In silico design of novel probes for the atypical opioid receptor MRGPRX2
Open accessAbstract
The primate-exclusive MRGPRX2 G protein-coupled receptor (GPCR) has been suggested to modulate pain and itch. Despite putative peptide and small-molecule MRGPRX2 agonists, selective nanomolar-potency probes have not yet been reported. To identify a MRGPRX2 probe, we first screened 5,695 small molecules and found that many opioid compounds activated MRGPRX2, including (-)- and (+)-morphine, hydrocodone, sinomenine, dextromethorphan, and the prodynorphin-derived peptides dynorphin A, dynorphin B, and α- and β-neoendorphin. We used these to select for mutagenesis-validated homology models and docked almost 4 million small molecules. From this docking, we predicted ZINC-3573-a potent MRGPRX2-selective agonist, showing little activity against 315 other GPCRs and 97 representative kinases-along with an essentially inactive enantiomer. ZINC-3573 activates endogenous MRGPRX2 in a human mast cell line, inducing degranulation and calcium release. MRGPRX2 is a unique atypical opioid-like receptor important for modulating mast cell degranulation, which can now be specifically modulated with ZINC-3573.
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52 non-olfactory GPCRs are categorized as Tdark, and new screening platforms have begun the process of illuminating them.
“Although 52 non-olfactory GPCRs are categorized as Tdark, the availability of new screening platforms to discover chemical matter for these GPCRs has begun the process of illumination64,67,68.”
From Unexplored therapeutic opportunities in the human genome (2018) · cites this paper as [68]
The Abstract describes new physical and computational screening approaches for finding ligands for understudied GPCRs, and the Results report their use to identify compounds active at MRGPRX receptors. That supports the claim that screening platforms have begun to illuminate these receptors. The paper does not give the figure of 52 non-olfactory GPCRs or categorize that group as Tdark; its Abstract instead discusses approximately 120 orphan or understudied non-olfactory GPCRs. (LLM, conf=0.86)
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Cites
ZINC − A Free Database of Commercially Available Compounds for Virtual Screening
Irwin, J. J., & Shoichet, B. K. (2005) · Journal of Chemical Information and Modeling · doi:10.1021/ci049714+ · Cited by 4,058 · see citing works
Self-citationHow many drug targets are there?
Overington, J. P., Al-Lazikani, B., & Hopkins, A. L. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd2199 · Cited by 3,505 · see citing works
Ballesteros, J. A., & Weinstein, H. (1995) · Methods in neurosciences · doi:10.1016/s1043-9471(05)80049-7 · Cited by 3,001 · see citing works
Comparative Protein Structure Modeling Using MODELLER
Eswar, N., Webb, B., Martı́-Renom, M. A., Madhusudhan, M. S., Eramian, D., Shen, M., Pieper, U., & Šali, A. (2007) · Current Protocols in Protein Science · doi:10.1002/0471140864.ps0209s50 · Cited by 2,862 · see citing works
On the Role of the Crystal Environment in Determining Protein Side-chain Conformations
Jacobson, M. P., Friesner, R. A., Xiang, Z., & Honig, B. H. (2002) · Journal of Molecular Biology · doi:10.1016/s0022-2836(02)00470-9 · Cited by 1,289 · see citing works
PROMALS3D: a tool for multiple protein sequence and structure alignments
Pei, J., Kim, B., & Grishin, N. V. (2008) · Nucleic Acids Research · doi:10.1093/nar/gkn072 · Cited by 1,267 · see citing works
Identification of a mast cell specific receptor crucial for pseudo-allergic drug reactions
McNeil, B. D., Pundir, P., Meeker, S., Han, L., Undem, B., Kulka, M., & Dong, X.-Z. (2014) · Nature · doi:10.1038/nature14022 · Cited by 1,164 · see citing works
GPCRdb: an information system for G protein-coupled receptors
Ísberg, V., Mordalski, S., Munk, C., Rataj, K., Harpsøe, K., Hauser, A. S., Vroling, B., Bojarski, A. J., Vriend, G., & Gloriam, D. E. I. (2015) · Nucleic Acids Research · doi:10.1093/nar/gkv1178 · Cited by 1,067 · see citing works
Automated docking with grid‐based energy evaluation
Meng, E. C., Shoichet, B. K., & Kuntz, I. D. (1992) · Journal of Computational Chemistry · doi:10.1002/jcc.540130412 · Cited by 956 · see citing works
Self-citationJordan, M., Schallhorn, A., & Wurm, F. M. (1996) · Nucleic Acids Research · doi:10.1093/nar/24.4.596 · Cited by 862 · see citing works
PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome
Kroeze, W. K., Sassano, M. F., Huang, X.-P., Lansu, K., McCorvy, J. D., Giguère, P. M., Sciaky, N., & Roth, B. L. (2015) · Nature Structural & Molecular Biology · doi:10.1038/nsmb.3014 · Cited by 755 · see citing works
Self-citationA Diverse Family of GPCRs Expressed in Specific Subsets of Nociceptive Sensory Neurons
Dong, X., Han, S.-K., Zylka, M. J., Simon, M. I., & Anderson, D. J. (2001) · Cell · doi:10.1016/s0092-8674(01)00483-4 · Cited by 742 · see citing works
The Repertoire of G-Protein–Coupled Receptors in Fully Sequenced Genomes
Fredriksson, R., & Schiöth, H. B. (2005) · Molecular Pharmacology · doi:10.1124/mol.104.009001 · Cited by 613 · see citing works
Kirshenbaum, A. S., Akin, C., Wu, Y., Rottem, M., Goff, J. P., Beaven, M. A., Rao, V. K., & Metcalfe, D. D. (2003) · Leukemia Research · doi:10.1016/s0145-2126(02)00343-0 · Cited by 513 · see citing works
Hutchinson, M. R., Shavit, Y., Grace, P. M., Rice, K. C., Maier, S. F., & Watkins, L. R. (2011) · Pharmacological Reviews · doi:10.1124/pr.110.004135 · Cited by 397 · see citing works
Proenkephalin A gene products activate a new family of sensory neuron–specific GPCRs
Lembo, P. M. C., Grazzini, E., Groblewski, T., O’Donnell, D., Roy, M., Zhang, J., Hoffert, C., Cao, J., Schmidt, R., Pelletier, M., et al. (2002) · Nature Neuroscience · doi:10.1038/nn815 · Cited by 385 · see citing works
Immunoglobulin E-independent activation of mast cell is mediated by Mrg receptors.
