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Sergio C. Chai, Ph.D. - Publications

Affiliations: 
2006 University of Massachusetts, Amherst, Amherst, MA 
Area:
Inorganic Chemistry, Analytical Chemistry
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38 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2023 Huber AD, Poudel S, Wu J, Miller DJ, Lin W, Yang L, Bwayi MN, Rimmer MA, Gee RRF, Seetharaman J, Chai SC, Chen T. A bromodomain-independent mechanism of gene regulation by the BET inhibitor JQ1: direct activation of nuclear receptor PXR. Nucleic Acids Research. PMID 38084912 DOI: 10.1093/nar/gkad1175  0.335
2020 Slavish PJ, Chi L, Yun MK, Tsurkan L, Martinez NE, Jonchere B, Chai SC, Connelly M, Waddell MB, Das S, Neale G, Li Z, Shadrick WR, Olsen RR, Freeman KW, et al. Bromodomain-selective BET inhibitors are potent antitumor agents against MYC-driven pediatric cancer. Cancer Research. PMID 32651255 DOI: 10.1158/0008-5472.Can-19-3934  0.382
2020 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. Journal of Medicinal Chemistry. PMID 31965799 DOI: 10.1021/Acs.Jmedchem.9B02067  0.401
2019 Lin W, Bwayi M, Wu J, Li Y, Chai SC, Huber AD, Chen T. CITCO Directly Binds to and Activates Human Pregnane X Receptor. Molecular Pharmacology. PMID 31882411 DOI: 10.1124/Mol.119.118513  0.391
2019 Chai SC, Wright WC, Chen T. Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer. Medicinal Research Reviews. PMID 31782213 DOI: 10.1002/Med.21648  0.39
2019 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 Discovery Today. PMID 30731240 DOI: 10.1016/J.Drudis.2019.01.021  0.377
2018 Buchman CD, Chai SC, Chen T. A current structural perspective on PXR and CAR in drug metabolism. Expert Opinion On Drug Metabolism & Toxicology. PMID 29757018 DOI: 10.1080/17425255.2018.1476488  0.392
2018 Cherian MT, Chai SC, Wright WC, Singh A, Alexandra Casal M, Zheng J, Wu J, Lee RE, Griffin PR, Chen T. CINPA1 binds directly to constitutive androstane receptor and inhibits its activity. Biochemical Pharmacology. PMID 29608908 DOI: 10.1016/J.Bcp.2018.03.029  0.445
2017 Shadrick WR, Slavish PJ, Chai SC, Waddell B, Connelly M, Low JA, Tallant C, Young BM, Bharatham N, Knapp S, Boyd VA, Morfouace M, Roussel MF, Chen T, Lee RE, et al. Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. Bioorganic & Medicinal Chemistry. PMID 29170024 DOI: 10.1016/J.Bmc.2017.10.042  0.332
2017 Lin W, Wang YM, Chai SC, Lv L, Zheng J, Wu J, Zhang Q, Wang YD, Griffin PR, Chen T. SPA70 is a potent antagonist of human pregnane X receptor. Nature Communications. 8: 741. PMID 28963450 DOI: 10.1038/S41467-017-00780-5  0.42
2017 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, et al. Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase. Nature Chemical Biology. PMID 28581483 DOI: 10.1038/Nchembio.2386  0.367
2016 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 Metabolism and Disposition: the Biological Fate of Chemicals. PMID 27519550 DOI: 10.1124/Dmd.116.071993  0.438
2016 Chai SC, Cherian MT, Wang YM, Chen T. Small-molecule modulators of PXR and CAR. Biochimica Et Biophysica Acta. PMID 26921498 DOI: 10.1016/J.Bbagrm.2016.02.013  0.392
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. Biochemical Pharmacology. PMID 26902414 DOI: 10.1016/J.Bcp.2016.02.009  0.439
2016 Min J, Scott DC, Chai SC, Goktug AN, Hammill JT, Huang G, Connelly MC, Matheny A, Shelat A, Singh B, Chen T, Schulman BA, Guy RK. Abstract LB-056: Discovery of novel small molecule inhibitors of the DCN1-Ubc12 interaction by high throughput screening technology Cancer Research. 76. DOI: 10.1158/1538-7445.Am2016-Lb-056  0.349
2015 Lin W, Yang L, Chai SC, Lu Y, Chen T. Development of CINPA1 analogs as novel and potent inverse agonists of constitutive androstane receptor. European Journal of Medicinal Chemistry. 108: 505-528. PMID 26717202 DOI: 10.1016/J.Ejmech.2015.12.018  0.381
2015 Wang YM, 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. Biochemical Pharmacology. PMID 26119819 DOI: 10.1016/J.Bcp.2015.06.018  0.382
2015 Cherian MT, Chai SC, Chen T. Small-molecule modulators of the constitutive androstane receptor. Expert Opinion On Drug Metabolism & Toxicology. 11: 1099-114. PMID 25979168 DOI: 10.1517/17425255.2015.1043887  0.366
2014 Wang YM, Chai SC, Brewer CT, Chen T. Pregnane X receptor and drug-induced liver injury. Expert Opinion On Drug Metabolism & Toxicology. 10: 1521-32. PMID 25252616 DOI: 10.1517/17425255.2014.963555  0.322
