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

Taosheng Chen, PhD, PMP

Associate 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 in drug toxicity, drug resistance and human diseases
  • Regulation of PAX3-FOXO1 and muscle differentiation in the development of rhabdomyosarcoma
  • Development of drug discovery technologies
  • High throughput screening (HTS) and high content screening (HCS)

Selected Publications

Churchman ML, Low J, Qu C, Paietta EM, Kasper LH, Chang Y, Payne-Turner D, Althoff MJ, Song G, Chen SC, Ma J, Rusch M, McGoldrick D, Edmonson M, Gupta P, Wang YD, Caufield W, Freeman B, Li L, Panetta JC, Baker S, Yang YL, Roberts KG, McCastlain K, Iacobucci I, Peters JL, Centonze VE, Notta F, Dobson SM, Zandi S, Dick JE, Janke L, Peng J, Kodali K, Pagala V, Min J, Mayasundari A, Williams RT, Willman CL, Rowe J, Luger S, Dickins RA, Guy RK, Chen T, Mullighan CG. Efficacy of retinoids in IKZF1-mutated BCR-ABL1 acute lymphoblastic leukemia. Cancer Cell Aug 26, 2015. pii: S1535-6108(15)00268-8. doi: 10.1016/j.ccell.2015.07.016. [Epub ahead of print].

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.

Chai SC, Goktug AN, Chen T. Assay validation in high throughput screening - from concept to application, Drug Discovery and Development – From Molecules to Medicine, Omboon Vallisuta and Suleiman Olimat (Ed.), pp. 221-239, Chapter 10. ISBN: 978-953-51-2128-2, InTech, Croatia, DOI: 10.5772/59765, 2015. 

Rodriguez DA, Weinlich R, Brown S, Guy C, Fitzgerald P, Dillon CP, Oberst A, Quarato G, Low J, Cripps JG, Chen T, Green DR, Characterization of RIPK3-mediated phosphorylation of the activation loop of MLKL during necroptosis. Cell Death Differ May 29, 2015. Epub ahead of print. doi: 10.1038/cdd.2015.70.

Pabla N, Gibson AA, Buege M, Ong SS, Li L, Hu S, Du G, Sprowl JA, Vasilyeva A, Janke LJ, Schlatter E, Chen T, Ciarimboli G, Sparreboom A, Mitigation of acute kidney injury by cell-cycle inhibitors that suppress both CDK4/6 and OCT2 functions. Proc Natl Acad Sci USA 112:5231-5236, 2015.

Cherian MT, Chai SC, Chen T. Small-molecule modulators of the constitutive androstane receptor. Expert Opin Drug Metab Toxicol 1-16; May 15, 2015. Epub ahead of print.

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.

Leung W-H, Vong QP, Lin W, Bouck D, Wendt S, Sullivan E, Li Y, Bari R, Chen T, and Leung W. PRL-3 mediates the protein maturation of ULBP2 by regulating the tyrosine phosphorylation of HSP60. J Immunol 194:2930-2941, 2015.

Sharma LK, Leonardi R, Lin W, Boyd VA, Goktug A, Shelat AA, Chen T, Jackowski S, Rock CO. A high-throughput screen reveals new small-molecule activators and inhibitors of pantothenate kinases. J Med Chem 58(3):1563-8, 2015.

Pondugula PR, Flannery PC, Apte U, Babu JR, Geetha T, Rege SD, Chen T, Abbott KL. PPM1A phosphatase is involved in regulating PXR-mediated CYP3A4 gene expression. Drug Metab Dispos Jan 5, 2015. Epub ahead of print. pii: dmd.114.062083.

Banerjee M, Robbins D, Chen T. Targeting xenobiotic receptors PXR and CAR in human diseases. Drug Discov Today 20(5):618-28, 2014. pii: S1359-6446(14)00456-5. doi: 10.1016/j.drudis.2014.11.011.  

Beard JA, Tenga A, Chen T. The interplay of NR4A receptors and the oncogene–tumor suppressor networks in cancer. Cell Signal Nov, 2014. Epub ahead of print. pii: S0898-6568(14)00355-6. doi: 10.1016/j.cellsig.2014.11.009.

Wang YM, Chai SC, Brewer CT, Chen T. Pregnane X receptor and drug-induced liver injury. Expert Opin Drug Metab Toxicol 2014 Sep 25. doi:10.1517/17425255.2014.963555. [Epub ahead of print].

Banerjee M, Chen T. Thiazide-like diuretic drug metolazone activates human pregnane X receptor to induce cytochrome 3A4 and multidrug-resistance protein 1. Biochem Pharmacol 2014 Aug 30. doi: 10.1016/j.bcp.2014.08.025. [Epub ahead of print].

