Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu 5 ) X-ray Structures

Journal of Medicinal Chemistry

Volumn 62, Issue 1, 2019, Pages 207-222

  Christopher, John A ^a   Orgován, Zoltán ^b   Congreve, Miles ^a   Doré, Andrew S ^a   Errey, James C ^a   Marshall, Fiona H ^a   Mason, Jonathan S ^a   Okrasa, Krzysztof ^a   Rucktooa, Prakash ^a   Serrano Vega, Maria J ^a   Ferenczy, György G ^b   Keseru, György M ^b  

^a Heptares Therapeutics Ltd   (United Kingdom)

^b INSTITUTE OF EXPERIMENTAL MEDICINE   (Hungary)

Author keywords

[No Author keywords available]

Indexed keywords

AGENTS AFFECTING PROTEIN METABOLISM; FENOBAM; G PROTEIN COUPLED RECEPTOR; M MPEP; MAVOGLURANT; METABOTROPIC RECEPTOR 5; UNCLASSIFIED DRUG; 3-((2-METHYL-1,3-THIAZOL-4-YL)ETHYNYL)PYRIDINE; IMIDAZOLE DERIVATIVE; INDOLE DERIVATIVE; LIGAND; PYRIDINE DERIVATIVE; THIAZOLE DERIVATIVE; WATER;

ALLOSTERISM; ARTICLE; DRUG PROTEIN BINDING; DRUG STRUCTURE; MOLECULAR DOCKING; X RAY; ALLOSTERIC SITE; CHEMISTRY; DRUG DESIGN; HUMAN; METABOLISM; PROTEIN TERTIARY STRUCTURE; X RAY CRYSTALLOGRAPHY;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; IMIDAZOLES; INDOLES; LIGANDS; MOLECULAR DOCKING SIMULATION; PROTEIN STRUCTURE, TERTIARY; PYRIDINES; RECEPTOR, METABOTROPIC GLUTAMATE 5; THIAZOLES; WATER;

EID: 85059808266     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.7b01722     Document Type: Article

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