Ontology highlight
ABSTRACT:
SUBMITTER: Bian Y
PROVIDER: S-EPMC9948676 | biostudies-literature | 2020 Nov
REPOSITORIES: biostudies-literature
European journal of medicinal chemistry 20200809
Designing covalent allosteric modulators brings new opportunities to the field of drug discovery towards G-protein-coupled receptors (GPCRs). Targeting an allosteric binding pocket can allow a modulator to have protein subtype selectivity and low drug resistance. Utilizing covalent warheads further enables the modulator to increase the binding potency and extend the duration of action. This review starts with GPCR allosteric modulation to discuss the structural biology of allosteric binding pock ...[more]