BioCentury
ARTICLE | Targets & Mechanisms

Smoother tumor targets

June 30, 2011 7:00 AM UTC

Texas researchers have identified two kinases-GRK2 and CKI-a-that are responsible for phosphorylating smoothened, the central player in the hedgehog signaling pathway.1 The findings could open a new front against the tumor-promoting pathway if sufficiently selective inhibitors can be developed.

Because G protein-coupled receptor kinase 2 (GRK2; GPRK2) and casein kinase 1a (CSNK1A; CKI-a) help bring smoothened (SMO) to a cellular structure in which SMOreceives a proliferative signal, blocking them mightovercome activating mutations in SMO that cause resistance to SMO antagonists...