Ontology highlight
ABSTRACT:
SUBMITTER: Yoshida T
PROVIDER: S-EPMC3681492 | biostudies-literature | 2012 Dec
REPOSITORIES: biostudies-literature
Yoshida Takayuki T Kakegawa Junya J Yamaguchi Takayuki T Hantani Yoshiji Y Okajima Nobuyuki N Sakai Toshiyuki T Watanabe Yoshihiro Y Nakamura Motonao M
Oncotarget 20121201 12
A small molecule compound, JTP-74057/GSK1120212/trametinib, had been discovered as a very potent antiproliferative agent able to induce the accumulation of CDK inhibitor p15INK4b. To conduct its drug development rationally as an anticancer agent, molecular targets of this compound were identified as MEK1/2 using compound-affinity chromatography. It was shown that JTP-74057 directly bound to MEK1 and MEK2 and allosterically inhibited their kinase activities, and that its inhibitory characteristic ...[more]