BROWSE

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Author

Park, Jiyoung
Molecular Metabolism Laboratory (MML)
Research Interests
  • Obesity, diabetes, adipose tissue, cancer, cancer-associated adipocyte, dermal adipocyte, metabolic memory

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PPAR gamma Antagonist Gleevec Improves Insulin Sensitivity and Promotes the Browning of White Adipose Tissue

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Title
PPAR gamma Antagonist Gleevec Improves Insulin Sensitivity and Promotes the Browning of White Adipose Tissue
Author
Choi, Sun-silKim, Eun-SunJung, Ji-EunMarciano, David P.Jo, AlaKoo, Ja YoungChoi, Soo YounYang, Yong RyoulJang, Hyun-JunKim, Eung-KyunPark, JiyoungKwon, H. MooLee, In HeePark, Seung BumMyung, KyungjaeSuh, Pann-GhillGriffin, Patrick R.Choi, Jang Hyun
Keywords
ACTIVATED-RECEPTOR-GAMMA; IMATINIB-MESYLATE GLEEVEC; BEIGE FAT; IN-VITRO; LIGAND; PHOSPHORYLATION; GLUCOSE; OBESITY; THIAZOLIDINEDIONE; INFLAMMATION
Issue Date
201604
Publisher
AMER DIABETES ASSOC
Citation
DIABETES, v.65, no.4, pp.829 - 839
Abstract
Blocking phosphorylation of peroxisome proliferator–activated receptor (PPAR)γ at Ser273 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. Furthermore, Gleevec reduces lipogenic and gluconeogenic gene expression in liver and ameliorates inflammation in adipose tissues. Interestingly, Gleevec increases browning of white adipose tissue and energy expenditure. Taken together, the results indicate that Gleevec exhibits greater beneficial effects on both glucose/lipid metabolism and energy homeostasis by blocking PPARγ phosphorylation. These data illustrate that Gleevec could be a novel therapeutic agent for use in insulin resistance and type 2 diabetes.
URI
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DOI
http://dx.doi.org/10.2337/db15-1382
ISSN
0012-1797
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