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 2014 Aug 18. [Epub ahead of print]. DOI: 10.1021/bc5002856.

Yu DD, Lin W, Forman BM, Chen T. Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor. Bioorg Med Chem 22:2919-2938, 2014.

Robbins D, Chen T. Tissue-specific regulation of pregnane X receptor in cancer development and therapy. Cell Biosci 4(1):17, 2014.

Walters BJ, Lin W, Diao S, Brimble M, Iconaru LI, Dearman J, Goktug A, Chen T, Zuo J. High-throughput screening reveals alsterpaullone, 2-cyanoethyl as a potent p27Kip1 transcriptional inhibitor. PLoS ONE 9(3):e91173, 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 Jan 20, 2014. doi:10.1042/BJ20130558. [Epub ahead of print]

Leung WH, Vong QP, Lin W, Janke L, Chen T, Leung W. Modulation of NKG2D ligand expression and metastasis in tumors by spironolactone via RXRγ activation. J Exp Med Nov 4, 2013. [Epub ahead of print].

Elias A, High AA, Mishra A, Ong SS, Wu J, Peng J, Chen T. Identification and Characterization of Phosphorylation Sites within the Pregnane X Receptor Protein. Biochem Pharmacol Oct 30, 2013. doi:pii: S0006-2952(13)00682-5. 10.1016/j.bcp.2013.10.015. [Epub ahead of print]

McCoy F, Darbandi R, Lee HC, Bharatham K, Moldoveanu T, Royappa G, Dodd K, Lin W, Chen S-I, Tangallapally RP, Kurokawa M, Lee RE, Shelat A, Chen T, Green DR, Harria RA, Lin S-H, Fissore RA, Colbran RJ, Nutt LK. Metabolic activation of CaMKII by Coenzyme A. Molecular Cell 2013. http://dx.doi.org/10.1016/j.molcel.2013.08.043.

Lin W, Chen T. A vinblastine fluorescent probe for pregnane X receptor in a time-resolved fluorescence resonance energy transfer assay. Anal Biochem September 14, 2013. pii: S0003-2697(13)00439-9. doi: 10.1016/j.ab.2013.09.009. [Epub ahead of print].

Takwi AA, Wang YM, Wu J, Michaelis M, Cinatl J Jr, Chen T. miR-137 regulates the constitutive androstane receptor and modulates doxorubicin sensitivity in parental and doxorubicin-resistant neuroblastoma cells. Oncogene, 2013 Aug 12. doi:10.1038/onc.2013.330. [Epub ahead of print].

Banerjee M, Chen T. Differential regulation of CYP3A4 promoter activity by a new class of natural product derivatives binding to pregnane X receptor. Biochem Pharmacol Aug 5, 2013. pii: S0006-2952(13)00459-0. doi: 10.1016/j.bcp.2013.07.023. [Epub ahead of print].

Banerjee M, Robbins D, Chen T. Modulation of xenobiotic receptors by steroids. Molecules 18(7), 7389-7406, 2013.

Wang YM, Lin W, Chai SC, Wu J, Ong SS, Schuetz EG, Chen T. Piperine activates human pregnane X receptor to induce the expression of cytochrome P450 3A4 and multidrug resistance protein 1. Toxicol Appl Pharmacol May 12, 2013. doi:pii: S0041-008X(13)00222-6. doi: 10.1016/j.taap.2013.05.014. [Epub ahead of print].

Yu DD*, Lin W, Chen T* (*co-corresponding author), Forman BM. Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery. Bioorg Med Chem 21: 4266-4278, 2013.

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

Goktug AN, Chai SC, Chen T. A timetable organizer for the planning and implementation of screenings in manual or semi-automation mode. J Biomol Screen, 2013 May 7. [Epub ahead of print].

Vrijens K, Lin W, Cui J, Farmer D, Low J, Pronier E, Zeng FY, Shelat AA, Guy K, Taylor MR, Chen T, Roussel MF. Identification of small molecule activators of BMP signaling. PLoS ONE 8(3): e59045. doi:10.1371/journal.pone.0059045, 2013.

Liu L, Wu J, Ong SS, Chen T. Cyclin-dependent kinase 4 phosphorylates and positively regulates PAX3-FOXO1 in human alveolar rhabdomyosarcoma cells. PLoS ONE 8(2): e58193. doi: 10.1371/journal.pone.0058193, 2013.