Tatemoto, K., Nozaki, Y., Tsuda, R., Konno, S., Tomura, K., Furuno, M., Ogasawara, H., Edamura, K., Takagi, H., Iwamura, H., et al. (2006) · Biochemical and Biophysical Research Communications - BBRC · doi:10.1016/j.bbrc.2006.08.177 · Cited by 364 · see citing works
Model for Aqueous Solvation Based on Class IV Atomic Charges and First Solvation Shell Effects
Chambers, C. C., Hawkins, G. D., Cramer, C. J., & Truhlar, D. G. (1996) · The Journal of Physical Chemistry · doi:10.1021/jp9610776 · Cited by 360 · see citing works
GPCRDB: an information system for G protein-coupled receptors
Horn, F. (1998) · Nucleic Acids Research · doi:10.1093/nar/26.1.275 · Cited by 338 · see citing works
Rapid Context-Dependent Ligand Desolvation in Molecular Docking
Mysinger, M. M., & Shoichet, B. K. (2010) · Journal of Chemical Information and Modeling · doi:10.1021/ci100214a · Cited by 319 · see citing works
Self-citationHistamine Release during Morphine and Fentanyl Anesthesia
Rosow, C. E., Moss, J., Philbin, D. M., & Savarese, J. J. (1982) · Anesthesiology · doi:10.1097/00000542-198202000-00003 · Cited by 314 · see citing works
Ligand discovery from a dopamine D3 receptor homology model and crystal structure
Carlsson, J., Coleman, R. G., Setola, V., Irwin, J. J., Fan, H., Schlessinger, A., Šali, A., Roth, B. L., & Shoichet, B. K. (2011) · Nature Chemical Biology · doi:10.1038/nchembio.662 · Cited by 305 · see citing works
Self-citationAllosteric ligands for the pharmacologically dark receptors GPR68 and GPR65
Huang, X.-P., Karpiak, J., Kroeze, W. K., Zhu, H., Chen, X., Moy, S. S., Saddoris, K. A., Nikolova, V. D., Farrell, M. S., Wang, S., et al. (2015) · Nature · doi:10.1038/nature15699 · Cited by 284 · see citing works
Self-citationRask-Andersen, M., Masuram, S., & Schiöth, H. B. (2014) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-011613-135943 · Cited by 282 · see citing works
Docking Screens for Novel Ligands Conferring New Biology
Irwin, J. J., & Shoichet, B. K. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b02008 · Cited by 281 · see citing works
Self-citationAtypical expansion in mice of the sensory neuron-specific Mrg G protein-coupled receptor family
Zylka, M. J., Dong, X., Southwell, A. L., & Anderson, D. J. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1732949100 · Cited by 266 · see citing works
New Class IV Charge Model for Extracting Accurate Partial Charges from Wave Functions
Li, J., Zhu, T., Cramer, C. J., & Truhlar, D. G. (1998) · The Journal of Physical Chemistry A · doi:10.1021/jp972682r · Cited by 260 · see citing works
MrgX2 Is a High Potency Cortistatin Receptor Expressed in Dorsal Root Ganglion
Robas, N. M., Mead, E. J., & Fidock, M. D. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m302456200 · Cited by 250 · see citing works
Strategies to Discover Unexpected Targets for Drugs Active at G Protein–Coupled Receptors
Allen, J. A., & Roth, B. L. (2011) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010510-100553 · Cited by 216 · see citing works
Self-citationDiscovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases
Paruch, K., Dwyer, M. P., Alvarez, C., Brown, C., Chan, T., Doll, R. J., Keertikar, K. M., Knutson, C. E., McKittrick, B. A., Rivera, J., et al. (2010) · ACS Medicinal Chemistry Letters · doi:10.1021/ml100051d · Cited by 184 · see citing works
Southern, C., Cook, J. M., Neetoo‐Isseljee, Z., Taylor, D. L., Kettleborough, C. A., Merritt, A. T., Bassoni, D. L., Raab, W. J., Quinn, E. R., Wehrman, T. S., et al. (2013) · SLAS DISCOVERY · doi:10.1177/1087057113475480 · Cited by 181 · see citing works
Neuraxial opioid-induced pruritus: An update
Kumar, K., & Singh, S. (2013) · Journal of Anaesthesiology Clinical Pharmacology · doi:10.4103/0970-9185.117045 · Cited by 177 · see citing works
New insights from structural biology into the druggability of G protein-coupled receptors
Mason, J. S., Bortolato, A., Congreve, M., & Marshall, F. H. (2012) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2012.02.005 · Cited by 171 · see citing works
Histamine-Releasing and Allergenic Properties of Opioid Analgesic Drugs: Resolving the Two
Baldo, B. A., & Pham, N. H. (2012) · Anaesthesia and Intensive Care · doi:10.1177/0310057x1204000204 · Cited by 170 · see citing works
Jacquet, Y. F., Klee, W. A., Rice, K. C., Iijima, I., & Minamikawa, J. (1977) · Science · doi:10.1126/science.199942 · Cited by 165 · see citing works
β-Defensins Activate Human Mast Cells via Mas-Related Gene X2
Subramanian, H., Gupta, K., Lee, D., Bayir, A., Ahn, H., & Ali, H. (2013) · The Journal of Immunology · doi:10.4049/jimmunol.1300023 · Cited by 146 · see citing works
Determining the Neurotransmitter Concentration Profile at Active Synapses
Scimemi, A., & Beato, M. (2009) · Molecular Neurobiology · doi:10.1007/s12035-009-8087-7 · Cited by 145 · see citing works
Identification of Novel Functionally Selective κ-Opioid Receptor Scaffolds
White, K. L., Scopton, A. P., Rives, M., Bikbulatov, R. V., Polepally, P. R., Brown, P. J., Kenakin, T., Javitch, J. A., Zjawiony, J. K., & Roth, B. L. (2013) · Molecular Pharmacology · doi:10.1124/mol.113.089649 · Cited by 142 · see citing works
Self-citationMast Cell/Nerve Interactions In Vitro and In Vivo
Bienenstock, J., MacQUEEN, G. M., Sestini, P., Marshall, J. S., Stead, R. H., & Perdue, M. H. (1991) · American Review of Respiratory Disease · doi:10.1164/ajrccm/143.3_pt_2.s55 · Cited by 138 · see citing works
Pharmacology of sinomenine, an anti-rheumatic alkaloid from Sinomenium acutum.
