Ontology highlight
ABSTRACT:
SUBMITTER: Lin W
PROVIDER: S-EPMC5622171 | biostudies-literature | 2017 Sep
REPOSITORIES: biostudies-literature
Lin Wenwei W Wang Yue-Ming YM Chai Sergio C SC Lv Lili L Zheng Jie J Wu Jing J Zhang Qijun Q Wang Yong-Dong YD Griffin Patrick R PR Chen Taosheng T
Nature communications 20170929 1
Many drugs bind to and activate human pregnane X receptor (hPXR) to upregulate drug-metabolizing enzymes, resulting in decreased drug efficacy and increased resistance. This suggests that hPXR antagonists have therapeutic value. Here we report that SPA70 is a potent and selective hPXR antagonist. SPA70 inhibits hPXR in human hepatocytes and humanized mouse models and enhances the chemosensitivity of cancer cells, consistent with the role of hPXR in drug resistance. Unexpectedly, SJB7, a close an ...[more]