metabotropic glutamate receptors in the basal ganglia motor circuit

Conn, P. J., Battaglia, G., Marino, M. J., & Nicoletti, F. (2005) · Nature reviews. Neuroscience · doi:10.1038/nrn1763 · Cited by 330 · see citing works

New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism

Kenakin, T. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1875 · Cited by 319 · see citing works

Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity

Porter, R. H. P., Jaeschke, G., Spooren, W., Ballard, T. M., Büttelmann, B., Kolczewski, S., Peters, J.-U., Prinssen, E., Wichmann, J., Vieira, E., et al. (2005) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.089839 · Cited by 308 · see citing works

A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral Models

Kinney, G. G., O’Brien, J. A., Lemaire, W., Burno, M., Bickel, D. J., Clements, M. K., Chen, T., Wisnoski, D. D., Lindsley, C. W., Tiller, P. R., et al. (2005) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.104.079244 · Cited by 298 · see citing works

N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl- d -aspartate receptor activity

Sur, C., Mallorga, P. J., Wittmann, M., Jacobson, M. A., Pascarella, D. M., Williams, J. B., Brandish, P. E., Pettibone, D. J., Scolnick, E. M., & Conn, P. J. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1835612100 · Cited by 295 · see citing works

Physiological Antagonism between 5-Hydroxytryptamine2A and Group II Metabotropic Glutamate Receptors in Prefrontal Cortex

Marek, G. J., Wright, R. A., Schoepp, D. D., Monn, J. A., & Aghajanian, G. K. (2000) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)35262-0 · Cited by 280 · see citing works

Orphan G-protein-coupled receptors and natural ligand discovery

Howard, A. D., McAllister, G., Feighner, S. D., Liu, Q., Nargund, R. P., der Ploeg, L. H. T. V., & Patchett, A. A. (2001) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(00)01636-9 · Cited by 271 · see citing works

The Non-competitive Antagonists 2-Methyl-6-(phenylethynyl)pyridine and 7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic Acid Ethyl Ester Interact with Overlapping Binding Pockets in the Transmembrane Region of Group I Metabotropic Glutamate Receptors

Pagano, A., Rüegg, D., Litschig, S., Stoehr, N., Stierlin, C., Heinrich, M., Floersheim, P., Prézeau, L., Carroll, F. Y., Pin, J., et al. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.m006230200 · Cited by 271 · see citing works

Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors.

Lazareno, S., & Birdsall, N. J. M. (1995) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)10255-1 · Cited by 266 · see citing works

Molecular Interactions of Cyclam and Bicyclam Non-peptide Antagonists with the CXCR4 Chemokine Receptor

Gerlach, L. O., Skerlj, R. T., Bridger, G. J., & Schwartz, T. W. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m010429200 · Cited by 261 · see citing works

Novel Selective Allosteric Activator of the M1Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats

Jones, C. K., Brady, A. E., Davis, A. A., Xiang, Z., Bubser, M., Tantawy, M. N., Kane, A. S., Bridges, T. M., Kennedy, J. P., Bradley, S. R., et al. (2008) · Journal of Neuroscience · doi:10.1523/jneurosci.1850-08.2008 · Cited by 248 · see citing works

Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment

Marino, M. J., Williams, D. L., O’Brien, J. A., Valenti, O., McDonald, T. P., Clements, M. K., Wang, R., DiLella, A. G., Hess, J. F., Kinney, G. G., et al. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1835724100 · Cited by 240 · see citing works

Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site

Knoflach, F., Mutel, V., Jolidon, S., Kew, J. N. C., Malherbe, P., Vieira, E., Wichmann, J., & Kemp, J. A. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.231358298 · Cited by 239 · see citing works

Molecular Mechanism of AMD3100 Antagonism in the CXCR4 Receptor

ROSENKILDE, M. M., Gerlach, L., Jakobsen, J. S., Skerlj, R. T., Bridger, G. J., & Schwartz, T. W. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m309546200 · Cited by 238 · see citing works

Allosteric modulation of the muscarinic M 4 receptor as an approach to treating schizophrenia

Chan, W. Y., McKinzie, D. L., Bose, S., Mitchell, S. N., Witkin, J. M., Thompson, R. C., Christopoulos, A., Lazareno, S., Birdsall, N. J. M., Bymaster, F. P., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0800567105 · Cited by 235 · see citing works

Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro

Maeda, K., Nakata, H., Koh, Y., Miyakawa, T., Ogata, H., Takaoka, Y., Shibayama, S., Sagawa, K., Fukushima, D., Moravek, J., et al. (2004) · Journal of Virology · doi:10.1128/jvi.78.16.8654-8662.2004 · Cited by 221 · see citing works

Metabotropic Glutamate Subtype 5 Receptors Modulate Locomotor Activity and Sensorimotor Gating in Rodents

Kinney, G. G., Burno, M., Campbell, U. C., Hernández, L. M., Rodriguez, D. E., Bristow, L. J., & Conn, P. J. (2003) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.048702 · Cited by 219 · see citing works

A Family of Highly Selective Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5

O’Brien, J. A., Lemaire, W., Chen, T., Chang, R. S. L., Jacobson, M. A., Ha, S., Lindsley, C. W., Schaffhauser, H., Sur, C., Pettibone, D. J., et al. (2003) · Molecular Pharmacology · doi:10.1124/mol.64.3.731 · Cited by 209 · see citing works

LY354740, an mGlu2/3 Receptor Agonist as a Novel Approach to Treat Anxiety/Stress

Schoepp, D. D., Wright, R. A., Levine, L. R., Gaydos, B. L., & Potter, W. Z. (2003) · Stress · doi:10.1080/1025389031000146773 · Cited by 207 · see citing works

Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats

Brady, A. E., Jones, C. K., Bridges, T. M., Kennedy, J. P., Thompson, A. D., Heiman, J. U., Breininger, M. L., Gentry, P. R., Yin, H., Jadhav, S. B., et al. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.140350 · Cited by 204 · see citing works

Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (–)-(1 R, 4 S,5 S,6 S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039)

Fell, M. J., Svensson, K. A., Johnson, B. G., & Schoepp, D. D. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.136861 · Cited by 204 · see citing works

Analysis of the Mechanism by Which the Small-Molecule CCR5 Antagonists SCH-351125 and SCH-350581 Inhibit Human Immunodeficiency Virus Type 1 Entry

Tsamis, F., Gavrilov, S., Kajumo, F., Seibert, C., Kuhmann, S. E., Ketas, T., Trkola, A., Palani, A., Clader, J. W., Tagat, J. R., et al. (2003) · Journal of Virology · doi:10.1128/jvi.77.9.5201-5208.2003 · Cited by 203 · see citing works

The Heptahelical Domain of GABAB2 Is Activated Directly by CGP7930, a Positive Allosteric Modulator of the GABAB Receptor

Binet, V., Brajon, C., Corre, L. L., Acher, F., Pin, J., & Prézeau, L. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m400930200 · Cited by 200 · see citing works

Activation of NMDA receptors reverses desensitization of mGluR5 in native and recombinant systems

Alagarsamy, S., Marino, M. J., Rouse, S. T., Gereau, R. W., Heinemann, S. F., & Conn, P. J. (1999) · Nature Neuroscience · doi:10.1038/6338 · Cited by 199 · see citing works

(−)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection

Maj, M. (2003) · Neuropharmacology · doi:10.1016/s0028-3908(03)00271-5 · Cited by 197 · see citing works

Discovery of an Ectopic Activation Site on the M1Muscarinic Receptor

Spalding, T. A., Trotter, C., Skjærbæk, N., Messier, T., Currier, E. A., Burstein, E. S., Li, D., Hacksell, U., & Brann, M. R. (2002) · Molecular Pharmacology · doi:10.1124/mol.61.6.1297 · Cited by 193 · see citing works

Targeting metabotropic glutamate receptors for treatment of the cognitive symptoms of schizophrenia

Moghaddam, B. (2004) · Psychopharmacology · doi:10.1007/s00213-004-1792-z · Cited by 189 · see citing works

Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4

Niswender, C. M., Johnson, K. A., Weaver, C. D., Jones, C. K., Xiang, Z., Luo, Q., Rodriguez, A. L., Marlo, J. E., de Paulis, T., Thompson, A. D., et al. (2008) · Molecular Pharmacology · doi:10.1124/mol.108.049551 · Cited by 189 · see citing works

SIB-1757 and SIB-1893: Selective, Noncompetitive Antagonists of Metabotropic Glutamate Receptor Type 5

Varney, M. A., Cosford, N. D. P., Jachec, C., Rao, S. P., Sacaan, A. I., Lin, F., Bleicher, L. S., Santori, E. M., Flor, P. J., Allgeier, H., et al. (1999) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)34881-5 · Cited by 189 · see citing works

Anxiolytic effects of a novel group II metabotropic glutamate receptor agonist (LY354740) in the fear-potentiated startle paradigm in humans

Grillon, C., Cordova, J., Levine, L. R., & Morgan, C. A. (2003) · Psychopharmacology · doi:10.1007/s00213-003-1444-8 · Cited by 185 · see citing works

Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation

Hall, D. A. (2000) · Molecular Pharmacology · doi:10.1124/mol.58.6.1412 · Cited by 185 · see citing works

Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine

Johnson, M. P., Baez, M., Jagdmann, G. E., Britton, T. C., Large, T. H., Callagaro, D. O., Tizzano, J. P., Monn, J. A., & Schoepp, D. D. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm034015u · Cited by 182 · see citing works

A novel class of antagonists for metabotropic glutamate receptors, 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylates

Annoura, H., Fukunaga, A., Uesugi, M., Tatsuoka, T., & Horikawa, Y. (1996) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/0960-894x(96)00104-7 · Cited by 180 · see citing works

A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors Has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity

Galici, R., Echemendia, N. G., Rodriguez, A. L., & Conn, P. J. (2005) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.091074 · Cited by 175 · see citing works

A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity

Valant, C., Gregory, K. J., Hall, N. E., Scammells, P. J., Lew, M. J., Sexton, P. M., & Christopoulos, A. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m803801200 · Cited by 173 · see citing works

Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB‐1893 and MPEP

Mathiesen, J. M., Svendsen, N., Bräuner‐Osborne, H., Thomsen, C., & Ramirez, M. T. (2003) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0705159 · Cited by 173 · see citing works

Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That Potentiate Receptor Function in Vivo

Lindsley, C. W., Wisnoski, D. D., Leister, W., O’Brien, J. A., Lemaire, W., David L. Williams, Burno, M., Sur, C., Kinney, G. G., Pettibone, D. J., et al. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm049400d · Cited by 170 · see citing works

A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain

O’Brien, J. A., Lemaire, W., Wittmann, M., Jacobson, M. A., Ha, S., Wisnoski, D. D., Lindsley, C. W., Schaffhauser, H., Rowe, B. A., Sur, C., et al. (2004) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.061747 · Cited by 170 · see citing works

Biphenyl-indanone A, a Positive Allosteric Modulator of the Metabotropic Glutamate Receptor Subtype 2, Has Antipsychotic- and Anxiolytic-Like Effects in Mice

Galici, R., Jones, C. K., Hemstapat, R., Nong, Y., Echemendia, N. G., Williams, L. C., de Paulis, T., & Conn, P. J. (2006) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.106.102046 · Cited by 169 · see citing works

Metabotropic Glutamate Receptor Subtype 5 Antagonists MPEP and MTEP

Lea, P. M., & Faden, A. I. (2006) · CNS Drug Reviews · doi:10.1111/j.1527-3458.2006.00149.x · Cited by 168 · see citing works

Functional neuroanatomy of the basal ganglia in Parkinson's disease.

Wichmann, T., & DeLong, M. R. (2003) · PubMed · Cited by 167 · see citing works

Group III Metabotropic Glutamate Receptor-Mediated Modulation of the Striatopallidal Synapse

Valenti, O., Marino, M. J., Wittmann, M., Lis, E. V., DiLella, A. G., Kinney, G. G., & Conn, P. J. (2003) · Journal of Neuroscience · doi:10.1523/jneurosci.23-18-07218.2003 · Cited by 166 · see citing works

Treatment of Anxiety Using Fenobam (a Nonbenzodiazepine) in a Double-Blind Standard (Diazepam) Placebo-Controlled Study

Pecknold, J. C., McClure, D., APPELTAUER, L., Wrzesinski, L., & ALLAN, T. (1982) · Journal of Clinical Psychopharmacology · doi:10.1097/00004714-198204000-00010 · Cited by 165 · see citing works

Structural and Molecular Interactions of CCR5 Inhibitors with CCR5

Maeda, K., Das, D., Ogata-Aoki, H., Nakata, H., Miyakawa, T., Tojo, Y., Norman, R., Takaoka, Y., Ding, J., Arnold, G. F., et al. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m512688200 · Cited by 163 · see citing works

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission

Shirey-Rice, J. K., Xiang, Z., Orton, D., Brady, A. E., Johnson, K. A., Williams, R. D., Ayala, J. E., Rodriguez, A. L., Wess, J., Weaver, D., et al. (2007) · Nature Chemical Biology · doi:10.1038/nchembio.2007.55 · Cited by 161 · see citing works

Pharmacological Characterization and Identification of Amino Acids Involved in the Positive Modulation of Metabotropic Glutamate Receptor Subtype 2

Schaffhauser, H., Rowe, B. A., Morales, S., Chavez-Noriega, L. E., Yin, R., Jachec, C., Rao, S. P., Bain, G., Pinkerton, A. B., Vernier, J., et al. (2003) · Molecular Pharmacology · doi:10.1124/mol.64.4.798 · Cited by 160 · see citing works

A Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 2 Blocks a Hallucinogenic Drug Model of Psychosis

Benneyworth, M. A., Xiang, Z., Smith, R. L., Garcia, E. E., Conn, P. J., & Sanders‐Bush, E. (2007) · Molecular Pharmacology · doi:10.1124/mol.107.035170 · Cited by 159 · see citing works

Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s)

Johnson, M. P., Barda, D., Britton, T. C., Emkey, R., Hornback, W. J., Jagdmann, G. E., McKinzie, D. L., Nisenbaum, E. S., Tizzano, J. P., & Schoepp, D. D. (2005) · Psychopharmacology · doi:10.1007/s00213-004-2099-9 · Cited by 156 · see citing works

Progress Towards Validating the NMDA Receptor Hypofunction Hypothesis of Schizophrenia

Lindsley, C. W., Shipe, W. D., Wolkenberg, S. E., Theberge, C. R., Williams, D., Jr., Sur, C., & Kinney, G. G. (2006) · Current Topics in Medicinal Chemistry · doi:10.2174/156802606777057599 · Cited by 156 · see citing works

Homology Modeling of the Transmembrane Domain of the Human Calcium Sensing Receptor and Localization of an Allosteric Binding Site

Miedlich, S. U., Gama, L., Seuwen, K., Wolf, R. M., & Breitwieser, G. E. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m307191200 · Cited by 152 · see citing works

Interaction of N-methyl-D-aspartate and group 5 metabotropic glutamate receptors on behavioral flexibility using a novel operant set-shift paradigm

Darrah, J. M., Stefani, M. R., & Moghaddam, B. (2008) · Behavioural Pharmacology · doi:10.1097/fbp.0b013e3282feb0ac · Cited by 145 · see citing works

Activation of Group II Metabotropic Glutamate Receptors Inhibits Synaptic Excitation of the Substantia Nigra Pars Reticulata

Bradley, S. R., Marino, M. J., Wittmann, M., Rouse, S. T., Awad, H., Levey, A. I., & Conn, P. J. (2000) · The Journal of Neuroscience · doi:10.1523/jneurosci.20-09-03085.2000 · Cited by 141 · see citing works

Mutations in G proteins and G protein-coupled receptors in endocrine disease.

Am, S. (1996) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jcem.81.7.8675557 · Cited by 138 · see citing works

Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis.

Matsui, H., Lazareno, S., & Birdsall, N. J. M. (1995) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)08527-x · Cited by 136 · see citing works

Mutational Analysis and Molecular Modeling of the Allosteric Binding Site of a Novel, Selective, Noncompetitive Antagonist of the Metabotropic Glutamate 1 Receptor

Malherbe, P., Kratochwil, N. A., Knoflach, F., Zenner, M., Kew, J. N. C., Kratzeisen, C., Maerki, H. P., Adam, G., & Mutel, V. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m211759200 · Cited by 135 · see citing works

Modeling and Mutagenesis of the Binding Site of Calhex 231, a Novel Negative Allosteric Modulator of the Extracellular Ca2+-sensing Receptor

Pétrel, C., Kessler, A., Maslah, F., Dauban, P., Dodd, R. H., Rognan, D., & Ruat, M. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m308010200 · Cited by 135 · see citing works

Direct and Indirect Modulation of the N-Methyl D-Aspartate Receptor: Potential for the Development of Novel Antipsychotic Therapies

Marino, M. J., & Conn, P. J. (2002) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/1568007023339544 · Cited by 134 · see citing works

Substituent Effects ofN-(1,3-Diphenyl-1H-pyrazol-5-yl)benzamides on Positive Allosteric Modulation of the Metabotropic Glutamate-5 Receptor in Rat Cortical Astrocytes

de Paulis, T., Hemstapat, R., Chen, Y., Zhang, Y., Saleh, S., Alagille, D., Baldwin, R. M., Tamagnan, G. D., & Conn, P. J. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm051252j · Cited by 133 · see citing works

Characterization of a CNS penetrant, selective M1muscarinic receptor agonist, 77‐LH‐28‐1

Langmead, C. J., Austin, N. E., Branch, C. L., Brown, J. T., Buchanan, K. A., Davies, C. H., Forbes, I. T., Fry, V. A. H., Hagan, J. J., Herdon, H. J., et al. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.152 · Cited by 132 · see citing works

Muscarinic Receptors as a Target for Drugs Treating Schizophrenia

Bymaster, F. P., Felder, C. C., Ahmed, S., & McKinzie, D. L. (2002) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/1568007024606249 · Cited by 131 · see citing works

Distinct physiological roles of the Gq‐coupled metabotropic glutamate receptors co‐expressed in the same neuronal populations

Valenti, O., Conn, P. J., & Marino, M. J. (2002) · Journal of Cellular Physiology · doi:10.1002/jcp.10081 · Cited by 125 · see citing works

The mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) potentiates PCP-induced cognitive deficits in rats

Campbell, U. C., Lalwani, K., Hernández, L. M., Kinney, G. G., Conn, P. J., & Bristow, L. J. (2004) · Psychopharmacology · doi:10.1007/s00213-004-1827-5 · Cited by 123 · see citing works

A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators

Rodriguez, A. L., Nong, Y., Sekaran, N. K., Alagille, D., Tamagnan, G. D., & Conn, P. J. (2005) · Molecular Pharmacology · doi:10.1124/mol.105.016139 · Cited by 123 · see citing works

Pharmacological Activation of mGlu4 Metabotropic Glutamate Receptors Reduces Nigrostriatal Degeneration in Mice Treated with 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine

Battaglia, G., Busceti, C. L., Molinaro, G., Biagioni, F., Traficante, A., Nicoletti, F., & Bruno, V. (2006) · Journal of Neuroscience · doi:10.1523/jneurosci.1595-06.2006 · Cited by 120 · see citing works

Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

Langmead, C. J., & Christopoulos, A. (2006) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2006.07.009 · Cited by 114 · see citing works

New Insights into the Function of M4 Muscarinic Acetylcholine Receptors Gained Using a Novel Allosteric Modulator and a DREADD (Designer Receptor Exclusively Activated by a Designer Drug)

Nawaratne, V., Leach, K., Suratman, N., Loiacono, R. E., Felder, C. C., Armbruster, B. N., Roth, B. L., Sexton, P. M., & Christopoulos, A. (2008) · Molecular Pharmacology · doi:10.1124/mol.108.049353 · Cited by 112 · see citing works

Muscarinic Receptor Agonists and Antagonists in the Treatment of Alzheimers Disease

Clader, J. W., & Wang, Y. (2005) · Current Pharmaceutical Design · doi:10.2174/138161205774370762 · Cited by 112 · see citing works

Antiepileptic Drugs in Development: Prospects for the Near Future

Leppik, I. E. (1994) · Epilepsia · doi:10.1111/j.1528-1157.1994.tb05953.x · Cited by 108 · see citing works

Localization of Agonist- and Antagonist-Binding Domains of Human Corticotropin-Releasing Factor Receptors

Liaw, C. W., Grigoriadis, D. E., Lorang, M. T., Souza, E. B. D., & Maki, R. A. (1997) · Molecular Endocrinology · doi:10.1210/mend.11.13.0034 · Cited by 107 · see citing works

Thiochrome Enhances Acetylcholine Affinity at Muscarinic M4 Receptors: Receptor Subtype Selectivity via Cooperativity Rather than Affinity

Lazareno, S., Doležal, V., Popham, A., & Birdsall, N. J. M. (2004) · Molecular Pharmacology · doi:10.1124/mol.65.1.257 · Cited by 104 · see citing works

Targeting Group III Metabotropic Glutamate Receptors Produces Complex Behavioral Effects in Rodent Models of Parkinson's Disease

Lopez, S., Turle-Lorenzo, N., Acher, F., Leonibus, E. D., Mele, A., & Amalric, M. (2007) · Journal of Neuroscience · doi:10.1523/jneurosci.0299-07.2007 · Cited by 102 · see citing works

Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes

Zhang, Y., Rodriguez, A. L., & Conn, P. J. (2005) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.090308 · Cited by 102 · see citing works

Preclinical Pharmacology of mGlu2 / 3 Receptor Agonists: Novel Agents for Schizophrenia?

Schoepp, D. D., & Marek, G. J. (2002) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/1568007024606177 · Cited by 100 · see citing works

Identification of Indole Derivatives Exclusively Interfering with a G Protein-Independent Signaling Pathway of the Prostaglandin D2 Receptor CRTH2

Mathiesen, J. M., Ulven, T., Martini, L., Gerlach, L. O., Heinemann, Á., & Kostenis, E. (2005) · Molecular Pharmacology · doi:10.1124/mol.104.010520 · Cited by 100 · see citing works

Genetic Variations and Polymorphisms of G Protein-Coupled Receptors: Functional and Therapeutic Implications

Rana, B. K., Shiina, T., & Insel, P. A. (2001) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.41.1.593 · Cited by 100 · see citing works

NMDA-induced potentiation of mGluR5 is mediated by activation of protein phosphatase 2B/calcineurin

Alagarsamy, S., Saugstad, J. A., Warren, L., Mansuy, I. M., Gereau, R. W., & Conn, P. J. (2005) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.05.005 · Cited by 99 · see citing works

N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) Acts through a Novel Site as a Positive Allosteric Modulator of Group 1 Metabotropic Glutamate Receptors

Chen, Y., Goudet, C., Pin, J., & Conn, P. J. (2007) · Molecular Pharmacology · doi:10.1124/mol.107.040097 · Cited by 96 · see citing works

