Estimation of ligand affinity constants for receptor states in functional studies involving the allosteric modulation of G protein-coupled receptors: Implications for ligand bias

Journal of Pharmacological and Toxicological Methods

Volumn 69, Issue 3, 2014, Pages 253-279

  Ehlert, Frederick J ^a,b   Griffin, Michael T ^a,b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b CHAPMAN UNIVERSITY   (United States)

Author keywords

Affinity modulation; Agonist bias; Allosterism; Constitutive activity; Efficacy modulation; Ligand bias; Monod Wyman Changeux; Muscarinic receptor; Probe dependence; Receptor states

Indexed keywords

G PROTEIN COUPLED RECEPTOR; LIGAND;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; COMPLEX FORMATION; CRYSTAL STRUCTURE; ISOMERIZATION; LIGAND BINDING; MOLECULAR INTERACTION; PROTEIN DETERMINATION; PROTEIN EXPRESSION; PROTEIN FUNCTION; RECEPTOR BINDING; RECEPTOR DOWN REGULATION; SENSITIVITY ANALYSIS; SIGNAL TRANSDUCTION; COMPUTER SIMULATION; HUMAN; INVERSE AGONISM; METABOLISM; PHYSIOLOGY; VALIDATION STUDY;

ALLOSTERIC REGULATION; COMPUTER SIMULATION; DRUG INVERSE AGONISM; HUMANS; LIGANDS; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION;

EID: 84896383220     PISSN: 10568719     EISSN: 1873488X     Source Type: Journal    
DOI: 10.1016/j.vascn.2014.01.002     Document Type: Article

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