Selective chemical inhibition of promiscuous xenobiotic receptor and drug-metabolizing enzymes
Includes a Live Web Event on 08/19/2025 at 3:00 PM (EDT)
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| Pregnane X receptor (PXR) transcriptionally induces drug-metabolizing enzymes such as CYP3A4/5 to control drug metabolism, and might cause drug-drug interactions, toxicities, and resistance. Therefore, inhibitors of PXR and CYP3A4/5 might have therapeutic value. Many drugs bind to and activate PXR, and CYP3A4/5 metabolize 50% of the marketed drugs. The large and dynamic ligand binding pockets of PXR, CYP3A4, and CYP3A5 enable their promiscuous accommodation of structurally diverse ligands, and present challenges to selectively modulate them. We take structural, chemical and pharmacological approaches to selectively modulate PXR and CYP3A4/5. Our efforts provide effective approaches and novel chemical probes (e.g., inhibitors of PXR, CYP3A4 and CYP3A5) to selectively modulate the promiscuous drug metabolism pathway. At the end of this webinar, attendees should be able to: |
Taosheng Chen
Full Member (Professor) and Director of HTB Center
St. Jude Children's Research Hospital, USA
Dr. Taosheng Chen is a Professor (Full Member) of Chemical Biology & Therapeutics Department, and Director of High Throughput Bioscience Center at St. Jude Children’s Research Hospital, USA. He received his BS and MS from Fudan University, Ph.D. from University of Vermont and completed postdoctoral training at University of Virginia. Prior to joining St. Jude in 2006, he was a Senior Research Investigator at Bristol-Myers Squibb, and a Research Scientist at SAIC-Frederick, National Cancer Institute. He serves on several journal Editorial Boards, and NIH grant review panels and study section (e.g., chairperson of the DMP study section). He has authored more than 190 publications (in journals such as Nat Commun, PNAS, JACS, including 2 books), and 18 patents. His laboratory studies the regulation of nuclear receptors PXR and CAR and drug-metabolizing enzymes CYP3A4 and CYP3A5, by using biology, chemistry and structural biology approaches to develop novel chemical probes for mechanistic studies and lead compounds for therapeutic development. The goals are to understand nuclear receptor-regulated transcription networks, enzyme-drug interactions, and design therapeutic approaches to overcome drug resistance and toxicity - the leading causes of therapeutic failures.
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