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Taosheng Chen, PhD, PMP
Taosheng Chen, PhD, PMP

Taosheng Chen, PhD, PMP

Member, St. Jude Faculty

  • Director, High Throughput Bioscience Center



PhD – University of Vermont
MS – Fudan University, Shanghai
BS – Fudan University, Shanghai

Research Interests

  • Regulation of PXR and CAR (nuclear receptors), and CYP3A (drug–metabolizing enzymes) in drug toxicity, drug resistance and human diseases
  • Development of chemical probes and therapeutic leads for PXR, CAR and CYP3A
  • Development of drug discovery technologies
  • High throughput screening (HTS) and high content screening (HCS)

Selected Publications

Lin W, Huber AD, Poudel S, Li Y, Seetharaman J, Miller DJ, Chen T. Structure-guided approach to modulate small molecule binding to a promiscuous ligand-activated protein. Proc Natl Acad Sci U S A 120(10): e2217804120, 2023.

Li Y, Lin W, Chai SC, Wu J, Annu K, Chen T. Design and Optimization of 1 H-1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR. J Med Chem 65(24):16829-16859, 2022.

Bwayi MN, Garcia-Maldonado E, Chai SC, Xie B, Chodankar S, Huber AD, Wu J, Annu K, Wright WC, Lee HM, Seetharaman J, Wang J, Buchman CD, Peng J, Chen T. Molecular basis of crosstalk in nuclear receptors: heterodimerization between PXR and CAR and the implication in gene regulation. Nucleic Acids Res 50(6):3254-3275, 2022.

Wang J, Buchman CD, Seetharaman J, Miller DJ, Huber AD, Wu J, Chai SC, Garcia-Maldonado E, Wright WC, Chenge J, Chen T. Unraveling the Structural Basis of Selective Inhibition of Human Cytochrome P450 3A5. J Am Chem Soc 143(44):18467-18480, 2021.

Li Y, Lin W, Wright WC, Chai SC, Wu J, Chen T. Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70. J Med Chem 64(3):1733-1761, 2021.

Huber AD, Wright WC, Lin W, Majumder K, Low JA, Wu J, Buchman CD, Pintel DJ, Chen T. Mutation of a single amino acid of pregnane X receptor switches an antagonist to agonist by altering AF-2 helix positioning. Cell Mol Life Sci 78(1):317-335, 2021. 

Wright WC, Chenge J, Wang J, Girvan HM, Yang L, Chai SC, Huber AD, Wu J, Oladimeji PO, Munro AW, Chen T. Clobetasol propionate is a heme-mediated selective inhibitor of human cytochrome P450 3A5. J Med Chem 63(3):1415-1433, 2020.

Lin W, Bwayi M, Wu J, Li Y, Chai SC, Huber AD, Chen T. CITCO directly binds to and activates human pregnane X receptor. Mol Pharmacol 97(3):180-190, 2020.

Cherian MT, Chai SC, Wright WC, Singh A, Casal MA, Zheng J, Wu J, Lee RE, Griffin PR, Chen T. CINPA1 binds directly to constitutive androstane receptor and inhibits its activity. Biochem Pharmacol 152:211-223, 2018.

Li Y, Bakke J, Finkelstein D, Zeng H, Wu J, Chen T. HNRNPH1 is required for rhabdomyosarcoma cell growth and survival. Oncogenesis 7(1):9, 2018.

Lin W, Wang Y-M, Chai SC, Lv L, Zheng J, Wu J, Zhang Q, Wang Y-D, Griffin PR, Chen T. SPA70 is a potent antagonist of human pregnane X receptor. Nat Commun 8:741, 2017.

Cherian MT, Yang L, Chai SC, Lin W, Chen T. Identification and characterization of CINPA1 metabolites facilitates structure-activity studies of the constitutive androstane receptor. Drug Metab Dispos 44(11):1759-1770, 2016.

Banerjee M, Chai SC, Wu J, Robbins D, Chen T. Tryptophan 299 is a conserved residue of human pregnane X receptor critical for the functional consequence of ligand binding. Biochem Pharmacol 104:131-138, 2016.

Lin W, Yang L, Chai SC, Lu Y, Chen T. Development of CINPA1 analogs as novel and potent inverse agonists of constitutive androstane receptor. Eur J Med Chem 108:505-528, 2016.

Wang Y, Chai SC, Lin W, Chai X, Elias A, Wu J, Ong SS, Pondugula SR, Beard JA, Schuetz EG, Zeng S, Xie W, Chen T. Serine 350 of human pregnane X receptor is crucial for its heterodimerization with retinoid X receptor alpha and transactivation of target genes in vitro and in vivo. Biochem Pharmacol 96:357-368, 2015.

Cherian MT, Lin W, Wu J, Chen T. CINPA1 is an inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). Mol Pharmacol 87(5):878-889, 2015.

Lin W, Liu J, Jeffries C, Yang L, Lu Y, Lee RE, Chen T. Development of BODIPY FL vindoline as a novel and high-affinity pregnane X receptor fluorescent probe. Bioconjug Chem 25:1664-1677, 2014.

Ong SS, Goktug AN, Elias A, Wu J, Saunders D, Chen T. Stability of the human pregnane X receptor is regulated by E3 ligase UBR5 and serine/threonine kinase DYRK2. Biochem J 459:193-203, 2014.

Elias A, Wu J, Chen T. Tumor suppressor protein p53 negatively regulates human pregnane X receptor activity. Mol Pharmacol 83(6):1229-1236, 2013.

Pondugula SR, Brimer-Cline C, Wu J, Schuetz EG, Tyagi RK, Chen T. A phosphomimetic mutation at threonine-57 abolishes transactivation activity and alters nuclear localization pattern of human pregnane X receptor. Drug Metab Dispos 37:719-730, 2009.

Lin W, Wu J, Dong H, Bouck D, Zeng FY, Chen T. Cyclin-dependent kinase 2 negatively regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells. J Biol Chem 283:30650-30657, 2008.

Chai SC, Wright WC, Chen T. Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer. Med Res Rev 40(3):1061-1083, 2020.

Chai SC, Lin W, Li Y, Chen T. Drug discovery technologies to identify and characterize modulators of the pregnane X receptor and the constitutive androstane receptor. Drug Discov Today 24(3):906-915, 2019.

Oladimeji P, Chen T. PXR: more than just a master xenobiotic receptor. Mol Pharmacol 93(2):119-127, 2018.

Buchman CD, Chai SC, Chen T. A current structural perspective on PXR and CAR in drug metabolism. Expert Opin Drug Metab Toxicol 14(6):635-647, 2018.

Chai SC, Cherian MT, Wang Y, Chen T. Small-molecule modulators of PXR and CAR. Biochim Biophys Acta 1859:1141-1154, 2016.

Banerjee M, Robbins D, Chen T. Targeting xenobiotic receptors PXR and CAR in human diseases. Drug Discov Today 20:618-628, 2015.

Wang Y-M, Ong SS, Chai SC, Chen T. Role of CAR and PXR in xenobiotic sensing and metabolism. Expert Opin Drug Metab Toxicol 8(7):803-817, 2012.

Chen T. A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery” (T. Chen, ed.), CRC Press, Taylor & Francis Group, Boca Raton, FL, ISBN 978-1-4200-7050-7, 2010.

Chen T. Overcoming drug resistance by regulating nuclear receptors. Adv Drug Deliv Rev 62:1257-1264, 2010.

Chen T. Nuclear receptor drug discovery. Curr Opin Chem Biol 12:418-426, 2008. 

Last update: March 2023