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. Toxicology and Applied Pharmacology. 272: 96-107. PMID 23707768 DOI: 10.1016/J.Taap.2013.05.014  0.428
2012 Wang YM, Ong SS, Chai SC, Chen T. Role of CAR and PXR in xenobiotic sensing and metabolism. Expert Opinion On Drug Metabolism & Toxicology. 8: 803-17. PMID 22554043 DOI: 10.1517/17425255.2012.685237  0.359
2011 Wang WL, Chai SC, Ye QZ. Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors. Bioorganic & Medicinal Chemistry Letters. 21: 7151-4. PMID 22001086 DOI: 10.1016/J.Bmcl.2011.09.080  0.393
2011 Zhang Q, Xiao H, Chai SC, Hoang QQ, Lu H. Hydrophilic residues are crucial for ribosomal protein L11 (RPL11) interaction with zinc finger domain of MDM2 and p53 protein activation. The Journal of Biological Chemistry. 286: 38264-74. PMID 21903592 DOI: 10.1074/Jbc.M111.277012  0.366
2011 Chai SC, Wang WL, Ding DR, Ye QZ. Growth inhibition of Escherichia coli and methicillin-resistant Staphylococcus aureus by targeting cellular methionine aminopeptidase. European Journal of Medicinal Chemistry. 46: 3537-40. PMID 21575996 DOI: 10.1016/J.Ejmech.2011.04.056  0.347
2011 Yuan H, Chai SC, Lam CK, Howard Xu H, Ye QZ. Two methionine aminopeptidases from Acinetobacter baumannii are functional enzymes. Bioorganic & Medicinal Chemistry Letters. 21: 3395-8. PMID 21524572 DOI: 10.1016/J.Bmcl.2011.03.116  0.446
2011 Lee JH, Zhang Q, Jo S, Chai SC, Oh M, Im W, Lu H, Lim HS. Novel pyrrolopyrimidine-based α-helix mimetics: cell-permeable inhibitors of protein−protein interactions. Journal of the American Chemical Society. 133: 676-9. PMID 21171592 DOI: 10.1021/Ja108230S  0.33
2010 Chai SC, Ye QZ. A cell-based assay that targets methionine aminopeptidase in a physiologically relevant environment. Bioorganic & Medicinal Chemistry Letters. 20: 2129-32. PMID 20207144 DOI: 10.1016/J.Bmcl.2010.02.052  0.389
2010 Lu JP, Chai SC, Ye QZ. Catalysis and inhibition of Mycobacterium tuberculosis methionine aminopeptidase. Journal of Medicinal Chemistry. 53: 1329-37. PMID 20038112 DOI: 10.1021/Jm901624N  0.4
2009 Chai SC, Ye QZ. Analysis of the stoichiometric metal activation of methionine aminopeptidase. Bmc Biochemistry. 10: 32. PMID 20017927 DOI: 10.1186/1471-2091-10-32  0.383
2009 Chai SC, Ye QZ. Metal-mediated inhibition is a viable approach for inhibiting cellular methionine aminopeptidase. Bioorganic & Medicinal Chemistry Letters. 19: 6862-4. PMID 19889537 DOI: 10.1016/J.Bmcl.2009.10.082  0.411
2009 Chai SC, Lu JP, Ye QZ. Determination of binding affinity of metal cofactor to the active site of methionine aminopeptidase based on quantitation of functional enzyme. Analytical Biochemistry. 395: 263-4. PMID 19712663 DOI: 10.1016/J.Ab.2009.07.054  0.4
2009 Wang WL, Chai SC, Ye QZ. Synthesis and structure-function analysis of Fe(II)-form-selective antibacterial inhibitors of Escherichia coli methionine aminopeptidase. Bioorganic & Medicinal Chemistry Letters. 19: 1080-3. PMID 19167218 DOI: 10.1016/J.Bmcl.2009.01.011  0.388
2008 Wang WL, Chai SC, Huang M, He HZ, Hurley TD, Ye QZ. Discovery of inhibitors of Escherichia coli methionine aminopeptidase with the Fe(II)-form selectivity and antibacterial activity. Journal of Medicinal Chemistry. 51: 6110-20. PMID 18785729 DOI: 10.1021/Jm8005788  0.463
2008 Chai SC, Wang WL, Ye QZ. FE(II) is the native cofactor for Escherichia coli methionine aminopeptidase. The Journal of Biological Chemistry. 283: 26879-85. PMID 18669631 DOI: 10.1074/Jbc.M804345200  0.456
2008 Chai SC, Ju T, Dang M, Goldsmith RB, Maroney MJ, Pochapsky TC. Characterization of metal binding in the active sites of acireductone dioxygenase isoforms from Klebsiella ATCC 8724. Biochemistry. 47: 2428-38. PMID 18237192 DOI: 10.1021/Bi7004152  0.618
2006 Ju T, Goldsmith RB, Chai SC, Maroney MJ, Pochapsky SS, Pochapsky TC. One protein, two enzymes revisited: a structural entropy switch interconverts the two isoforms of acireductone dioxygenase. Journal of Molecular Biology. 363: 823-34. PMID 16989860 DOI: 10.1016/J.Jmb.2006.08.060  0.588
2006 Chai SC, Bruyere JR, Maroney MJ. Probes of the catalytic site of cysteine dioxygenase. The Journal of Biological Chemistry. 281: 15774-9. PMID 16611641 DOI: 10.1074/Jbc.M601269200  0.597
2005 Chai SC, Jerkins AA, Banik JJ, Shalev I, Pinkham JL, Uden PC, Maroney MJ. Heterologous expression, purification, and characterization of recombinant rat cysteine dioxygenase. The Journal of Biological Chemistry. 280: 9865-9. PMID 15623508 DOI: 10.1074/Jbc.M413733200  0.583
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