Ontology highlight
ABSTRACT:
SUBMITTER: Lindsley CW
PROVIDER: S-EPMC4988345 | biostudies-literature | 2016 Jun
REPOSITORIES: biostudies-literature
Chemical reviews 20160216 11
Allosteric modulation of GPCRs has initiated a new era of basic and translational discovery, filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique conformations of the GPCR that afford fundamentally new receptors, capable of novel pharmacology, unprecedented subtype selectivity, and unique signal bias. This review provides a comprehensive overview of the basics of GPCR allosteric pharmacology, medicinal chemistry, drug metabolism, and validated approaches ...[more]