Progress in Mapping Human Epilepsy Genes

Delgado‐Escueta, A. V., Serratosa, J. M., Liu, A. Y., Weissbecker, K., Medina, M. T., Gee, M. N., Treiman, L. J., & Sparkes, R. S. (1994) · Epilepsia · doi:10.1111/j.1528-1157.1994.tb05926.x · Cited by 95 · see citing works

Group II mGlu Receptor Activation Suppresses Norepinephrine Release in the Ventral Hippocampus and Locomotor Responses to Acute Ketamine Challenge

Lorrain, D. S., Schaffhauser, H., Campbell, U. C., Baccei, C. S., Correa, L. D., Rowe, B. A., Rodriguez, D. E., Anderson, J. J., Varney, M. A., Pinkerton, A. B., et al. (2003) · Neuropsychopharmacology · doi:10.1038/sj.npp.1300238 · Cited by 93 · see citing works

Group III Metabotropic Glutamate-Receptor-Mediated Modulation of Excitatory Transmission in Rodent Substantia Nigra Pars Compacta Dopamine Neurons

Valenti, O., Mannaioni, G., Seabrook, G. R., Conn, P. J., & Marino, M. J. (2005) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.104.080481 · Cited by 92 · see citing works

Site-Directed Mutagenesis Reveals Two Epitopes Involved in the Subtype Selectivity of the Allosteric Interactions of Gallamine at Muscarinic Acetylcholine Receptors

Gnagey, A. L., Seidenberg, M., & Ellis, J. (1999) · Molecular Pharmacology · doi:10.1124/mol.56.6.1245 · Cited by 91 · see citing works

Interaction of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 with the Negative Allosteric Antagonist Site Is Required for Potentiation of Receptor Responses

Chen, Y., Nong, Y., Goudet, C., Hemstapat, R., de Paulis, T., Pin, J., & Conn, P. J. (2007) · Molecular Pharmacology · doi:10.1124/mol.106.032425 · Cited by 89 · see citing works

Allosteric Site on Muscarinic Acetylcholine Receptors: Identification of Two Amino Acids in the Muscarinic M2 Receptor That Account Entirely for the M2/M5 Subtype Selectivities of Some Structurally Diverse Allosteric Ligands in N-Methylscopolamine-Occupied Receptors

Voigtländer, U., Jöhren, K., Mohr, M., Raasch, A., Tränkle, C., Buller, S., Ellis, J., Höltje, H., & Mohr, K. (2003) · Molecular Pharmacology · doi:10.1124/mol.64.1.21 · Cited by 88 · see citing works

Coordinate regulation of metabotropic glutamate receptors

Alagarsamy, S., Sorensen, S. D., & Conn, P. J. (2001) · Current Opinion in Neurobiology · doi:10.1016/s0959-4388(00)00219-1 · Cited by 84 · see citing works

Schizophrenia: Moving Beyond Monoamine Antagonists

Conn, P. J., Tamminga, C. A., Schoepp, D. D., & Lindsley, C. W. (2008) · Molecular Interventions · doi:10.1124/mi.8.2.7 · Cited by 84 · see citing works

Allosteric modulators of G-protein-coupled receptors

May, L. T. (2003) · Current Opinion in Pharmacology · doi:10.1016/s1471-4892(03)00107-3 · Cited by 84 · see citing works

Differential antagonism of the anticonflict effects of typical and atypical anxiolytics

Patel, J. B., Martin, C., & Malick, J. B. (1982) · European Journal of Pharmacology · doi:10.1016/0014-2999(82)90331-4 · Cited by 83 · see citing works

Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated

Ayala, J. E., Niswender, C. M., Luo, Q., Banko, J. L., & Conn, P. J. (2007) · Neuropharmacology · doi:10.1016/j.neuropharm.2007.12.009 · Cited by 80 · see citing works

Ethanol differentially affects ATP-gated P2X and P2X receptor subtypes expressed in oocytes

Davies, D. L., Kochegarov, A., Kuo, S. T., Kulkarni, A. A., WOODWARD, J., King, B. F., & Alkana, R. L. (2005) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.03.015 · Cited by 78 · see citing works

Calcium Sensing Receptor Activators: Calcimimetics

Harrington, P. E., & Fotsch, C. H. (2007) · Current Medicinal Chemistry · doi:10.2174/092986707782794096 · Cited by 75 · see citing works

Muscarinic agonists and antagonists in the treatment of Alzheimer's disease

Greenlee, W. J., CLADER, J. W., Asberom, T., McCombie, S. W., Ford, J., Guzik, H. S., Kozlowski, J. A., Li, S., Liu, C., Lowe, D., et al. (2001) · Il Farmaco · doi:10.1016/s0014-827x(01)01102-8 · Cited by 72 · see citing works

Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA

Zhao, Z., Wisnoski, D. D., O’Brien, J. A., Lemaire, W., Williams, D. L., Jacobson, M. A., Wittman, M., Ha, S., Schaffhauser, H., Sur, C., et al. (2006) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2006.11.081 · Cited by 71 · see citing works

A Novel Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Interact with a Site Distinct from That of Negative Allosteric Modulators

Hemstapat, R., de Paulis, T., Chen, Y., Brady, A. E., Grover, V. K., Alagille, D., Tamagnan, G. D., & Conn, P. J. (2006) · Molecular Pharmacology · doi:10.1124/mol.105.021857 · Cited by 68 · see citing works

Treatment of Motor Fluctuations in Parkinsonʼs Disease with an Oral Sustained-Release Preparation of L-Dopa

Poewe, W., Lees, A. J., & Stern, G. M. (1986) · Clinical Neuropharmacology · doi:10.1097/00002826-198610000-00003 · Cited by 62 · see citing works

Allosteric Interactions with Muscarinic Acetylcholine Receptors: Complex Role of the Conserved Tryptophan M2422Trp in a Critical Cluster of Amino Acids for Baseline Affinity, Subtype Selectivity, and Cooperativity

Prilla, S., Schrobang, J., Ellis, J., Höltje, H., & Mohr, K. (2006) · Molecular Pharmacology · doi:10.1124/mol.106.023481 · Cited by 59 · see citing works

Critical Amino Acid Residues of the Common Allosteric Site on the M2 Muscarinic Acetylcholine Receptor: More Similarities than Differences between the Structurally Divergent Agents Gallamine and Bis(ammonio)alkane-Type Hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)ammonium]dibromide

Huang, X., Prilla, S., Mohr, K., & Ellis, J. (2005) · Molecular Pharmacology · doi:10.1124/mol.105.014043 · Cited by 57 · see citing works

Allosteric Site on Muscarinic Acetylcholine Receptors: A Single Amino Acid in Transmembrane Region 7 Is Critical to the Subtype Selectivities of Caracurine V Derivatives and Alkane-Bisammonium Ligands

Buller, S., Zlotos, D. P., Mohr, K., & Ellis, J. (2002) · Molecular Pharmacology · doi:10.1124/mol.61.1.160 · Cited by 56 · see citing works

Point Mutations in the Transmembrane Region of GABAB2 Facilitate Activation by the Positive Modulator N,N′-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the Absence of the GABAB1 Subunit

Dupuis, D. S., Relkovic, D., Lhuillier, L., Mosbacher, J., & Kaupmann, K. (2006) · Molecular Pharmacology · doi:10.1124/mol.106.028183 · Cited by 54 · see citing works

Recent Advances in Non-Competitive mGlu5 Receptor Antagonists and their Potential Therapeutic Applications

Slassi, A., Isaac, M. B., Edwards, L. G., Minidis, A. B. E., Wensbo, D., Mattsson, J. P., Nilsson, K. A., Raboisson, P., McLeod, D. A., Stormann, T. M., et al. (2005) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026054750236 · Cited by 54 · see citing works

Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus

Poisik, O. V., Raju, D. V., Verreault, M., Rodriguez, A. L., Abeniyi, O. A., Conn, P. J., & Smith, Y. (2005) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.03.006 · Cited by 53 · see citing works