Yamasaki, H. (1976) · PubMed · Cited by 136 · see citing works
Structure-based ligand discovery for the protein–protein interface of chemokine receptor CXCR4
Mysinger, M. M., Weiss, D. R., Ziarek, J. J., Gravel, S., Doak, A. K., Karpiak, J. D., Heveker, N., Shoichet, B. K., & Volkman, B. F. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1120431109 · Cited by 129 · see citing works
Self-citationSharp, K. A. (1995) · Biopolymers · doi:10.1002/bip.360360210 · Cited by 117 · see citing works
Kamohara, M., Matsuo, A., Takasaki, J., Kohda, M., Matsumoto, M., Matsumoto, S., Soga, T., Hiyama, H., Kobori, M., & Katou, M. (2005) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2005.03.088 · Cited by 110 · see citing works
A pharmacological organization of G protein–coupled receptors
Lin, H., Sassano, M. F., Roth, B. L., & Shoichet, B. K. (2013) · Nature Methods · doi:10.1038/nmeth.2324 · Cited by 103 · see citing works
Self-citationNMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor
O’Connor, C., White, K. L., Doncescu, N., Didenko, T., Roth, B. L., Czaplicki, G., Stevens, R. C., Kurt Wüthrich, A., & Milon, A. (2015) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1510117112 · Cited by 96 · see citing works
Self-citationIdentifying ligands at orphan GPCRs: current status using structure‐based approaches
Ngo, T., Kufareva, I., Coleman, J. L. J., Graham, R. M., Abagyan, R. A., & Smith, N. J. (2016) · British Journal of Pharmacology · doi:10.1111/bph.13452 · Cited by 87 · see citing works
The Recognition of Identical Ligands by Unrelated Proteins
Barelier, S., Sterling, T., O’Meara, M. J., & Shoichet, B. K. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00683 · Cited by 74 · see citing works
Self-citationThe Emerging Role of Spinal Dynorphin in Chronic Pain: A Therapeutic Perspective
Podvin, S., Yaksh, T. L., & HOOK, V. Y. H. (2016) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010715-103042 · Cited by 56 · see citing works
Ísberg, V., Andersen, K. B., Bisig, C., Dietz, G. P. H., Bräuner‐Osborne, H., & Gloriam, D. E. I. (2014) · Journal of Chemical Information and Modeling · doi:10.1021/ci500197a · Cited by 56 · see citing works
Minocycline prevents dynorphin-induced neurotoxicity during neuropathic pain in rats
Rojewska, E., Makuch, W., Przewłocka, B., & Mika, J. (2014) · Neuropharmacology · doi:10.1016/j.neuropharm.2014.08.001 · Cited by 52 · see citing works
The pharmacological profile of δ opioid receptor ligands, (+) and (−) TAN-67 on pain modulation
Nagase, H., Yajima, Y., Fujii, H., Kawamura, K., Narita, M., Kamei, J., & Suzuki, T. (2001) · Life Sciences · doi:10.1016/s0024-3205(01)01010-4 · Cited by 49 · see citing works
Self-citationSweetnam, P. M., Neale, J. H., Barker, J. L., & D, A. G. M. (1982) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.79.21.6742 · Cited by 45 · see citing works
Activation of opioid μ-receptor by sinomenine in cell and mice
Wang, M. H., Chang, C.-K., Cheng, J.-H., Wu, H., Li, Y.-X., & Cheng, J. (2008) · Neuroscience Letters · doi:10.1016/j.neulet.2008.07.088 · Cited by 36 · see citing works
Malik, L., Kelly, N. M., Ma, J., Currier, E. A., Burstein, E. S., & Olsson, R. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.01.085 · Cited by 29 · see citing works
Staats, H. F., Kirwan, S. M., Choi, H. W., Shelburne, C. P., Abraham, S. N., Leung, G. Y. C., & Chen, D. Y. ‐. (2012) · MedChemComm · doi:10.1039/c2md20073b · Cited by 24 · see citing works
Building alternate protein structures using the elastic network model
Yang, Q., & Sharp, K. A. (2008) · Proteins Structure Function and Bioinformatics · doi:10.1002/prot.22184 · Cited by 23 · see citing works
Preliminary Pharmacological Evaluation of Enantiomeric Morphinans
Sromek, A. W., Provencher, B. A., Russell, S. E., Chartoff, E. H., Knapp, B. I., Bidlack, J. M., & Neumeyer, J. L. (2014) · ACS Chemical Neuroscience · doi:10.1021/cn400205z · Cited by 21 · see citing works
Complanadine A, a selective agonist for the Mas-related G protein-coupled receptor X2
Johnson, T., & Siegel, D. R. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.05.060 · Cited by 20 · see citing works
Wu, H.-E., Schwasinger, E. T., Terashvili, M., & Tseng, L. F. (2007) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2007.01.083 · Cited by 17 · see citing works
Morphine is an exogenous ligand for MrgX2, a G protein-coupled receptor for cortistatin
Akuzawa, N., Obinata, H., Izumi, T., & Takeda, S. (2009) · Journal of Cell and Animal Biology · doi:10.5897/jcab.9000110 · Cited by 13 · see citing works
Jacobson, M. P. (2002) · Current Treatment Options in Neurology · doi:10.1007/s11940-002-0002-8 · Cited by 5 · see citing works
[Recreational usage of dextromethorphan--analysis based on internet users experiences].
