Amelioration of PXR-mediated CYP3A4 induction by mGluR2 modulators.

Roy J Vaz,Yi Li, Vinolia Chellaraj,Stephan Reiling,Theresa Kuntzweiler,Donglai Yang,Hong Shen,Joseph D Batchelor,Ying Zhang,Xin Chen,Larry R McLean, Raymond Kosley

Bioorganic & Medicinal Chemistry Letters（2018）

引用 11|浏览22

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摘要

•CYP3A4 induction data lead to PXR activation data for mGluR2 allosteric activators.•One of the compounds was also crystallized with PXR & deposited in the PDB (6DUP).•Subsequent modification lead to induction-free compounds with good mGluR2 activity.

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关键词

mGluR2,PXR,X-ray,CYP3A4/5 induction

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