Ontology highlight
ABSTRACT:
SUBMITTER: Homan KT
PROVIDER: S-EPMC4621012 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
Homan Kristoff T KT Wu Emily E Cannavo Alessandro A Koch Walter J WJ Tesmer John J G JJ
Molecules (Basel, Switzerland) 20141022 10
G protein-coupled receptor kinases (GRKs) have been implicated in human diseases ranging from heart failure to diabetes. Previous studies have identified several compounds that selectively inhibit GRK2, such as paroxetine and balanol. Far fewer selective inhibitors have been reported for GRK5, a target for the treatment of cardiac hypertrophy, and the mechanism of action of reported compounds is unknown. To identify novel scaffolds that selectively inhibit GRK5, a differential scanning fluoromet ...[more]