Zając, M., Andrzejczyk, A. P., Kuich, A., Tyrańska-Fobke, A., Waldman, W., & Anand, J. S. (2013) · PubMed · Cited by 4 · see citing works
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- [52]Kirshenbaum AS Characterization of novel stem cell factor responsive human mast cell lines LAD 1 and 2 established from a patient with mast cell sarcoma/leukemia; activation following aggregation of FcepsilonRI or FcgammaRI Leuk Res 27 677 82 2003 12801524
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How Ligands Illuminate GPCR Molecular Pharmacology
Wacker, D., Stevens, R. C., & Roth, B. L. (2017) · Cell · doi:10.1016/j.cell.2017.07.009 · Cited by 560 · see citing works
Self-citationA practical guide to large-scale docking
Bender, B. J., Gahbauer, S., Luttens, A., Lyu, J., Webb, C. M., Stein, R. M., Fink, E. A., Balius, T. E., Carlsson, J., Irwin, J. J., et al. (2021) · Nature Protocols · doi:10.1038/s41596-021-00597-z · Cited by 546 · see citing works
Self-citationThe Art and Science of Molecular Docking
Paggi, J. M., Pandit, A., & Dror, R. O. (2024) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-030222-120000 · Cited by 511 · see citing works
Unexplored therapeutic opportunities in the human genome
Oprea, T. I., Bologa, C. G., Brunak, S., Campbell, A., Gan, G. N., Gaulton, A., Gomez, S. M., Guha, R., Hersey, A., Holmes, J., et al. (2018) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2018.14 · Cited by 378 · see citing works
Self-citationHouse dust mites activate nociceptor–mast cell clusters to drive type 2 skin inflammation
Serhan, N., Basso, L., Sibilano, R., Petitfils, C., Meixiong, J., Bonnart, C., Reber, L. L., Marichal, T., Starkl, P. M., Cénac, N., et al. (2019) · Nature Immunology · doi:10.1038/s41590-019-0493-z · Cited by 347 · see citing works
Erratum: Unexplored therapeutic opportunities in the human genome
Oprea, T. I., Bologa, C., Brunak, S., Campbell, A., Gan, G. N., Gaulton, A., Gomez, S. M., Guha, R., Hersey, A., Holmes, J., et al. (2018) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2018.52 · Cited by 304 · see citing works
Self-citationVirtual discovery of melatonin receptor ligands to modulate circadian rhythms
Stein, R. M., Kang, H. J., McCorvy, J. D., Glatfelter, G. C., Jones, A., Che, T., Slocum, S. T., Huang, X., Savych, O., Moroz, Y. S., et al. (2020) · Nature · doi:10.1038/s41586-020-2027-0 · Cited by 306 · see citing works
Self-citationPhysiology and Pathophysiology of Itch
Cevikbas, F., & Lerner, E. A. (2019) · Physiological Reviews · doi:10.1152/physrev.00017.2019 · Cited by 284 · see citing works
D4dopamine receptor high-resolution structures enable the discovery of selective agonists
Wang, S., Wacker, D., Levit, A., Che, T., Betz, R. M., McCorvy, J. D., Venkatakrishnan, A., Huang, X., Dror, R. O., Shoichet, B. K., et al. (2017) · Science · doi:10.1126/science.aan5468 · Cited by 263 · see citing works
Self-citationBespoke library docking for 5-HT2A receptor agonists with antidepressant activity
Kaplan, A. L., Confair, D. N., Kim, K., Barros-Álvarez, X., Rodriguiz, R. M., Ying, Y., Kweon, O. S., Che, T., McCorvy, J. D., Kamber, D. N., et al. (2022) · Nature · doi:10.1038/s41586-022-05258-z · Cited by 249 · see citing works
Self-citationStructure, function and pharmacology of human itch GPCRs
Cao, C., Kang, H. J., Singh, I., Chen, H., Zhang, C., Ye, W., Hayes, B. W., Liu, J., Gumpper, R. H., Bender, B. J., et al. (2021) · Nature · doi:10.1038/s41586-021-04126-6 · Cited by 236 · see citing works
Self-citationMas-Related G Protein-Coupled Receptor-X2 (MRGPRX2) in Drug Hypersensitivity Reactions
Porębski, G., Kwiecień, K., Pawica, M., & Kwitniewski, M. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2018.03027 · Cited by 191 · see citing works
Multifaceted MRGPRX2: New insight into the role of mast cells in health and disease
Roy, S., Ayudhya, C. C. N., Thapaliya, M., Deepak, V., & Ali, H. (2021) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2021.03.049 · Cited by 178 · see citing works
Structure, function and pharmacology of human itch receptor complexes
Yang, F., Guo, L., Li, Y., Wang, G., Wang, J., Zhang, C., Fang, G.-X., Chen, X., Liu, L., Yan, X., et al. (2021) · Nature · doi:10.1038/s41586-021-04077-y · Cited by 144 · see citing works
Meixiong, J., Vasavda, C., Snyder, S. H., & Dong, X. (2019) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1903316116 · Cited by 162 · see citing works
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
MRGPRX2-mediated mast cell response to drugs used in perioperative procedures and anaesthesia
Navinés‐Ferrer, A., Serrano‐Candelas, E., Lafuente, A., Muñoz‐Cano, R., Martı́n, M., & Gastaminza, G. (2018) · Scientific Reports · doi:10.1038/s41598-018-29965-8 · Cited by 160 · see citing works
Comparative epidemiology of suspected perioperative hypersensitivity reactions
Mertès, P., Ebo, D. G., Garcez, T. P., Rose, M. A., Sabato, V., Takazawa, T., Cooke, P., Clarke, R. C., Dewachter, P., Garvey, L. H., et al. (2019) · British Journal of Anaesthesia · doi:10.1016/j.bja.2019.01.027 · Cited by 153 · see citing works
Human mast cells and basophils—How are they similar how are they different?
