[HTML][HTML] Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase
CD Mol, DR Dougan, TR Schneider, RJ Skene… - Journal of Biological …, 2004 - ASBMB
The activity of the c-Kit receptor protein-tyrosine kinase is tightly regulated in normal cells,
whereas deregulated c-Kit kinase activity is implicated in the pathogenesis of human
cancers. The c-Kit juxtamembrane region is known to have an autoinhibitory function;
however the precise mechanism by which c-Kit is maintained in an autoinhibited state is not
known. We report the 1.9-Å resolution crystal structure of native c-Kit kinase in an
autoinhibited conformation and compare it with active c-Kit kinase. Autoinhibited c-Kit is …
whereas deregulated c-Kit kinase activity is implicated in the pathogenesis of human
cancers. The c-Kit juxtamembrane region is known to have an autoinhibitory function;
however the precise mechanism by which c-Kit is maintained in an autoinhibited state is not
known. We report the 1.9-Å resolution crystal structure of native c-Kit kinase in an
autoinhibited conformation and compare it with active c-Kit kinase. Autoinhibited c-Kit is …