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Original Article

GPCR Drug Discovery Through the Exploitation of Allosteric Drug Binding Sites

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Pages 261-268 | Published online: 04 Dec 2011

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Read on this site (8)

Rumin Zhang & Michael Kavana. (2015) Quantitative analysis of receptor allosterism and its implication for drug discovery. Expert Opinion on Drug Discovery 10:7, pages 763-780.
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Darren R Flower. (2012) Systematic identification of small molecule adjuvants. Expert Opinion on Drug Discovery 7:9, pages 807-817.
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Luigi Francesco Agnati, Diego Guidolin, Giuseppina Leo, Michele Guescini, Marina Pizzi, Vilberto Stocchi, Pier Francesco Spano, Roberta Ghidoni, Francisco Ciruela, Susanna Genedani & Kjell Fuxe. (2011) Possible new targets for GPCR modulation: allosteric interactions, plasma membrane domains, intercellular transfer and epigenetic mechanisms. Journal of Receptors and Signal Transduction 31:5, pages 315-331.
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Terry Kenakin. (2010) G protein coupled receptors as allosteric proteins and the role of allosteric modulators. Journal of Receptors and Signal Transduction 30:5, pages 313-321.
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Terry Kenakin. (2009) Interrogating 7TM receptors: Does texture in the question yield greater texture in the answer?. Journal of Receptors and Signal Transduction 29:3-4, pages 132-139.
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TERRY KENAKIN. (2008) Functional Assays as Prismatic Views of Drug Activity: Relevance to New Drug Discovery. Journal of Receptors and Signal Transduction 28:1-2, pages 109-125.
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DJ McLoughlin, F Bertelli & C Williams. (2007) The A, B, Cs of G-protein-coupled receptor pharmacology in assay development for HTS. Expert Opinion on Drug Discovery 2:5, pages 603-619.
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TERRY KENAKIN. (2007) Allosteric Agonist Modulators. Journal of Receptors and Signal Transduction 27:4, pages 247-259.
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Terry Kenakin. 2022. GPCRs as Therapeutic Targets. GPCRs as Therapeutic Targets 60 80 .
Jingchen Zhai, Xibing He, Yuchen Sun, Zhuoya Wan, Beihong Ji, Shuhan Liu, Song Li & Junmei Wang. (2022) In silico binding affinity prediction for metabotropic glutamate receptors using both endpoint free energy methods and a machine learning-based scoring function . Physical Chemistry Chemical Physics.
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Aman Chandra Kaushik, Shakti Sahi & Dong-Qing Wei. 2022. Computational Methods for Estimating the Kinetic Parameters of Biological Systems. Computational Methods for Estimating the Kinetic Parameters of Biological Systems 161 174 .
Xiao-Chen Yuan & Ya-Xiong Tao. (2018) Fenoprofen—An Old Drug Rediscovered as a Biased Allosteric Enhancer for Melanocortin Receptors. ACS Chemical Neuroscience 10:3, pages 1066-1074.
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Yuna Jung, Hyeim Jung & Dongbin Lim. (2015) Bacteriophage membrane protein P9 as a fusion partner for the efficient expression of membrane proteins in Escherichia coli. Protein Expression and Purification 116, pages 12-18.
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Claudia Mugnaini, Valentina Pedani, Angelo Casu, Carla Lobina, Alberto Casti, Paola Maccioni, Alessandra Porcu, Daniela Giunta, Stefania Lamponi, Maurizio Solinas, Stefania Dragoni, Massimo Valoti, Giancarlo Colombo, Maria Paola Castelli, Gian Luigi Gessa & Federico Corelli. (2013) Synthesis and Pharmacological Characterization of 2-(Acylamino)thiophene Derivatives as Metabolically Stable, Orally Effective, Positive Allosteric Modulators of the GABA B Receptor . Journal of Medicinal Chemistry 56:9, pages 3620-3635.
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Swapna Bhagwanth, Ram K Mishra & Rodney L Johnson. (2013) Development of peptidomimetic ligands of Pro-Leu-Gly-NH 2 as allosteric modulators of the dopamine D 2 receptor . Beilstein Journal of Organic Chemistry 9, pages 204-214.
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Terry P. Kenakin. (2010) Ligand Detection in the Allosteric World. SLAS Discovery 15:2, pages 119-130.
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Seok-Ki Choi, David Green, Anne Ho, Uwe Klein, Daniel Marquess, Robert Taylor & S. Derek Turner. (2008) Designing Selective, High Affinity Ligands of 5-HT 1D Receptor by Covalent Dimerization of 5-HT 1F Ligands Derived From 4-Fluoro- N -[3-(1-methyl-4-piperidinyl)-1 H -indol-5-yl]benzamide . Journal of Medicinal Chemistry 51:12, pages 3609-3616.
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T Kenakin. (2008) What systems can and can't do. British Journal of Pharmacology 153:5, pages 841-843.
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R A Ross. (2007) Tuning the endocannabinoid system: allosteric modulators of the CB 1 receptor . British Journal of Pharmacology 152:5, pages 565-566.
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Kakon Nag, Naznin Sultana, Akira Kato & Shigehisa Hirose. (2007) Headless splice variant acting as dominant negative calcitonin receptor. Biochemical and Biophysical Research Communications 362:4, pages 1037-1043.
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Lotte Bjerre KnudsenDan KielMin TengCarsten BehrensDilip Bhumralkar, János T. KodraJens J. Holst, Claus B. JeppesenMichael D. JohnsonJohannes Cornelis de JongAnker Steen JorgensenTim Kercher, Jarek Kostrowicki, Peter MadsenPreben H. OlesenJacob S. PetersenFritz PoulsenUlla G. Sidelmann, Jeppe SturisLarry Truesdale, John MayJesper Lau. (2007) Small-molecule agonists for the glucagon-like peptide 1 receptor. Proceedings of the National Academy of Sciences 104:3, pages 937-942.
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Keshava RajagopalErin J. WhalenJonathan D. ViolinJonathan A. StiberPaul B. RosenbergRichard T. PremontThomas M. CoffmanHoward A. Rockman & Robert J. Lefkowitz. (2006) β-Arrestin2-mediated inotropic effects of the angiotensin II type 1A receptor in isolated cardiac myocytes. Proceedings of the National Academy of Sciences 103:44, pages 16284-16289.
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A. Christopoulos, L.T. May, V.A. Avlani & P.M. Sexton. (2004) G-protein-coupled receptor allosterism: the promise and the problem(s). Biochemical Society Transactions 32:5, pages 873-877.
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