Perspective: Implications of Ligand-Receptor Binding Kinetics for Therapeutic Targeting of G Protein-Coupled Receptors.

ABSTRACT: The concept of ligand-receptor binding kinetics has been broadly applied in drug development pipelines focusing on G protein-coupled receptors (GPCRs). The ligand residence time (RT) for a receptor describes how long a ligand-receptor complex exists, and is defined as the reciprocal of the dissociation rate constant (k _off). RT has turned out to be a valuable parameter for GPCR researchers focusing on drug development as a good predictor of in vivo efficacy. The positive correlation between RT and in vivo efficacy has been established for several drugs targeting class A GPCRs (e.g., the neurokinin-1 receptor (NK₁R), the β₂ adrenergic receptor (β₂AR), and the muscarinic 3 receptor (M₃R)) and for drugs targeting clas

SUBMITTER: van der Velden WJC 

PROVIDER: S-EPMC7155193 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature