Ontology highlight
ABSTRACT:
SUBMITTER: Ranjitkar P
PROVIDER: S-EPMC2871157 | biostudies-literature | 2010 Feb
REPOSITORIES: biostudies-literature
Ranjitkar Pratistha P Brock Amanda M AM Maly Dustin J DJ
Chemistry & biology 20100201 2
A number of small-molecule inhibitors have been developed that target the catalytic domains of protein kinases that are not in an active conformation. An inactive form that has been observed in several kinases is the DFG-out conformation. This conformation is characterized by an almost 180 degrees rotation of the conserved Asp-Phe-Gly (DFG) motif in the ATP-binding cleft relative to the active form. However, the sequence and structural determinants that allow a kinase to stably adopt the DFG-out ...[more]