Goktug AN, Chai SC, Chen T. Data analysis approaches in high throughput screening. Drug Discovery, Prof. Hany El-Shemy (Ed.), pp. 201-226. ISBN: 978-953-51-0906-8, InTech, DOI: 10.5772/52508, 2013. [Available from: http://www.intechopen.com/books/drug-discovery/data-analysis-approaches-in-high-throughput-screening]

Chai SC, Goktug AN, Cui J, Low J, Chen T. Practical considerations of liquid handling devices in drug discovery. Drug Discovery, Prof. Hany El-Shemy (Ed.), pp. 177-200. ISBN: 978-953-51-0906-8, InTech, DOI: 10.5772/52546, 2013. [Available from: http://www.intechopen.com/books/drug-discovery/practical-considerations-of-liquid-handling-devices-in-drug-discovery]

Goktug AN, Ong SS, Chen T. GUItars: a GUI tool for analysis of high-throughput RNA interference screening data. PLoS ONE 7(11):e49386, 2012.

Liu L, Chen T. PAX3-FKHR regulates the expression of pleiotrophin to mediate motility in alveolar rhabdomyosarcoma cells. J Can Res Updates 1:49-56, 2012.

Wang YM, Ong SS, Chai SC, Chen T. Role of CAR and PXR in xenobiotic sensing and metabolism. Expert Opin Drug Metab Toxicol May 3, 2012.

Liu L, Wang YD, Wu J, Cui J, Chen T. Carnitine palmitoyltransferase 1A (CPT1A): a transcriptional target of PAX3-FKHR and mediates PAX3-FKHR-dependent motility in alveolar rhabdomyosarcoma cells. BMC Cancer 12(1):154, 2012.

Li G, Lin W, Araya JJ, Chen T, Timmermann BN, Guo GL. A tea catechin, epigallocatechin-3-gallate, is a unique modulator of the farnesoid X receptor. Toxicol Appl Pharmacol 258(2):268-274, 2012

Ong SS, Wang Y-M, Chai SC, Chen T. Pregnane X receptor in drug development. In “Drug Development – A Case Study Based Insight into Modern Strategies” (C. Rundfeldt, ed.), pp.337-364. Intech, ISBN 978-953-307-257-9, 2011.

Zhao Y, Hammoudeh D, Lin W, Das S, Yun MK, Li Z, Griffith E, Chen T, White SW, Lee RE. Development of a pterin-based fluorescent probe for screening dihydropteroate synthase. Bioconjug Chem September 30, 2011.

Cui J, Chai SC, Shelat AA, Guy RK, Chen T. An automated approach to efficiently reformat a large collection of compounds. Curr Chem Genomics 5:42-47, 2011.

Bouck DC, Shu P, Cui J, Shelat A, Chen T. A high-content screen identifies inhibitors of nuclear export of forkhead transcription factors. J Biomol Screen 16(4):394-404, 2011.

Ashley JW, McCoy EM, Clements DA, Shi Z, Chen T, Feng X. Development of cell-based high-throughput assays for the identification of inhibitors of receptor activator of nuclear factor-kappa B signaling. Assay Drug Dev Technol 9(1):40-49, 2011.

Pondugula SR, Xie W, Chen T. PXR and hepatocyte proliferation. J Exp Clin Med 2: 260-261, 2010.

Young BM, Hyatt JL, Bouck DC, Chen T, Hanumesh P, Price J, Boyd VA, Potter PM, Webb TR. Structure-activity relationships of substituted 1-Pyridyl-2-phenyl-1,2-ethanediones: potent, selective carboxylesterase inhibitors. J Med Chem 53(24):8709-8715, 2010.

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

Leonardi R, Zhang Y-M, Yun M-K, Zhou R, Zeng F-Y, Lin W, Cui J, Chen T, Rock CO, White SW, Jackowski S. Modulation of pantothenate kinase 3 activity by small molecules that interact with the substrate/allosteric regulatory domain. Chem Biol 17: 892-902, 2010.

Dong H, Lin W, Wu J, Chen T. Flavonoids activate pregnane X receptor-mediated CYP3A4 gene expression by inhibiting cyclin-dependent kinases in HepG2 liver carcinoma cells. BMC Biochem 11:23, 2010.

Pondugula SR, Tong AA, Wu J, Cui J, Chen T. Protein phosphatase 2C?l regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells. Drug Metab Dispos 38: 1411-1416, 2010.

Zeng FY, Dong H, Cui J, Liu L, Chen T. Glycogen synthase kinase 3 regulates PAX3-FKHR-mediated cell proliferation in human alveolar rhabdomyosarcoma cells. Biochem Biophys Res Commun 391: 1049-1055, 2010.

Last update: September 2015