Varricchi, G., Raap, U., Rivellese, F., Marone, G., & Gibbs, B. F. (2018) · Immunological Reviews · doi:10.1111/imr.12627 · Cited by 151 · see citing works
Mas-related G protein–coupled receptor X2 and its activators in dermatologic allergies
Kühn, H., Kolkhir, P., Babina, M., Düll, M. M., Frischbutter, S., Fok, J. S., Jiao, Q., Metz, M., Scheffel, J., Wolf, K., et al. (2020) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2020.08.027 · Cited by 138 · see citing works
Property-Unmatched Decoys in Docking Benchmarks
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Meyrath, M., Szpakowska, M., Zeiner, J., Massotte, L., Merz, M. P., Benkel, T., Simon, K., Ohnmacht, J., Turner, J. D., Krüger, R., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-16664-0 · Cited by 130 · see citing works
Biased ligands at opioid receptors: Current status and future directions
Che, T., Dwivedi‐Agnihotri, H., Shukla, A. K., & Roth, B. L. (2021) · Science Signaling · doi:10.1126/scisignal.aav0320 · Cited by 125 · see citing works
Self-citationMolecular basis of opioid receptor signaling
Che, T., & Roth, B. L. (2023) · Cell · doi:10.1016/j.cell.2023.10.029 · Cited by 123 · see citing works
Self-citationMRGPRX2 and Adverse Drug Reactions
McNeil, B. D. (2021) · Frontiers in Immunology · doi:10.3389/fimmu.2021.676354 · Cited by 117 · see citing works
Kumar, M., Duraisamy, K., & Chow, B. (2021) · Cells · doi:10.3390/cells10051033 · Cited by 113 · see citing works
Heterogeneity of Human Mast Cells With Respect to MRGPRX2 Receptor Expression and Function
Varricchi, G., Pecoraro, A., Loffredo, S., Poto, R., Rivellese, F., Genovese, A., Marone, G., & Spadaro, G. (2019) · Frontiers in Cellular Neuroscience · doi:10.3389/fncel.2019.00299 · Cited by 111 · see citing works
Ebo, D. G., Clarke, R. C., Mertès, P., Platt, P. R., Sabato, V., & Sadleir, P. H. M. (2019) · British Journal of Anaesthesia · doi:10.1016/j.bja.2019.01.031 · Cited by 110 · see citing works
Discovery of new GPCR ligands to illuminate new biology
Roth, B. L., Irwin, J. J., & Shoichet, B. K. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2490 · Cited by 94 · see citing works
Self-citationVEGAS as a Platform for Facile Directed Evolution in Mammalian Cells
English, J. G., Olsen, R. H. J., Lansu, K., Patel, M., White, K., Cockrell, A. S., Singh, D., Strachan, R. T., Wacker, D., & Roth, B. L. (2019) · Cell · doi:10.1016/j.cell.2019.05.051 · Cited by 98 · see citing works
Self-citationChen, E., Chuang, L.-S. F., Giri, M., Villaverde, N., Hsu, N.-Y., Sabic, K., Joshowitz, S., Gettler, K., Nayar, S., Chai, Z., et al. (2021) · Gastroenterology · doi:10.1053/j.gastro.2020.12.076 · Cited by 100 · see citing works
Mast Cell-Specific MRGPRX2: a Key Modulator of Neuro-Immune Interaction in Allergic Diseases
Thapaliya, M., Ayudhya, C. C. N., Amponnawarat, A., Roy, S., & Ali, H. (2021) · Current Allergy and Asthma Reports · doi:10.1007/s11882-020-00979-5 · Cited by 95 · see citing works
The transcriptional program, functional heterogeneity, and clinical targeting of mast cells
Cildir, G., Pant, H., Lopez, A. F., & Tergaonkar, V. (2017) · The Journal of Experimental Medicine · doi:10.1084/jem.20170910 · Cited by 94 · see citing works
Nonantimicrobial Actions of Macrolides: Overview and Perspectives for Future Development
Kricker, J. A., Page, C. P., Gardarsson, F. R., Baldursson, Ó., Guðjónsson, Þ., & Parnham, M. J. (2021) · Pharmacological Reviews · doi:10.1124/pharmrev.121.000300 · Cited by 92 · see citing works
Therapeutic Potential of MRGPRX2 Inhibitors on Mast Cells
Ogasawara, H., & Noguchi, M. (2021) · Cells · doi:10.3390/cells10112906 · Cited by 87 · see citing works
Neurotransmitter and neuropeptide regulation of mast cell function: a systematic review
Xu, H., Shi, X., Li, X., Zou, J.-X., Zhou, C., Liu, W., Shao, H., Chen, H., & Shi, L. (2020) · Journal of Neuroinflammation · doi:10.1186/s12974-020-02029-3 · Cited by 87 · see citing works
Alkanfari, I., Gupta, K., Jahan, T., & Ali, H. (2018) · Journal of Immunology · doi:10.4049/jimmunol.1701793 · Cited by 80 · see citing works
In Vitro Diagnosis of Immediate Drug Hypersensitivity During Anesthesia: A Review of the Literature
Ebo, D. G., Faber, M. A., Elst, J., Gasse, A. L. V., Bridts, C. H., Mertens, C. H., Clerck, L. S. D., Hagendorens, M. M., & Sabato, V. (2018) · The Journal of Allergy and Clinical Immunology In Practice · doi:10.1016/j.jaip.2018.01.004 · Cited by 80 · see citing works
Osthole, a Natural Plant Derivative Inhibits MRGPRX2 Induced Mast Cell Responses
Callahan, B. N., Kammala, A. K., Syed, M., Yang, C., Occhiuto, C. J., Nellutla, R., Chumanevich, A. P., Oskeritzian, C. A., Das, R., & Subramanian, H. (2020) · Frontiers in Immunology · doi:10.3389/fimmu.2020.00703 · Cited by 78 · see citing works
New roles and controls of mast cells
Espinosa, É., & Valitutti, S. (2017) · Current Opinion in Immunology · doi:10.1016/j.coi.2017.10.012 · Cited by 78 · see citing works
Role of mast cells and basophils in pruritus
Steinhoff, M. S., Buddenkotte, J., & Lerner, E. A. (2018) · Immunological Reviews · doi:10.1111/imr.12635 · Cited by 78 · see citing works
Quercetin inhibits Mrgprx2-induced pseudo-allergic reaction via PLCγ-IP3R related Ca2+ fluctuations
Ding, Y., Che, D., Li, C., Cao, J., Wang, J., Ma, P., Zhao, T., An, H., & Zhang, T. (2018) · International Immunopharmacology · doi:10.1016/j.intimp.2018.11.025 · Cited by 76 · see citing works
Mechanisms of human drug-induced anaphylaxis
Bruhns, P., & Chollet‐Martin, S. (2021) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2021.02.013 · Cited by 76 · see citing works
Ayudhya, C. C. N., Roy, S., Alkanfari, I., Ganguly, A., & Ali, H. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20215247 · Cited by 74 · see citing works
Takazawa, T., Sabato, V., & Ebo, D. G. (2019) · British Journal of Anaesthesia · doi:10.1016/j.bja.2019.01.002 · Cited by 73 · see citing works
MRGPRX2 is essential for sinomenine hydrochloride induced anaphylactoid reactions
Liu, R., Che, D., Zhao, T., Pundir, P., Cao, J., Lv, Y., Wang, J., Ma, P., Fu, J., Wang, N., et al. (2017) · Biochemical Pharmacology · doi:10.1016/j.bcp.2017.09.017 · Cited by 71 · see citing works
Korczynska, M., Clark, M. J., Valant, C., Xu, J. Z., Moo, E. V., Albold, S., Weiss, D. R., Torosyan, H., Huang, W., Kruse, A. C., et al. (2018) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1718037115 · Cited by 71 · see citing works
Self-citationIntrathecal Drug Delivery: Advances and Applications in the Management of Chronic Pain Patient
Andrés, J. A. D., Hayek, S. M., Perruchoud, C., Lawrence, M. M., Reina, M. Á., Andrés-Serrano, C. D., Rubio-Haro, R., Hunt, M. A., & Yaksh, T. L. (2022) · Frontiers in Pain Research · doi:10.3389/fpain.2022.900566 · Cited by 72 · see citing works
Wang, N., Che, D., Zhang, T., Liu, R., Cao, J., Wang, J., Zhao, T., Ma, P., Dong, X., & He, L. (2017) · Biochemical Pharmacology · doi:10.1016/j.bcp.2017.12.017 · Cited by 70 · see citing works
Ali, H. (2017) · Advances in immunology · doi:10.1016/bs.ai.2017.06.002 · Cited by 69 · see citing works
Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs
Roth, B. L. (2019) · Nature Structural & Molecular Biology · doi:10.1038/s41594-019-0252-8 · Cited by 68 · see citing works
Self-citationMast cell disorders: From infancy to maturity
Wilcock, A., Bahri, R., Bulfone‐Paus, S., & Arkwright, P. D. (2018) · Allergy · doi:10.1111/all.13657 · Cited by 68 · see citing works
Hamwi, G. A., Riedel, Y. K., Clemens, S., Namasivayam, V., Thimm, D., & Müller, C. E. (2022) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2022.108259 · Cited by 66 · see citing works
Ogasawara, H., Furuno, M., Edamura, K., & Noguchi, M. (2019) · Journal of Leukocyte Biology · doi:10.1002/jlb.2ab1018-405r · Cited by 66 · see citing works
The Interplay between Chronic Pain, Opioids, and the Immune System
Malafoglia, V., Ilari, S., Vitiello, L., Tenti, M., Balzani, E., Muscoli, C., Raffaeli, W., & Bonci, A. (2021) · The Neuroscientist · doi:10.1177/10738584211030493 · Cited by 63 · see citing works
Receptor structure-based discovery of non-metabolite agonists for the succinate receptor GPR91
Trauelsen, M., Ulven, E. R., Hjorth, S. A., Brvar, M., Monaco, C. G., Frimurer, T. M., & Schwartz, T. W. (2017) · Molecular Metabolism · doi:10.1016/j.molmet.2017.09.005 · Cited by 63 · see citing works
Kolkhir, P., Pyatilova, P., Ashry, T., Jiao, Q., Abad‐Perez, A. T., Altrichter, S., Vera, C., Church, M. K., He, J., Lohse, K., et al. (2022) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2022.02.021 · Cited by 63 · see citing works
Wang, Z., & Babina, M. (2020) · Experimental Dermatology · doi:10.1111/exd.14182 · Cited by 63 · see citing works
Grimes, J., Desai, S. D., Charter, N. W., Lodge, J., Santos, R. M., Isidro‐Llobet, A., Mason, A. M., Wu, Z., Wolfe, L. A., Anantharaman, L., et al. (2019) · Pharmacology Research & Perspectives · doi:10.1002/prp2.547 · Cited by 59 · see citing works
Babina, M., Wang, Z., Roy, S., Guhl, S., Franke, K., Artuc, M., Ali, H., & Zuberbier, T. (2020) · Journal of Investigative Dermatology · doi:10.1016/j.jid.2020.09.017 · Cited by 55 · see citing works
The MRGPR family of receptors in immunity
Gour, N., & Dong, X. (2024) · Immunity · doi:10.1016/j.immuni.2023.12.012 · Cited by 58 · see citing works
Zheng, M., Zhao, J., Cui, C., Fu, Z., Li, X., Liu, X., Ding, X., Tan, X., Li, F., Luo, X., et al. (2018) · Medicinal Research Reviews · doi:10.1002/med.21483 · Cited by 53 · see citing works
A group of cationic amphiphilic drugs activates MRGPRX2 and induces scratching behavior in mice
Wolf, K., Kühn, H., Boehm, F., Gebhardt, L., Glaudo, M., Agelopoulos, K., Ständer, S., Ectors, P., Zahn, D., Riedel, Y. K., et al. (2021) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2020.12.655 · Cited by 53 · see citing works
The structure, function, and pharmacology of MRGPRs
Cao, C., & Roth, B. L. (2023) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2023.02.002 · Cited by 57 · see citing works
Self-citationMast cell-mediated hypersensitivity to fluoroquinolone is MRGPRX2 dependent
Liu, R., Hu, S., Zhang, Y., Che, D., Cao, J., Wang, J., Zhao, T., Jia, Q., Wang, N., & Zhang, T. (2019) · International Immunopharmacology · doi:10.1016/j.intimp.2019.02.001 · Cited by 53 · see citing works
Morphine acts on spinal dynorphin neurons to cause itch through disinhibition
Nguyen, E. K., Lim, G., Ding, H., Hachisuka, J., Ko, M., & Ross, S. E. (2021) · Science Translational Medicine · doi:10.1126/scitranslmed.abc3774 · Cited by 53 · see citing works
Mast cell activation tests by flow cytometry: A new diagnostic asset?
