PPARγ Antagonist Imatinib Improves Insulin Sensitivity

This article originally appeared here.
Share this content:
PPARγ Antagonist Imatinib Improves Insulin Sensitivity
PPARγ Antagonist Imatinib Improves Insulin Sensitivity

WEDNESDAY, Jan. 13, 2016 (HealthDay News) -- Imatinib (Gleevec) blocks CDK5-mediated peroxisome proliferator-activated receptor γ (PPARγ) phosphorylation as an antagonist ligand, improving insulin sensitivity and promoting browning of white adipose tissue, according to a study published online Jan. 6 in Diabetes.

Sunsil Choi, from the Ulsan National Institute of Science and Technology in South Korea, and colleagues used high throughput phosphorylation screening to describe the mechanism of action of imatinib.

The researchers note that imatinib blocks CDK5-mediated PPARγ phosphorylation acting as a PPARγ antagonist ligand. Imatinib improved insulin sensitivity in high fat-fed mice, without causing severe side effects associated with other PPARγ-targeting drugs. Imatinib was also found to reduce lipogenic and gluconeogenic gene expression in the liver and improved inflammation in adipose tissues. Increased browning of white adipose tissue and energy expenditure were also seen with imatinib.

"Taken together, Gleevec exhibits greater beneficial effects on both glucose/lipid metabolism and energy homeostasis by blocking PPARγ phosphorylation," the authors write. "These data illustrate that Gleevec could be a novel therapeutic agent for use in insulin resistance and type 2 diabetes."

One author was employed by Hyundai Pharm Co.

Abstract
Full Text (subscription or payment may be required)

Share this content:

is free, fast, and customized just for you!




Already a member?

Sign In Now »

Trending Activities

All Professions

Drug Lookup

Browse drugs by: BrandGenericDisease

More in Home

NIH Panel Will No Longer Review Gene Therapy Experiments

NIH Panel Will No Longer Review Gene Therapy ...

FDA will now assess gene therapy experiments and products as it does with other treatments, drugs

Doctors Remove Contact Lens Embedded in Eyelid for Years

Doctors Remove Contact Lens Embedded in Eyelid for ...

Lens was encapsulated within the upper eyelid soft tissue since childhood eye trauma

CDC: Brucellosis in Dogs Remains a Public Health Risk

CDC: Brucellosis in Dogs Remains a Public Health ...

Infection is under-recognized, may remain a threat without stronger intervention measures

is free, fast, and customized just for you!




Already a member?

Sign In Now »