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 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

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. doi: 10.1038/s41467-017-00780-5.

Lolodi O, Wang YM, Wright WC, Chen T. Differential regulation of CYP3A4 and CYP3A5 and its implication in drug discovery. Curr Drug Metab 2017. doi: 10.2174/1389200218666170531112038.

Bakke J, Wright WC, Zamora AE, Ong SS, Wang YM, Hoyer JD, Brewer CT, Thomas PG, Chen T. Transcription factor ZNF148 is a negative regulator of human muscle differentiation. Sci Rep 7(1):8138, 2017.

Yang J, Milasta S, Hu D, AlTahan AM, Interiano RB, Zhou J, Davidson J, Low J, Lin W, Bao J, Goh P, Nathwani AC, Wang R, Wang Y, Ong SS, Boyd VA, Young B, Das S, Shelat A, Wu Y, Li Z, Zheng JJ,  Mishra A, Cheng Y, Qu C, Peng J, Green DR, White S, Guy RK, Chen T, Davidoff AM. Targeting histone demethylases in MYC-driven neuroblastomas with ciclopirox. Cancer Res 2017. doi: 10.1158/0008-5472.CAN-16-0826.

Genthe JR, Min J, Farmer DM, Shelat AA, Grenet JA, Lin W, Finkelstein D, Vrijens K, Chen T, Guy RK, Clements WK, Roussel MF. Ventromorphins: A new class of small molecule activators of the canonical BMP signaling pathway. ACS Chem Biol 2017. doi: 10.1021/acschembio.7b00527.

Scott DC, Hammill JT, Min J, Rhee DY, Connelly M, Sviderskiy VO, Bhasin D, Chen Y, Ong SS, Chai SC, Goktug AN, Huang G, Monda JK, Low J, Kim HS, Paulo JA, Cannon JR, Shelat AA, Chen T, Kelsall IR, Alpi AF, Pagala V, Wang X, Peng J, Singh B, Harper JW, Schulman BA, Guy RK. Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase. Nat Chem Biol 13: 850-857, 2017.

Oladimeji P, Lin W, Brewer CT, Chen T. Glucose-dependent regulation of pregnane X receptor is modulated by AMP-activated protein kinase. Sci Rep 7:46751, 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. 

Brewer CT, Chen T. PXR variants: the impact on drug metabolism and therapeutic responses. Acta Pharm Sin B, 6(5):441-449, 2016. 

Oladimeji P, Cui H, Zhang C, Chen T. Regulation of PXR and CAR by protein-protein interaction and signaling crosstalk. Expert Opin Drug Metab Toxicol 2016 Jun 23: 1-14. [Epub ahead of print].

Teitz T, Goktug AN, Chen T, Zuo J. Development of cell-Based high-throughput chemical screens for protection against cisplatin-Induced ototoxicity. Methods Mol Biol 1427: 419-430, 2016.

Robbins D, Bakke J, Cherian MT, Wu J, Chen T. PXR interaction with p53: the meeting of two masters. Cell Death Dis 7:e2218, 2016. doi:10.1038/cddis.2016.122.

Chai SC, Cherian MT, Wang Y, Chen T. Small-molecule modulators of PXR and CAR. Biochim Biophys Acta Feb 24, 2016. [Epub ahead of print]. pii: S1874-9399(16)30035-9. doi: 10.1016/j.bbagrm.2016.02.013.

LIambi F, Wang YM, Victor B, Yang M, Schneider DM, Gingras S, Parsons MJ, Zheng JH, Brown SA, Pelletier S, Moldoveanu T, Chen T, Green DR. BOK is a non-canonical BCL-2 family effector of apoptosis regulated by ER-associated degradation. Cell 165:421-433, 2016.

Sprowl JA, Ong SS, Gibson AA, Hu S, Du G, Lin W, Li L, Bharill S, Ness RA, Stecula A, Offer SM, Diasio RB, Nies AT, Schwab M, Cavaletti G, Schlatter E, Ciarimboli G, Schellens JH, Isacoff EY, Sali A, Chen T, Baker SD, Sparreboom A, Pabla N. A phosphotyrosine switch regulates organic cation transporters. Nat Commun 7:10880, 2016. doi: 10.1038/ncomms10880.

Robbins D, Cherian M, Wu J, Chen T. Human pregnane X receptor compromises the function of p53 and promotes malignant transformation. Cell Death Discovery 2:16023, 2016. doi:10.1038/cddiscovery.2016.23.

Beard JA, Tenga A, Hills J, Hoyer JD, Cherian MT, Wang YD, Chen T. The orphan nuclear receptor NR4A2 is part of a p53−microRNA-34 network. Sci Rep 6:25108, 2016. doi: 10.1038/srep25108.

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. 

Twarog NR, Low JA, Currier DG, Mill G, Chen T, Shelat AA. Robust classification of small-molecule mechanism of action using a minimalist high-content microscopy screen and multidimensional phenotypic trajectory analysis. PLoS ONE 11(2):e0149439, 2016. doi: 10.1371/journal.pone.0149439.

Tenga A, Beard JA, Takwi A, Wang YM, Chen T. Regulation of nuclear receptor Nur77 by miR-124. PLoS ONE 11(2):e0148433, 2016. doi:10.1371/journal.pone.0148433. 

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.

Zimmerman EI, Gibson AA, Hu S, Vasilyeva A, Orwick SJ, Du G, Mascara GP, Ong SS, Chen T, Vogel P, Inaba H, Maitland ML, Sparreboom A, Baker SD. Multikinase inhibitors induce cutaneous toxicity through OAT6-mediated uptake and MAP3K7-driven cell death. Cancer Res 76(1):117-126, 2016. doi:10.1158/0008-5472.CAN-15-0694.

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 28(3):343-56, 2015. doi: 10.1016/j.ccell.2015.07.016.

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. In: Drug Discovery and Development – From Molecules to Medicine. Vallisuta O, Olimat S, eds. InTech: Rijecka, Croatia; 221-239, 2015. ISBN: 978-953-51-2128-2. doi: 10.5772/59765. 

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 23(1):76-88, 2016. 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 11(7):1099-114, 2015. doi: 10.1517/17425255.2015.1043887.

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.

Show More

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 92(2):389-402, 2014. doi: 10.1016/j.bcp.2014.08.025.

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(9):1664-77, 2014. 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 459(1):193-203. doi:10.1042/BJ20130558.

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 MedNov 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 PharmacolOct 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.

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 27(2):257-66, 2014. 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 10(11):1521-32, 2014. doi:10.1517/17425255.2014.963555. 

Last update: September 2017