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The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism.

Abstract：

:Farnesoid X receptor (FXR) has important roles in maintaining bile acid and cholesterol homeostasis. Here we report that the antiparasitic drug ivermectin is a ligand for nuclear FXR. We identify ivermectin using a high-throughput compound library screening and show that it induces the transcriptional activity of the FXR with distinctive properties in modulating coregulator recruitment. The crystal structure of ivermectin complexed with the ligand-binding domain of FXR reveals a unique binding mode of ivermectin in the FXR ligand-binding pocket, including the highly dynamic AF-2 helix and an expanded ligand-binding pocket. Treatment of wild-type mice, but not of FXR-null mice, with ivermectin decreases serum glucose and cholesterol levels, suggesting that ivermectin regulates metabolism through FXR. Our results establish FXR as the first mammalian protein targeted by ivermectin with high selectivity. Considering that ivermectin is a widely used clinical drug, our findings reveal a safe template for the design of novel FXR ligands.

journal_name

Nat Commun

journal_title

Nature communications

authors

Jin L,Feng X,Rong H,Pan Z,Inaba Y,Qiu L,Zheng W,Lin S,Wang R,Wang Z,Wang S,Liu H,Li S,Xie W,Li Y

doi

10.1038/ncomms2924

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

1937

issn

2041-1723

pii

ncomms2924

journal_volume

4

pub_type

杂志文章

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