Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs

Trends in Pharmacological Sciences

Volumn 38, Issue 9, 2017, Pages 837-847

  Congreve, Miles ^a   Oswald, Christine ^a   Marshall, Fiona H ^a  

^a Heptares Therapeutics Ltd   (United Kingdom)

Author keywords

allosteric modulator; G protein coupled receptor; structure based drug design; X ray crystallography

Indexed keywords

BENZYLQUINOLONE CARBOXYLIC ACID; CARBOXYLIC ACID; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CXCR4; G PROTEIN COUPLED RECEPTOR; GLUCAGON RECEPTOR ANTAGONIST; LY 2119620; MK 0893; MUSCARINIC M1 RECEPTOR; MUSCARINIC M1 RECEPTOR ANTAGONIST; MUSCARINIC M2 RECEPTOR; MUSCARINIC M2 RECEPTOR ANTAGONIST; MUSCARINIC M3 RECEPTOR; PURINERGIC P2Y1 RECEPTOR; TIOTROPIUM BROMIDE; UNCLASSIFIED DRUG; LIGAND;

ALLOSTERISM; BINDING AFFINITY; BINDING SITE; CRYSTAL STRUCTURE; DRUG BINDING; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; LIGAND BINDING; MOLECULARLY TARGETED THERAPY; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN INTERACTION; PROTEIN STRUCTURE; REVIEW; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; STRUCTURE BASED DRUG DESIGN; AGONISTS; ANTAGONISTS AND INHIBITORS; CHEMISTRY; HUMAN; METABOLISM; X RAY CRYSTALLOGRAPHY;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; LIGANDS; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85021129087     PISSN: 01656147     EISSN: 18733735     Source Type: Journal    
DOI: 10.1016/j.tips.2017.05.010     Document Type: Review

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