Discovery of a potent FKBP38 agonist that ameliorates HFD-induced hyperlipidemia
10.1016/j.apsb.2021.03.031
- Author:
Ping-Ting XIAO
1
;
Zhi-Shen XIE
2
;
Yu-Jia KUANG
1
;
Shi-Yu LIU
1
;
Chun ZENG
3
;
Ping LI
1
;
E-Hu LIU
1
Author Information
1. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
2. Academy of Chinese Medical Sciences, Henan University of Chinese Medicine, Zhengzhou 450046, China.
3. Departments of Pediatrics and Cellular & Molecular Medicine, Pediatric Diabetes Research Center and Institute for Genomic Medicine, University of California, San Diego, La Jolla, CA 92093, USA.
- Publication Type:Journal Article
- Keywords:
3,5,6,7,8,3ʹ,4ʹ-heptamethoxyflavone;
FKBP38;
Hyperlipidemia;
SREBP;
mTOR
- From:
Acta Pharmaceutica Sinica B
2021;11(11):3542-3552
- CountryChina
- Language:English
-
Abstract:
The mammalian target of rapamycin (mTOR)-sterol regulatory element-binding proteins (SREBPs) signaling promotes lipogenesis. However, mTOR inhibitors also displayed a significant side effect of hyperlipidemia. Thus, it is essential to develop mTOR-specific inhibitors to inhibit lipogenesis. Here, we screened the endogenous inhibitors of mTOR, and identified that FKBP38 as a vital regulator of lipid metabolism. FKBP38 decreased the lipid content