Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders

Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease

Niswender, C. M., & Conn, P. J. (2010) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.011008.145533 · Cited by 1,889 · see citing works

Structural diversity of G protein-coupled receptors and significance for drug discovery

Lagerström, M. C., & Schiöth, H. B. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2518 · Cited by 1,489 · see citing works

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

Jeffrey Conn, P., Christopoulos, A., & Lindsley, C. W. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2760 · Cited by 1,063 · 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

Allosteric Modulation of G Protein–Coupled Receptors

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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

Pharmacodynamics of the Type II Calcimimetic Compound Cinacalcet HCl

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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

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

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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

LY354740 is a Potent and Highly Selective Group II Metabotropic Glutamate Receptor Agonist in Cells Expressing Human Glutamate Receptors

Schoepp, D. D., Johnson, B. G., Wright, R. A., Salhoff, C. R., Mayne, N. G., Wu, S., Cockerham, S. L., Burnett, J. P., BELEGAJE, R., Bleakman, D., et al. (1997) · Neuropharmacology · doi:10.1016/s0028-3908(96)00160-8 · Cited by 225 · 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

G-Protein-Coupled Receptors: From Classical Modes of Modulation to Allosteric Mechanisms

Bridges, T. M., & Lindsley, C. W. (2008) · ACS Chemical Biology · doi:10.1021/cb800116f · 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

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

“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

Structure and ligand recognition of class C GPCRs

Chun, L., Zhang, W., & Liu, J. (2012) · Acta Pharmacologica Sinica · doi:10.1038/aps.2011.186 · Cited by 136 · see citing works

In Vitro Pharmacological Characterization of Novel Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists

Suzuki, G., Tsukamoto, N., Fushiki, H., Kawagishi, A., Nakamura, M., Kurihara, H., Mitsuya, M., Ohkubo, M., & Ohta, H. (2007) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.107.124701 · Cited by 132 · see citing works

‘7TM Receptor Allostery: Putting Numbers to Shapeshifting Proteins

Kenakin, T. (2009) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2009.06.007 · Cited by 126 · 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

The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with l-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson’s Disease

Jones, C. K., Bubser, M., Thompson, A. D., Dickerson, J. W., Turle-Lorenzo, N., Amalric, M., Blobaum, A. L., Bridges, T. M., Morrison, R. D., Jadhav, S. B., et al. (2011) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.187443 · Cited by 104 · see citing works

A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential

Goudet, C., Vilar, B., Courtiol, T., Deltheil, T., Bessiron, T., Brabet, I., Oueslati, N., Rigault, D., Bertrand, H., McLean, H., et al. (2012) · The FASEB Journal · doi:10.1096/fj.11-195941 · Cited by 96 · see citing works

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

Sharma, S., Rodriguez, A. L., Conn, P. J., & Lindsley, C. W. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.05.091 · Cited by 86 · see citing works

In utero exposure to cocaine delays postnatal synaptic maturation of glutamatergic transmission in the VTA

Bellone, C., Mameli, M., & Lüscher, C. (2011) · Nature Neuroscience · doi:10.1038/nn.2930 · Cited by 84 · see citing works

Allosteric modulation of kinases and GPCRs: design principles and structural diversity

Lewis, J. A., Lebois, E. P., & Lindsley, C. W. (2008) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2008.02.014 · Cited by 71 · see citing works

Recent Advances in the Design and Development of Novel Negative Allosteric Modulators of mGlu5

Emmitte, K. A. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn2000266 · Cited by 70 · see citing works

Deleterious GRM1 Mutations in Schizophrenia

Ayoub, M. A., Angelicheva, D., Vile, D., Chandler, D., Morar, B., Cavanaugh, J. A., Visscher, P. M., Jablensky, A. V., Pfleger, K. D. G., & Kalaydjieva, L. V. (2012) · PLoS ONE · doi:10.1371/journal.pone.0032849 · Cited by 70 · 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

Improved Bioavailability of the mGlu2/3 Receptor Agonist LY354740 Using a Prodrug Strategy: In Vivo Pharmacology of LY544344

Rorick‐Kehn, L. M., Perkins, E. J., Knitowski, K. M., Hart, J. C., Johnson, B. G., Schoepp, D. D., & McKinzie, D. L. (2006) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.091926 · Cited by 66 · see citing works

Clustered Coding Variants in the Glutamate Receptor Complexes of Individuals with Schizophrenia and Bipolar Disorder

