Ontology highlight
ABSTRACT:
SUBMITTER: Waldschmidt HV
PROVIDER: S-EPMC4890168 | biostudies-literature | 2016 Apr
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20160413 8
G protein-coupled receptors (GPCRs) are central to many physiological processes. Regulation of this superfamily of receptors is controlled by GPCR kinases (GRKs), some of which have been implicated in heart failure. GSK180736A, developed as a Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor, was identified as an inhibitor of GRK2 and co-crystallized in the active site. Guided by its binding pose overlaid with the binding pose of a known potent GRK2 inhibitor, Takeda103A, a library of hybrid ...[more]