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The use of GPCR structures in drug design.
Congreve M, Langmead C, Marshall FH. Congreve M, et al. Adv Pharmacol. 2011;62:1-36. doi: 10.1016/B978-0-12-385952-5.00011-7. Adv Pharmacol. 2011. PMID: 21907905 Review.
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. Christopher JA, et al. J Med Chem. 2015 Aug 27;58(16):6653-64. doi: 10.1021/acs.jmedchem.5b00892. Epub 2015 Aug 12. J Med Chem. 2015. PMID: 26225459
Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.
Christopher JA, Orgován Z, Congreve M, Doré AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keserű GM. Christopher JA, et al. J Med Chem. 2019 Jan 10;62(1):207-222. doi: 10.1021/acs.jmedchem.7b01722. Epub 2018 Mar 1. J Med Chem. 2019. PMID: 29455526
840 results