Application of a Kinetic Model to the Apparently Complex Behavior of Negative and Positive Allosteric Modulators of Muscarinic Acetylcholine Receptors

Avlani, V. A., May, L. T., Sexton, P. M., & Christopoulos, A. (2004) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.059840 · Cited by 53 · see citing works

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators

Pinkerton, A. B., Cube, R. V., Hutchinson, J. H., James, J. K., Gardner, M. F., Rowe, B. A., Schaffhauser, H., Rodriguez, D. E., Campbell, U. C., Daggett, L. P., et al. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.01.077 · Cited by 49 · see citing works

Changes of Cooperativity between N-Methylscopolamine and Allosteric Modulators Alcuronium and Gallamine Induced by Mutations of External Loops of Muscarinic M3 Receptors

Krejčı́, A., & Tucek, S. (2001) · Molecular Pharmacology · doi:10.1016/s0026-895x(24)12303-6 · Cited by 49 · see citing works

Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): Efficacy in an animal model for schizophrenia

Govek, S. P., Bonnefous, C., Hutchinson, J. H., Kamenecka, T. M., McQuiston, J., Pracitto, R., Zhao, L., Gardner, M. F., James, J. K., Daggett, L. P., et al. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.06.017 · Cited by 43 · see citing works

Allosteric Agonist Modulators

Kenakin, T. (2007) · Journal of Receptors and Signal Transduction · doi:10.1080/10799890701509000 · Cited by 43 · see citing works

Transposition of Three Amino Acids Transforms the Human Metabotropic Glutamate Receptor (mGluR)-3-Positive Allosteric Modulation Site to mGluR2, and Additional Characterization of the mGluR2-Positive Allosteric Modulation Site

Rowe, B. A., Schaffhauser, H., Morales, S., Lubbers, L. S., Bonnefous, C., Kamenecka, T. M., McQuiston, J., & Daggett, L. P. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.138271 · Cited by 40 · see citing works

Fish and fisheries of the Prespa lakes

Crivelli, A. J., Catsadorakis, G., Malakou, M., & Rosecchi, E. (1997) · Springer eBooks · doi:10.1007/978-94-011-5180-1_8 · Cited by 37 · see citing works

Asparagine, Valine, and Threonine in the Third Extracellular Loop of Muscarinic Receptor Have Essential Roles in the Positive Cooperativity of Strychnine-Like Allosteric Modulators

Jakubík, J., Krejčı́, A., & Doležal, V. (2005) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.104.080358 · Cited by 25 · see citing works

3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)

Cube, R. V., Vernier, J., Hutchinson, J. H., Gardner, M. F., James, J. K., Rowe, B. A., Schaffhauser, H., Daggett, L. P., & Pinkerton, A. B. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.02.078 · Cited by 24 · see citing works

Recent Developments of the PET Imaging Agents for Metabotropic Glutamate Receptor Subtype 5

Yu, M. (2007) · Current Topics in Medicinal Chemistry · doi:10.2174/156802607782507394 · Cited by 24 · see citing works

Allosteric effects of four stereoisomers of a fused indole ring system with 3H-N-methylscopolamine and acetylcholine at M1–M4 muscarinic receptors

Lazareno, S., Birdsall, B., Fukazawa, T., Gharagozloo, P., Hashimoto, T., Kuwano, H., Popham, A., Sugimoto, M., & Birdsall, N. J. M. (1999) · Life Sciences · doi:10.1016/s0024-3205(98)00596-7 · Cited by 21 · see citing works

Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract–piriform cortex synapse

Jones, P. J., Xiang, Z., & Conn, P. J. (2008) · Neuropharmacology · doi:10.1016/j.neuropharm.2008.06.043 · Cited by 18 · see citing works

Molecular Dynamics Simulation for All

Hollingsworth, S. A., & Dror, R. O. (2018) · Neuron · doi:10.1016/j.neuron.2018.08.011 · Cited by 3,313 · see citing works

The structure and function of G-protein-coupled receptors

Rosenbaum, D. M., Rasmussen, S. G. F., & Kobilka, B. K. (2009) · Nature · doi:10.1038/nature08144 · Cited by 2,534 · see citing works

Computational Methods in Drug Discovery

Sliwoski, G. R., Kothiwale, S., Meiler, J., & Lowe, E. W. (2013) · Pharmacological Reviews · doi:10.1124/pr.112.007336 · Cited by 2,226 · see citing works

How were new medicines discovered?

Swinney, D. C., & Anthony, J. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3480 · Cited by 1,812 · see citing works

Role of Molecular Dynamics and Related Methods in Drug Discovery

Vivo, M. D., Masetti, M., Bottegoni, G., & Cavalli, A. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01684 · Cited by 1,330 · see citing works

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

Fredholm, B. B., IJzerman, A. P., Jacobson, K. A., Linden, J. M., & Müller, C. E. (2011) · Pharmacological Reviews · doi:10.1124/pr.110.003285 · Cited by 1,307 · see citing works

GPCR Dynamics: Structures in Motion

Latorraca, N. R., Venkatakrishnan, A., & Dror, R. O. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.6b00177 · Cited by 843 · see citing works

Structure of an Agonist-Bound Human A 2A Adenosine Receptor

Xu, F., Wu, H., Katritch, V., Han, G. W., Jacobson, K. A., Gao, Z., Cherezov, V., & Stevens, R. C. (2011) · Science · doi:10.1126/science.1202793 · Cited by 816 · see citing works

Allostery in Disease and in Drug Discovery

Nussinov, R., & Tsai, C. (2013) · Cell · doi:10.1016/j.cell.2013.03.034 · Cited by 764 · see citing works

Pathway and mechanism of drug binding to G-protein-coupled receptors

Dror, R. O., Pan, A. C., Arlow, D. H., Borhani, D. W., Maragakis, P., Shan, Y., Xu, H., & Shaw, D. E. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1104614108 · Cited by 737 · see citing works

Excitotoxicity: Bridge to various triggers in neurodegenerative disorders

Mehta, A., Prabhakar, M., Kumar, P., Deshmukh, R. R., & Sharma, P. L. (2012) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2012.10.032 · Cited by 662 · see citing works

Ligand binding assays at equilibrium: validation and interpretation

Hulme, E. C., & Trevethick, M. (2010) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2009.00604.x · Cited by 661 · see citing works

Mutations causing syndromic autism define an axis of synaptic pathophysiology

Auerbach, B. D., Osterweil, E. K., & Bear, M. F. (2011) · Nature · doi:10.1038/nature10658 · Cited by 592 · see citing works

Emerging principles in protease-based drug discovery

Drąg, M., & Salvesen, G. S. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3053 · Cited by 605 · see citing works

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

Kenakin, T., & Miller, L. J. (2010) · Pharmacological Reviews · doi:10.1124/pr.108.000992 · Cited by 573 · see citing works

G Protein–Coupled Receptor Oligomerization Revisited: Functional and Pharmacological Perspectives

Ferré, S., Casadó, V., Devi, L. A., Filizola, M., Jockers, R., Lohse, M. J., Milligan, G., Pin, J., & Guitart, X. (2014) · Pharmacological Reviews · doi:10.1124/pr.113.008052 · Cited by 574 · see citing works

The changing opioid crisis: development, challenges and opportunities

Volkow, N. D., & Blanco, C. (2020) · Molecular Psychiatry · doi:10.1038/s41380-020-0661-4 · Cited by 564 · see citing works

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

Bokoch, M. P., Zou, Y., Rasmussen, S. G. F., Liu, C. W., Nygaard, R., Rosenbaum, D. M., Fung, J. J., Choi, H., Thian, F. S., Kobilka, T. S., et al. (2010) · Nature · doi:10.1038/nature08650 · Cited by 471 · see citing works