Frank, R. A. W., McRae, A. F., Pocklington, A. J., van de Lagemaat, L. N., Navarro, P., Croning, M. D. R., Komiyama, N. H., Bradley, S. J., Challiss, R. A. J., Armstrong, J. D., et al. (2011) · PLoS ONE · doi:10.1371/journal.pone.0019011 · Cited by 65 · see citing works

Progress toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5)

Stauffer, S. R. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn2000519 · Cited by 58 · see citing works

Recent Progress in the Synthesis and Characterization of Group II Metabotropic Glutamate Receptor Allosteric Modulators

Sheffler, D. J., Pinkerton, A. B., Dahl, R. S., Markou, A., & Cosford, N. D. P. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn200008d · Cited by 49 · see citing works

Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges

Duvoisin, R. M., Villasana, L., Davis, M. J., Winder, D. G., & Raber, J. (2011) · Behavioural Brain Research · doi:10.1016/j.bbr.2011.02.049 · Cited by 40 · see citing works

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM

Sheffler, D. J., Wenthur, C. J., Bruner, J. A., Carrington, S. J. S., Vinson, P. N., Gogi, K. K., Blobaum, A. L., Morrison, R. D., Vamos, M., Cosford, N. D. P., et al. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.04.112 · Cited by 40 · see citing works

Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics

Robichaud, A. J., Engers, D. W., Lindsley, C. W., & Hopkins, C. R. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn200043e · Cited by 38 · see citing works

Discovery of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 (mGluR5)

Williams, D., Jr., & Lindsley, C. W. (2005) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026054750290 · Cited by 36 · see citing works

Recent Advances in the Medicinal Chemistry of the Metabotropic Glutamate Receptor 1 (mGlu1)

Owen, D. R. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn2000124 · Cited by 30 · see citing works

AMN082, an allosteric mGluR7 agonist that inhibits afferent glutamatergic transmission in rat basolateral amygdala

Ugolini, A., Large, C. H., & Corsi, M. (2008) · Neuropharmacology · doi:10.1016/j.neuropharm.2008.04.020 · Cited by 26 · see citing works

Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: Unexpected ‘molecular switch’ from a closely related mGlu4 positive allosteric modulator

Utley, T. J., Haddenham, D., Salovich, J. M., Zamorano, R., Vinson, P. N., Lindsley, C. W., Hopkins, C. R., & Niswender, C. M. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.09.131 · Cited by 19 · see citing works

An industrial perspective on positive allosteric modulation as a means to discover safe and selective drugs

Rocheville, M., & Garland, S. L. (2010) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2010.06.004 · Cited by 16 · 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

Recent computational advances in the identification of allosteric sites in proteins

Lu, S., Huang, W., & Zhang, J. (2014) · Drug Discovery Today · doi:10.1016/j.drudis.2014.07.012 · Cited by 102 · see citing works

Effect of Novel Allosteric Modulators of Metabotropic Glutamate Receptors on Drug Self-administration and Relapse: A Review of Preclinical Studies and Their Clinical Implications

Caprioli, D., Justinova, Z., Venniro, M., & Shaham, Y. (2018) · Biological Psychiatry · doi:10.1016/j.biopsych.2017.08.018 · Cited by 55 · see citing works

A novel GABAB receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia

Murai, N., Kondo, Y., Akuzawa, S., Mihara, T., Shiraishi, N., Kakimoto, S., & Matsumoto, M. (2019) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2019.172750 · Cited by 34 · see citing works

G protein-coupled receptor allosteric modulators

Willard, F. S., & Wainscott, D. B. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-816228-6.00014-3

Discovery of ONO-8590580: A novel, potent and selective GABAA α5 negative allosteric modulator for the treatment of cognitive disorders

Lewis, A., Beresford, A. P., Chambers, M. S., et al. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127536 · Cited by 2 · see citing works

Identification and Characterization of the First Selective Y 4 Receptor Positive Allosteric Modulator

Schubert, M., Stichel, J., Du, Y., Tough, I. R., Sliwoski, G. R., Meiler, J., Cox, H. M., Weaver, C. D., & Beck‐Sickinger, A. G. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00976 · Cited by 19 · see citing works

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

Jörg, M., van der Westhuizen, E. T., Khajehali, E., Burger, W. A. C., White, J. M., Choy, K. H. C., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., et al. (2018) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.8b00613 · Cited by 11 · see citing works

An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor

Liu, X., Kaindl, J. M., Korczynska, M., Stößel, A., Dengler, D. G., Stanek, M., Hübner, H., Clark, M. J., Mahoney, J., Matt, R. A., et al. (2020) · Nature Chemical Biology · doi:10.1038/s41589-020-0549-2 · Cited by 79 · see citing works