Elst, J., van der Poorten, M. M., Gasse, A. L. V., Puysseleyr, L. P. D., Hagendorens, M. M., Faber, M. A., Houdt, M. V., Passante, E., Bahri, R., Walschot, M., et al. (2021) · Clinical & Experimental Allergy · doi:10.1111/cea.13984 · Cited by 52 · see citing works
A single amino acid in MRGPRX2 necessary for binding and activation by pruritogens
Reddy, V. B., Graham, T. A., Azimi, E., & Lerner, E. A. (2017) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2017.05.046 · Cited by 51 · see citing works
Structural Insights Accelerate the Discovery of Opioid Alternatives
Che, T., & Roth, B. L. (2021) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-061620-044044 · Cited by 51 · see citing works
Self-citationDrug Hypersensitivity Reactions
Dykewicz, M. S., & Lam, J. K. (2019) · Medical Clinics of North America · doi:10.1016/j.mcna.2019.09.003 · Cited by 50 · see citing works
Bawazir, M., Amponnawarat, A., Hui, Y. Y., Oskeritzian, C. A., & Ali, H. (2022) · Frontiers in Immunology · doi:10.3389/fimmu.2022.1033794 · Cited by 49 · see citing works
Cisatracurium induces mast cell activation and pseudo-allergic reactions via MRGPRX2
Che, D., Liu, R., Cao, J., Wang, J., Zhang, Y., Ding, Y., Zhao, T., Ma, P., An, H., Gao, Z., et al. (2018) · International Immunopharmacology · doi:10.1016/j.intimp.2018.07.020 · Cited by 49 · see citing works
Roy, S., Ganguly, A., Haque, M., & Ali, H. (2019) · The Journal of Immunology · doi:10.4049/jimmunol.1801227 · Cited by 49 · see citing works
MRGPRX2 and Immediate Drug Hypersensitivity: Insights From Cultured Human Mast Cells
Elst, J., Sabato, V., Faber, M. A., Bridts, C. H., Mertens, C. H., Houdt, M. V., Gasse, A. L. V., Hagendorens, M. M., Tendeloo, V. F. V., Maurer, M., et al. (2020) · Journal of Investigational Allergology and Clinical Immunology · doi:10.18176/jiaci.0557 · Cited by 48 · see citing works
Store-Operated Calcium Entry via STIM1 Contributes to MRGPRX2 Induced Mast Cell Functions
Occhiuto, C. J., Kammala, A. K., Yang, C., Nellutla, R., Garcia, M., Gomez, G., & Subramanian, H. (2020) · Frontiers in Immunology · doi:10.3389/fimmu.2019.03143 · Cited by 48 · see citing works
Ayudhya, C. C. N., Amponnawarat, A., & Ali, H. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22105318 · Cited by 47 · see citing works
Novel small molecule MRGPRX2 antagonists inhibit a murine model of allergic reaction
Kumar, M., Duraisamy, K., Annapureddy, R. R., Chan, C. B., & Chow, B. (2022) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2022.12.805 · Cited by 47 · see citing works
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets
Weiss, D. R., Karpiak, J. D., Huang, X., Sassano, M. F., Lyu, J., Roth, B. L., & Shoichet, B. K. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00718 · Cited by 45 · see citing works
Self-citationRocuronium Hypersensitivity: Does Off-Target Occupation of the MRGPRX2 Receptor Play a Role?
Gasse, A. L. V., Elst, J., Bridts, C. H., Mertens, C. H., Faber, M. A., Hagendorens, M. M., Clerck, L. S. D., Sabato, V., & Ebo, D. G. (2018) · The Journal of Allergy and Clinical Immunology In Practice · doi:10.1016/j.jaip.2018.09.034 · Cited by 45 · see citing works
Babina, M., Wang, Z., Franke, K., & Zuberbier, T. (2021) · Cells · doi:10.3390/cells10010102 · Cited by 45 · see citing works
Ayudhya, C. C. N., Amponnawarat, A., Roy, S., Oskeritzian, C. A., & Ali, H. (2021) · Cells · doi:10.3390/cells10010156 · Cited by 44 · see citing works
Suzuki, Y., Liu, S., Ogasawara, T., Sawasaki, T., Takasaki, Y., Yorozuya, T., & Mogi, M. (2020) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2020.173104 · Cited by 43 · see citing works
Baldo, B. A. (2023) · British Journal of Clinical Pharmacology · doi:10.1111/bcp.15845 · Cited by 42 · see citing works
Wang, J., Zhang, Y., Li, C., Ding, Y., Hu, S., & An, H. (2019) · Phytomedicine · doi:10.1016/j.phymed.2019.153149 · Cited by 41 · see citing works
Paeoniflorin inhibits MRGPRX2‐mediated pseudo‐allergic reaction via calcium signaling pathway
Wang, J., Zhang, Y., Wang, J., Liu, R., Zhang, G., Dong, K., & Zhang, T. (2019) · Phytotherapy Research · doi:10.1002/ptr.6531 · Cited by 40 · see citing works
A humanized mouse model to study mast cells mediated cutaneous adverse drug reactions
Mencarelli, A., Gunawan, M., Yong, K. S. M., Bist, P., Tan, W. W. S., Tan, S. Y., Liu, M., Huang, E. K., Fan, Y., Chan, J. K. Y., et al. (2020) · Journal of Leukocyte Biology · doi:10.1002/jlb.3ma1219-210rr · Cited by 39 · see citing works
Human Mast Cell Line HMC1 Expresses Functional Mas-Related G-Protein Coupled Receptor 2
Hermans, M. A. W., van Stigt, A. C., van de Meerendonk, S., Schrijver, B., van Daele, P. L. A., van Hagen, P. M., van Splunter, M. E., & Dik, W. A. (2021) · Frontiers in Immunology · doi:10.3389/fimmu.2021.625284 · Cited by 36 · see citing works
Lactic acid suppresses MRGPRX2 mediated mast cell responses