Diversity and Modularity of G Protein-Coupled Receptor Structures

Katritch, V., Cherezov, V., & Stevens, R. (2011) · TIPS - Trends in Pharmacological Sciences · doi:10.1016/j.tips.2011.09.003 · Cited by 495 · see citing works

Muscarinic acetylcholine receptors: novel opportunities for drug development

Kruse, A. C., Kobilka, B. K., Gautam, D., Sexton, P. M., Christopoulos, A., & Wess, J. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4295 · Cited by 437 · see citing works

Conus Venom Peptide Pharmacology

Lewis, R. J., Dutertre, S., Vetter, I., & Christie, M. J. (2012) · Pharmacological Reviews · doi:10.1124/pr.111.005322 · Cited by 425 · see citing works

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

Dore, A. S., Okrasa, K., Patel, J. C., Serrano‐Vega, M. J., Bennett, K. A., Cooke, R. M., Errey, J. C., Jazayeri, A., Khan, S. A., Tehan, B. G., et al. (2014) · Nature · doi:10.1038/nature13396 · Cited by 410 · see citing works

Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety

Burgin, A. B., Magnússon, Ó. Þ., Singh, J., Witte, P., Staker, B. L., Björnsson, J. M., Þorsteinsdóttir, M., Hrafnsdóttir, S., Hagen, T. J., Kiselyov, A. S., et al. (2009) · Nature Biotechnology · doi:10.1038/nbt.1598 · Cited by 396 · see citing works

Allostery and the Monod-Wyman-Changeux Model After 50 Years

Changeux, J. (2012) · Annual Review of Biophysics · doi:10.1146/annurev-biophys-050511-102222 · Cited by 393 · see citing works

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · see citing works

The role of serotonin 5-HT2A receptors in memory and cognition

Zhang, G., & Stackman, R. W. (2015) · Frontiers in Pharmacology · doi:10.3389/fphar.2015.00225 · Cited by 386 · see citing works

Therapies for rare diseases: therapeutic modalities, progress and challenges ahead

Tambuyzer, E., Vandendriessche, B., Austin, C. P., Brooks, P. J., Larsson, K., Miller Needleman, K. I., Valentine, J., Davies, K., Groft, S. C., Preti, R., et al. (2020) · Nature Reviews Drug Discovery · doi:10.1038/s41573-019-0049-9 · Cited by 357 · see citing works

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

Changeux, J., & Christopoulos, A. (2016) · Cell · doi:10.1016/j.cell.2016.08.015 · Cited by 341 · see citing works

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

Thal, D. M., Sun, B., Feng, D., Nawaratne, V., Leach, K., Felder, C. C., Bures, M. G., Evans, D. A. P., Weis, W. I., Bachhawat, P., et al. (2016) · Nature · doi:10.1038/nature17188 · Cited by 337 · see citing works

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

Conn, P. J., Lindsley, C. W., & Jones, C. K. (2008) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2008.10.006 · Cited by 330 · see citing works

Discovering Anti-Cancer Drugs via Computational Methods

Cui, W., Aouidate, A., Wang, S., Yu, Q., Li, Y.-H., & Yuan, S. (2020) · Frontiers in Pharmacology · doi:10.3389/fphar.2020.00733 · Cited by 310 · see citing works

Fluorescence/Bioluminescence Resonance Energy Transfer Techniques to Study G-Protein-Coupled Receptor Activation and Signaling

Lohse, M. J., Nuber, S., & Hoffmann, C. (2012) · Pharmacological Reviews · doi:10.1124/pr.110.004309 · Cited by 306 · see citing works

Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

Conn, P. J., Jones, C. K., & Lindsley, C. W. (2009) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2008.12.002 · Cited by 286 · see citing works

Drugs for Allosteric Sites on Receptors

Wenthur, C. J., Gentry, P. R., Mathews, T. P., & Lindsley, C. W. (2011) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010611-134525 · Cited by 274 · see citing works

Homeostatic Scaling Requires Group I mGluR Activation Mediated by Homer1a

Hu, J.-H., Park, J. M., Park, S. J., Xiao, B., Dehoff, M. H., Kim, S., Hayashi, T., Schwarz, M. K., Huganir, R. L., Seeburg, P. H., et al. (2010) · Neuron · doi:10.1016/j.neuron.2010.11.008 · Cited by 263 · see citing works

International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function

Barnes, N. M., Ahern, G. P., Bécamel, C., Bockaert, J., Camilleri, M., Chaumont‐Dubel, S., Claeysen, S., Cunningham, K. A., Fone, K. C. F., Gershon, M. D., et al. (2020) · Pharmacological Reviews · doi:10.1124/pr.118.015552 · Cited by 264 · see citing works

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

Keov, P., Sexton, P. M., & Christopoulos, A. (2010) · Neuropharmacology · doi:10.1016/j.neuropharm.2010.07.010 · Cited by 265 · see citing works

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

Conn, P. J., Lindsley, C. W., Meiler, J., & Niswender, C. M. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4308 · Cited by 259 · see citing works

Allostery at G Protein-Coupled Receptor Homo- and Heteromers: Uncharted Pharmacological Landscapes

Smith, N. J., & Milligan, G. (2010) · Pharmacological Reviews · doi:10.1124/pr.110.002667 · Cited by 261 · see citing works

Differential hydrogen/deuterium exchange mass spectrometry analysis of protein–ligand interactions

Chalmers, M. J., Busby, S. A., Pascal, B. D., West, G. M., & Griffin, P. R. (2011) · Expert Review of Proteomics · doi:10.1586/epr.10.109 · Cited by 255 · see citing works

Parkinson's Disease Therapeutics: New Developments and Challenges Since the Introduction of Levodopa

Smith, Y., Wichmann, T., Factor, S. A., & DeLong, M. R. (2011) · Neuropsychopharmacology · doi:10.1038/npp.2011.212 · Cited by 246 · see citing works

International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands

Christopoulos, A., Changeux, J., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R. R., Pin, J., et al. (2014) · Pharmacological Reviews · doi:10.1124/pr.114.008862 · Cited by 238 · see citing works

A Selective Allosteric Potentiator of the M 1 Muscarinic Acetylcholine Receptor Increases Activity of Medial Prefrontal Cortical Neurons and Restores Impairments in Reversal Learning

Shirey-Rice, J. K., Brady, A. E., Jones, P. J., Davis, A. A., Bridges, T. M., Kennedy, J. P., Jadhav, S. B., Menon, U. N., Xiang, Z., Watson, M. L., et al. (2009) · Journal of Neuroscience · doi:10.1523/jneurosci.3930-09.2009 · Cited by 237 · see citing works

Structural Modifications that Alter the P-Glycoprotein Efflux Properties of Compounds

Hitchcock, S. A. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201136z · Cited by 230 · see citing works

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

Melancon, B. J., Hopkins, C. R., Wood, M. R., Emmitte, K. A., Niswender, C. M., Christopoulos, A., Conn, P. J., & Lindsley, C. W. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm201139r · Cited by 230 · see citing works

Development of allosteric modulators of GPCRs for treatment of CNS disorders

Nickols, H. H., & Conn, P. J. (2013) · Neurobiology of Disease · doi:10.1016/j.nbd.2013.09.013 · Cited by 227 · see citing works

Muscarinic and Nicotinic Acetylcholine Receptor Agonists and Allosteric Modulators for the Treatment of Schizophrenia

Jones, C. K., Byun, N. E., & Bubser, M. (2011) · Neuropsychopharmacology · doi:10.1038/npp.2011.199 · Cited by 228 · see citing works

Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders

Foster, D. J., & Conn, P. J. (2017) · Neuron · doi:10.1016/j.neuron.2017.03.016 · Cited by 227 · see citing works

Quantifying Correlations Between Allosteric Sites in Thermodynamic Ensembles

McClendon, C. L., Friedland, G. D., Mobley, D. L., Amirkhani, H., & Jacobson, M. P. (2009) · Journal of Chemical Theory and Computation · doi:10.1021/ct9001812 · Cited by 227 · see citing works

