SPA70 is a potent antagonist of human pregnane X receptor

Wenwei Lin; Yue-Ming Wang; Sergio C. Chai; Lili Lv; Jie Zheng; Jing Wu; Qijun Zhang; Yong-Dong Wang; Patrick R. Griffin; Taosheng Chen

doi:10.1038/s41467-017-00780-5

Nature Communications (Sep 2017)

SPA70 is a potent antagonist of human pregnane X receptor

Wenwei Lin,
Yue-Ming Wang,
Sergio C. Chai,
Lili Lv,
Jie Zheng,
Jing Wu,
Qijun Zhang,
Yong-Dong Wang,
Patrick R. Griffin,
Taosheng Chen

Affiliations

Wenwei Lin: Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital
Yue-Ming Wang: Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital
Sergio C. Chai: Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital
Lili Lv: Structure Biology, Shanghai Medicilon Inc.
Jie Zheng: Department of Molecular Medicine, The Scripps Research Institute
Jing Wu: Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital
Qijun Zhang: Structure Biology, Shanghai Medicilon Inc.
Yong-Dong Wang: Department of Computational Biology, St. Jude Children’s Research Hospital
Patrick R. Griffin: Department of Molecular Medicine, The Scripps Research Institute
Taosheng Chen: Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital

DOI: https://doi.org/10.1038/s41467-017-00780-5
Journal volume & issue: Vol. 8, no. 1
pp. 1 – 14

Abstract

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The xenobiotic-activated human pregnane X receptor (hPXR) regulates drug metabolism. Here the authors develop hPXR modulators, which are of potential therapeutic interest and functionally and structurally characterize the antagonist SPA70 and the structurally related agonist SJB7.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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