Structure-based screening and biological validation of the anti-thrombotic drug-dicoumarol as a novel and potent PPARγ-modulating ligand
Bioorganic Chemistry(2022)
摘要
•Dic was revealed to be a potent SPPARγM by SB-VHTS and assays in vitro.•Dic exhibited weaker promotion of adipose differentiation than TZD drugs.•Dic showed anti-diabetic effects without body and organ weight gains in db/db mice.•Dic regulated the insulin-relative genes by inhibiting pPPARγ Ser273.•Dic performed a unique binding mode with PPARγ LBD.
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关键词
Anti-diabetic effects,Dicoumarol,Insulin sensitivity,SB-VHTS,SPPARγM,T2DM
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