Advances in G Protein-Coupled Receptor Allostery: From Function to Structure

Christopoulos, A. (2014) · Molecular Pharmacology · doi:10.1124/mol.114.094342 · Cited by 224 · see citing works

The Significance of G Protein-Coupled Receptor Crystallography for Drug Discovery

Salon, J. A., Lodowski, D. T., & Palczewski, K. (2011) · Pharmacological Reviews · doi:10.1124/pr.110.003350 · Cited by 221 · see citing works

Progress in Structure Based Drug Design for G Protein-Coupled Receptors

Congreve, M., LANGMEAD, C. J., Mason, J. S., & Marshall, F. H. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm200371q · Cited by 213 · see citing works

Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery

Slosky, L. M., Caron, M. G., & Barak, L. S. (2021) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2020.12.005 · Cited by 214 · see citing works

Molecular mechanism of the sweet taste enhancers

Zhang, F., Klebansky, B., Fine, R., Liu, H., Xu, H., Servant, G., Zoller, M. J., Tachdjian, C., & Li, X. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0911660107 · Cited by 207 · see citing works

Allosteric Modulation of Family C G-Protein-Coupled Receptors: from Molecular Insights to Therapeutic Perspectives

Urwyler, S. (2011) · Pharmacological Reviews · doi:10.1124/pr.109.002501 · Cited by 207 · see citing works

mGluR5 Positive Allosteric Modulators Facilitate both Hippocampal LTP and LTD and Enhance Spatial Learning

Ayala, J. E., Chen, Y., Banko, J. L., Sheffler, D. J., Williams, R. D., Telk, A. N., Watson, N. L., Xiang, Z., Zhang, Y., Jones, P. J., et al. (2009) · Neuropsychopharmacology · doi:10.1038/npp.2009.30 · Cited by 206 · see citing works

Novel Allosteric Modulators of G Protein-coupled Receptors

Gentry, P. R., Sexton, P. M., & Christopoulos, A. (2015) · Journal of Biological Chemistry · doi:10.1074/jbc.r115.662759 · Cited by 199 · see citing works

Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CB2 Receptors

Martínez‐Pinilla, E., Varani, K., Reyes‐Resina, I., Angelats, E., Vincenzi, F., Ferreiro‐Vera, C., Oyarzábal, J., Canela, E. I., Lanciego, J. L., Nadal, X., et al. (2017) · Frontiers in Pharmacology · doi:10.3389/fphar.2017.00744 · Cited by 200 · see citing works

DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo

Thompson, K. J., Khajehali, E., Bradley, S. J., Navarrete, J. S., Huang, X., Slocum, S. T., Jin, J. J., Liu, J., Xiong, Y., Olsen, R. H. J., et al. (2018) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.8b00012 · Cited by 195 · see citing works

Protein-protein interaction modulators: advances, successes and remaining challenges

Mabonga, L., & Kappo, A. P. (2019) · Biophysical Reviews · doi:10.1007/s12551-019-00570-x · Cited by 196 · see citing works

Exciting Times beyond the Brain: Metabotropic Glutamate Receptors in Peripheral and Non-Neural Tissues

Julio‐Pieper, M., Flor, P. J., Dinan, T. G., & Cryan, J. F. (2011) · Pharmacological Reviews · doi:10.1124/pr.110.004036 · Cited by 184 · see citing works

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

Lindsley, C. W., Emmitte, K. A., Hopkins, C. R., Bridges, T. M., Gregory, K. J., Niswender, C. M., & Conn, P. J. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.5b00656 · Cited by 183 · see citing works

ASD: a comprehensive database of allosteric proteins and modulators

Huang, Z., Zhu, L., Cao, Y., Wu, G. G., Liu, X., Chen, Y., Wang, Q., Shi, T., Zhao, Y., Wang, Y., et al. (2010) · Nucleic Acids Research · doi:10.1093/nar/gkq1022 · Cited by 177 · see citing works

An allosteric modulator to control endogenous G protein-coupled receptors with light

Pittolo, S., Gómez‐Santacana, X., Eckelt, K., Rovira, X., Dalton, J. A. R., Goudet, C., Pin, J., Llobet, A., Giraldo, J., Llebaria, A., et al. (2014) · Nature Chemical Biology · doi:10.1038/nchembio.1612 · Cited by 180 · see citing works

Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

Rodriguez, A. L., Grier, M. D., Jones, C. K., Herman, E. J., Kane, A. S., Smith, R. L., Williams, R. D., Zhou, Y., Marlo, J. E., Days, E., et al. (2010) · Molecular Pharmacology · doi:10.1124/mol.110.067207 · Cited by 178 · see citing works

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Schreiber, S. L., Kotz, J., Li, M., Aubé, J., Austin, C. P., Reed, J. C., Rosen, H., White, E. L., Sklar, L. A., Lindsley, C. W., et al. (2015) · Cell · doi:10.1016/j.cell.2015.05.023 · Cited by 168 · see citing works

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

Valant, C., Lane, J. R., Sexton, P. M., & Christopoulos, A. (2011) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010611-134514 · Cited by 169 · see citing works

Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties

Leach, K., Loiacono, R. E., Felder, C. C., McKinzie, D. L., Mogg, A. J., Shaw, D. B., Sexton, P. M., & Christopoulos, A. (2009) · Neuropsychopharmacology · doi:10.1038/npp.2009.194 · Cited by 167 · see citing works

The chemistry and biological activity of heterocycle-fused quinolinone derivatives: A review

Shiro, T., Fukaya, T., & Tobe, M. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.12.004 · Cited by 167 · see citing works

Computational design of peptide ligands

Vanhee, P., van der Sloot, A. M., Verschueren, E., Serrano, L. G., Rousseau, F., & Schymkowitz, J. W. H. (2011) · Trends in biotechnology · doi:10.1016/j.tibtech.2011.01.004 · Cited by 167 · see citing works

Cannabinoid receptors: nomenclature and pharmacological principles

Console‐Bram, L., Marcu, J. P., & Abood, M. E. (2012) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/j.pnpbp.2012.02.009 · Cited by 162 · see citing works

Structure-Based Virtual Screening for Ligands of G Protein–Coupled Receptors: What Can Molecular Docking Do for You?

Ballante, F., Kooistra, A. J., Kampen, S., de Graaf, C., & Carlsson, J. (2021) · Pharmacological Reviews · doi:10.1124/pharmrev.120.000246 · Cited by 160 · see citing works

Two Distinct Determinants of Ligand Specificity in T1R1/T1R3 (the Umami Taste Receptor)

Toda, Y., Nakagita, T., Hayakawa, T., Okada, S., Narukawa, M., Imai, H., Ishimaru, Y., & Misaka, T. (2013) · Journal of Biological Chemistry · doi:10.1074/jbc.m113.494443 · Cited by 159 · see citing works

Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts

Wold, E. A., Chen, J., Cunningham, K. A., & Zhou, J. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00875 · Cited by 158 · see citing works

Kappa-opioid ligands in the study and treatment of mood disorders

Carlezon, W. A., Béguin, C., Knoll, A. T., & Cohen, B. M. (2009) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2009.05.008 · Cited by 156 · see citing works

The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery

Robertson, N. J., Jazayeri, A., Errey, J. C., Baig, A. H., Hurrell, E., Zhukov, A., Langmead, C. J., Weir, M., & Marshall, F. H. (2010) · Neuropharmacology · doi:10.1016/j.neuropharm.2010.07.001 · Cited by 157 · see citing works

Focusing on Adenosine Receptors as a Potential Targeted Therapy in Human Diseases

Effendi, W. I., Nagano, T., Kobayashi, K., & Nishimura, Y. (2020) · Cells · doi:10.3390/cells9030785 · Cited by 157 · see citing works

