Ontology highlight
ABSTRACT:
SUBMITTER: Choi SS
PROVIDER: S-EPMC5314706 | biostudies-literature | 2016 Apr
REPOSITORIES: biostudies-literature
Choi Sun-Sil SS Kim Eun-Sun ES Jung Ji-Eun JE Marciano David P DP Jo Ala A Koo Ja Young JY Choi Soo Youn SY Yang Yong Ryoul YR Jang Hyun-Jun HJ Kim Eung-Kyun EK Park Jiyoung J Kwon Hyug Moo HM Lee In Hee IH Park Seung Bum SB Myung Kyung-Jae KJ Suh Pann-Ghill PG Griffin Patrick R PR Choi Jang Hyun JH
Diabetes 20160106 4
Blocking phosphorylation of peroxisome proliferator-activated receptor (PPAR)γ at Ser(273) is one of the key mechanisms for antidiabetes drugs to target PPARγ. Using high-throughput phosphorylation screening, we here describe that Gleevec blocks cyclin-dependent kinase 5-mediated PPARγ phosphorylation devoid of classical agonism as a PPARγ antagonist ligand. In high fat-fed mice, Gleevec improved insulin sensitivity without causing severe side effects associated with other PPARγ-targeting drugs. ...[more]