Syed, M., Kammala, A. K., Callahan, B. N., Oskeritzian, C. A., & Subramanian, H. (2021) · Cellular Immunology · doi:10.1016/j.cellimm.2021.104422 · Cited by 36 · see citing works
Redhu, D., Franke, K., Aparicio‐Soto, M., Kumari, V., Pažur, K., Illerhaus, A., Hartmann, K., Worm, M., & Babina, M. (2022) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2022.01.029 · Cited by 36 · see citing works
Mas-related G protein-coupled receptor MRGPRX2 in human basophils: Expression and functional studies
Toscano, A., Elst, J., Gasse, A. L. V., Beyens, M. M. J., van der Poorten, M. M., Bridts, C. H., Mertens, C. H., Houdt, M. V., Hagendorens, M. M., Remoortel, S. V., et al. (2023) · Frontiers in Immunology · doi:10.3389/fimmu.2022.1026304 · Cited by 35 · see citing works
Orphan G protein-coupled receptors: the ongoing search for a home
Jobe, A., & Vijayan, R. (2024) · Frontiers in Pharmacology · doi:10.3389/fphar.2024.1349097 · Cited by 35 · see citing works
Sabato, V., Ebo, D. G., van der Poorten, M. M., Toscano, A., Gasse, A. L. V., Mertens, C. H., Houdt, M. V., Beyens, M. M. J., & Elst, J. (2022) · The Journal of Allergy and Clinical Immunology In Practice · doi:10.1016/j.jaip.2022.12.014 · Cited by 35 · see citing works
Jia, Q., Sun, W., Zhang, L., Fu, J., Lv, Y., Lin, Y., & Han, S. (2019) · Journal of Separation Science · doi:10.1002/jssc.201900114 · Cited by 34 · see citing works
Anti-Allergic Effects of Quercetin and Quercetin Liposomes in RBL-2H3 Cells
Zhang, Y., Guan, R., & Huang, H. (2022) · Endocrine Metabolic & Immune Disorders - Drug Targets · doi:10.2174/1871530322666220627151830 · Cited by 33 · see citing works
Non–IgE-Mediated Immediate Drug-Induced Hypersensitivity Reactions
Arango, S. A., Kumar, M., Chow, T. G., & Sabato, V. (2024) · The Journal of Allergy and Clinical Immunology In Practice · doi:10.1016/j.jaip.2024.02.019 · Cited by 33 · see citing works
An African-specific haplotype in MRGPRX4 is associated with menthol cigarette smoking
Kozlitina, J., Risso, D. S., Lansu, K., Olsen, R. H. J., Sainz, E., Luiselli, D., Barik, A., Domingues, C. E. F., Pagani, L., Wooding, S., et al. (2019) · PLoS Genetics · doi:10.1371/journal.pgen.1007916 · Cited by 33 · see citing works
Self-citationMeyrath, M., Palmer, C. B., Reynders, N., Vanderplasschen, A. F. C., Ollert, M. W., Bouvier, M., Szpakowska, M., & Chevigné, A. (2021) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.1c00006 · Cited by 34 · see citing works
Atypical opioid receptors: unconventional biology and therapeutic opportunities
Palmer, C. B., Meyrath, M., Canals, M., Kostenis, E., Chevigné, A., & Szpakowska, M. (2021) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2021.108014 · Cited by 33 · see citing works
Melo, H., Basso, L., Iftinca, M., MacNaughton, W. K., Hollenberg, M. D., McKay, D. M., & Altier, C. (2018) · Scientific Reports · doi:10.1038/s41598-018-33620-7 · Cited by 32 · see citing works
- Authors
- Lansu, K., Karpiak, J., Liu, J., Huang, X.-P., McCorvy, J. D., Kroeze, W. K., Che, T., Nagase, H., Carroll, F. I., Jin, J., Shoichet, B. K., & Roth, B. L.
- Affiliations
- University of North Carolina at Chapel Hill (US)
- University of California, San Francisco (US)
- Icahn School of Medicine at Mount Sinai (US)
- University of Tsukuba (JP)
- RTI International (US)
- Corresponding author
- Roth, Bryan L
- ORCID
- Venue
- Nature Chemical Biology
- Published
- 2017-03-13
- Volume
- 13
- Issue
- 5
- Pages
- 529-536
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- PMC
- PMC5391270
- OpenAlex
- W2595605857
- Cited by
- 293
- References
- 62
- Citations by year
- 2026: 14 · 2025: 36 · 2024: 18 · 2023: 28 · 2022: 30 · 2021: 56 · 2020: 36 · 2019: 35 · 2018: 27 · 2017: 13
- FWCI
- 23.16
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature Chemical Biology (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- eScholarship (California Digital Library) (submittedVersion)
- Funders
- National Institute of Mental Health (U19MH082441, U01MH104974)
- National Institute on Drug Abuse (P01DA035764)
- National Institute of General Medical Sciences (T32GM007040)
- National Institute of Diabetes and Digestive and Kidney Diseases (U24DK116195)
- Topics
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Immunology and Microbiology › Immunology › Mast cells and histamine
- Keywords
- MRGPRX2, G protein-coupled receptors, opioid receptors, chemical probes, dynorphin, mast cell degranulation, calcium release, morphine, sinomenine, dextromethorphan, homology model, molecular docking, pruritus, pain modulation
- MeSH terms
- Calcium, Cell Line, Computer Simulation, Dose-Response Relationship, Drug, Drug Evaluation, Preclinical, Humans, Ligands, Mast Cells, Nerve Tissue Proteins, Pyrazoles, Pyrimidines, Structure-Activity Relationship, Drug Design, Molecular Probes, Molecular Structure, Cell Degranulation, Receptors, Neuropeptide, Receptors, G-Protein-Coupled, Molecular Docking Simulation
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