Metabotropic glutamate receptor-4 modulates adaptive immunity and restrains neuroinflammation

Fallarino, F., Volpi, C., Fazio, F., Notartomaso, S., Vacca, C., Busceti, C. L., Bicciato, S., Battaglia, G., Bruno, V., Puccetti, P., et al. (2010) · Nature Medicine · doi:10.1038/nm.2183 · Cited by 155 · see citing works

Pathway and Mechanism of Drug Binding to G-Protein-Coupled Receptors

Dror, R. O., Pan, A. C., Arlow, D. H., Borhani, D. W., Maragakis, P., Shan, Y., Xu, H., & Shaw, D. E. (2012) · Biophysical Journal · doi:10.1016/j.bpj.2011.11.2241 · Cited by 155 · see citing works

Exploring the role of receptor flexibility in structure-based drug discovery

Feixas, F., Lindert, S., Sinko, W., & McCammon, J. A. (2014) · Biophysical Chemistry · doi:10.1016/j.bpc.2013.10.007 · Cited by 156 · see citing works

“Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology

Wood, M. R., Hopkins, C. R., Brogan, J. T., Conn, P. J., & Lindsley, C. W. (2011) · Biochemistry · doi:10.1021/bi200129s · Cited by 154 · see citing works

Label-free whole-cell assays: expanding the scope of GPCR screening

Scott, C. W., & Peters, M. F. (2010) · Drug Discovery Today · doi:10.1016/j.drudis.2010.06.008 · Cited by 151 · see citing works

Probenecid Inhibits the Human Bitter Taste Receptor TAS2R16 and Suppresses Bitter Perception of Salicin

Greene, T. A., Alarcon, S., Thomas, A. A., Berdougo, E., Doranz, B. J., Breslin, P. A. S., & Rucker, J. B. (2011) · PLoS ONE · doi:10.1371/journal.pone.0020123 · Cited by 147 · see citing works

Harnessing Allostery: A Novel Approach to Drug Discovery

Lu, S., Li, S., & Zhang, J. (2014) · Medicinal Research Reviews · doi:10.1002/med.21317 · Cited by 146 · see citing works

M1 muscarinic acetylcholine receptor in Alzheimer’s disease

Jiang, S., Li, Y., Zhang, C., Zhao, Y., Bu, G., Xu, H., & Zhang, Y. (2014) · Neuroscience Bulletin · doi:10.1007/s12264-013-1406-z · Cited by 147 · see citing works

Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity

Marlo, J. E., Niswender, C. M., Days, E., Bridges, T. M., Xiang, Y., Rodriguez, A. L., Shirey-Rice, J. K., Brady, A. E., Nalywajko, T., Luo, Q., et al. (2008) · Molecular Pharmacology · doi:10.1124/mol.108.052886 · Cited by 146 · see citing works

Inhibition of Tumor Angiogenesis and Growth by a Small-Molecule Multi-FGF Receptor Blocker with Allosteric Properties

Bono, F., Smet, F. D., Herbert, C., Bock, K. D., Γεωργιάδου, Μ., Fons, P., Tjwa, M., Alcouffe, C., Ny, A., Bianciotto, M., et al. (2013) · Cancer Cell · doi:10.1016/j.ccr.2013.02.019 · Cited by 146 · see citing works

Muscarinic Acetylcholine Receptor Agonists as Novel Treatments for Schizophrenia

Paul, S. M., Yohn, S. E., Popiolek, M., Miller, A., & Felder, C. C. (2022) · American Journal of Psychiatry · doi:10.1176/appi.ajp.21101083 · Cited by 149 · see citing works

Biased Ligands for Better Cardiovascular Drugs

DeWire, S. M., & Violin, J. D. (2011) · Circulation Research · doi:10.1161/circresaha.110.231308 · Cited by 145 · see citing works

Endogenous Allosteric Modulators of G Protein–Coupled Receptors

van der Westhuizen, E. T., Valant, C., Sexton, P. M., & Christopoulos, A. (2015) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.114.221606 · Cited by 144 · see citing works

Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug–Target Interactions

Lu, S., & Zhang, J. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01844 · Cited by 144 · see citing works

Allo-network drugs: harnessing allostery in cellular networks

Nussinov, R., Tsai, C., & Csermely, P. (2011) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2011.08.004 · Cited by 143 · see citing works

Accelerated molecular dynamics simulations of ligand binding to a muscarinic G-protein-coupled receptor

Kappel, K., Miao, Y., & McCammon, J. A. (2015) · Quarterly Reviews of Biophysics · doi:10.1017/s0033583515000153 · Cited by 143 · see citing works

Regulation of β2-Adrenergic Receptor Function by Conformationally Selective Single-Domain Intrabodies

Staus, D. P., Wingler, L. M., Strachan, R. T., Rasmussen, S. G. F., Pardon, E., Ahn, S., Steyaert, J., Kobilka, B. K., & Lefkowitz, R. J. (2013) · Molecular Pharmacology · doi:10.1124/mol.113.089516 · Cited by 142 · see citing works

Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and Gi Protein-independent ERK1/2 Kinase Activation

Ahn, K. H., Mahmoud, M. M., & Kendall, D. A. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.316463 · Cited by 141 · see citing works

The Role of a Sodium Ion Binding Site in the Allosteric Modulation of the A2A Adenosine G Protein-Coupled Receptor

Gutiérrez‐de‐Terán, H., Massink, A., Rodriguez, D. J., Liu, W., Han, G. W., Joseph, J. S., Katritch, I., Heitman, L. H., Xia, L., IJzerman, A. P., et al. (2013) · Structure · doi:10.1016/j.str.2013.09.020 · Cited by 141 · see citing works

Muscarinic receptor subtype distribution in the central nervous system and relevance to aging and Alzheimer's disease

Lebois, E. P., Thorn, C. A., Edgerton, J. R., Popiolek, M., & Xi, S. (2017) · Neuropharmacology · doi:10.1016/j.neuropharm.2017.11.018 · Cited by 141 · see citing works

Norbin Is an Endogenous Regulator of Metabotropic Glutamate Receptor 5 Signaling

Wang, H., Westin, L., Nong, Y., Birnbaum, S. G., Bendor, J., Brismar, H., Nestler, E. J., Aperia, A. C., Flajolet, M., & Greengard, P. (2009) · Science · doi:10.1126/science.1178496 · Cited by 140 · see citing works

The Different Ways through Which Specificity Works in Orthosteric and Allosteric Drugs

Nussinov, R., & Tsai, C. (2012) · Current Pharmaceutical Design · doi:10.2174/138161212799436377 · Cited by 139 · see citing works

Positive allosteric modulators of the human sweet taste receptor enhance sweet taste

Servant, G., Tachdjian, C., Tang, X.-Q., Werner, S., Zhang, F., Li, X., Kamdar, P., Petrovic, G., Ditschun, T. L., Java, A., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0911670107 · Cited by 139 · see citing works

Development of allosteric modulators of GPCRs for treatment of CNS disorders

Nickols, H. H., & Conn, P. J. (2013) · Neurobiology of Disease · doi:10.1016/j.nbd.2013.09.013 · Cited by 227 · see citing works

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

Conn, P. J., Lindsley, C. W., Meiler, J., & Niswender, C. M. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4308 · Cited by 259 · see citing works

Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders

Foster, D. J., & Conn, P. J. (2017) · Neuron · doi:10.1016/j.neuron.2017.03.016 · Cited by 227 · see citing works

Allosteric modulators in CNS disorders: review

Sebastian, R. (2018) · Journal of Psychology & Clinical Psychiatry · doi:10.15406/jpcpy.2018.09.00592

Allosteric Modulation of G Protein-Coupled Receptors: An Emerging Approach of Drug Discovery.

Wild, C., Cunningham, K. A., & Zhou, J. (2014) · PubMed · Cited by 20 · see citing works