Thomas S. Dexheimer, Ph.D. - Publications

Affiliations: 
2006 University of Arizona, Tucson, AZ 
Area:
Pharmacy, Molecular Biology

44 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
2019 Kahl D, Hutchings KM, Lisabeth EM, Haak A, Leipprandt JR, Dexheimer TS, Khanna D, Tsou PS, Campbell PL, Fox DA, Wen B, Sun D, Bailie M, Neubig RR, Larsen SD. 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Reponse Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma. Journal of Medicinal Chemistry. PMID 30951312 DOI: 10.1021/acs.jmedchem.8b01772  0.52
2015 Lee JA, Shinn P, Jaken S, Oliver S, Willard FS, Heidler S, Peery RB, Oler J, Chu S, Southall N, Dexheimer TS, Smallwood J, Huang R, Guha R, Jadhav A, et al. Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays. Plos One. 10: e0130796. PMID 26177200 DOI: 10.1371/journal.pone.0130796  0.52
2014 Gormally MV, Dexheimer TS, Marsico G, Sanders DA, Lowe C, Matak-Vinkovi? D, Michael S, Jadhav A, Rai G, Maloney DJ, Simeonov A, Balasubramanian S. Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition. Nature Communications. 5: 5165. PMID 25387393 DOI: 10.1038/ncomms6165  0.52
2014 Guo D, Dexheimer TS, Pommier Y, Nash HA. Neuroprotection and repair of 3'-blocking DNA ends by glaikit (gkt) encoding Drosophila tyrosyl-DNA phosphodiesterase 1 (TDP1). Proceedings of the National Academy of Sciences of the United States of America. 111: 15816-20. PMID 25331878 DOI: 10.1073/pnas.1415011111  0.52
2014 Dexheimer TS, Rosenthal AS, Luci DK, Liang Q, Villamil MA, Chen J, Sun H, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ. Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer. Journal of Medicinal Chemistry. 57: 8099-110. PMID 25229643 DOI: 10.1021/jm5010495  0.52
2014 Carver J, Dexheimer TS, Hsu D, Weng MT, Smith JL, Guha R, Jadhav A, Simeonov A, Luo J. A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein. Plos One. 9: e103836. PMID 25093678 DOI: 10.1371/journal.pone.0103836  0.52
2014 Marchand C, Huang SY, Dexheimer TS, Lea WA, Mott BT, Chergui A, Naumova A, Stephen AG, Rosenthal AS, Rai G, Murai J, Gao R, Maloney DJ, Jadhav A, Jorgensen WL, et al. Biochemical assays for the discovery of TDP1 inhibitors. Molecular Cancer Therapeutics. 13: 2116-26. PMID 25024006 DOI: 10.1158/1535-7163.MCT-13-0952  0.52
2014 Liang Q, Dexheimer TS, Zhang P, Rosenthal AS, Villamil MA, You C, Zhang Q, Chen J, Ott CA, Sun H, Luci DK, Yuan B, Simeonov A, Jadhav A, Xiao H, et al. A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses. Nature Chemical Biology. 10: 298-304. PMID 24531842 DOI: 10.1038/nchembio.1455  0.52
2014 Dexheimer TS. DNA repair pathways and mechanisms Dna Repair of Cancer Stem Cells. 19-32. DOI: 10.1007/978-94-007-4590-2_2  0.52
2013 Rosenthal AS, Dexheimer TS, Gileadi O, Nguyen GH, Chu WK, Hickson ID, Jadhav A, Simeonov A, Maloney DJ. Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase. Bioorganic & Medicinal Chemistry Letters. 23: 5660-6. PMID 24012121 DOI: 10.1016/j.bmcl.2013.08.025  0.52
2013 Huang SY, Murai J, Dalla Rosa I, Dexheimer TS, Naumova A, Gmeiner WH, Pommier Y. TDP1 repairs nuclear and mitochondrial DNA damage induced by chain-terminating anticancer and antiviral nucleoside analogs. Nucleic Acids Research. 41: 7793-803. PMID 23775789 DOI: 10.1093/nar/gkt483  0.52
2013 Nguyen GH, Dexheimer TS, Rosenthal AS, Chu WK, Singh DK, Mosedale G, Bachrati CZ, Schultz L, Sakurai M, Savitsky P, Abu M, McHugh PJ, Bohr VA, Harris CC, Jadhav A, et al. A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells. Chemistry & Biology. 20: 55-62. PMID 23352139 DOI: 10.1016/j.chembiol.2012.10.016  0.52
2012 Murai J, Huang SY, Das BB, Dexheimer TS, Takeda S, Pommier Y. Tyrosyl-DNA phosphodiesterase 1 (TDP1) repairs DNA damage induced by topoisomerases I and II and base alkylation in vertebrate cells. The Journal of Biological Chemistry. 287: 12848-57. PMID 22375014 DOI: 10.1074/jbc.M111.333963  0.52
2011 Chen J, Dexheimer TS, Ai Y, Liang Q, Villamil MA, Inglese J, Maloney DJ, Jadhav A, Simeonov A, Zhuang Z. Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells. Chemistry & Biology. 18: 1390-400. PMID 22118673 DOI: 10.1016/j.chembiol.2011.08.014  0.52
2011 Kiselev E, DeGuire S, Morrell A, Agama K, Dexheimer TS, Pommier Y, Cushman M. 7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents. Journal of Medicinal Chemistry. 54: 6106-16. PMID 21823606 DOI: 10.1021/jm200719v  0.52
2011 Peterson KE, Cinelli MA, Morrell AE, Mehta A, Dexheimer TS, Agama K, Antony S, Pommier Y, Cushman M. Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity. Journal of Medicinal Chemistry. 54: 4937-53. PMID 21710981 DOI: 10.1021/jm101338z  0.52
2011 Guha R, Dexheimer TS, Kestranek AN, Jadhav A, Chervenak AM, Ford MG, Simeonov A, Roth GP, Thomas CJ. Exploratory analysis of kinetic solubility measurements of a small molecule library. Bioorganic & Medicinal Chemistry. 19: 4127-34. PMID 21640593 DOI: 10.1016/j.bmc.2011.05.005  0.52
2011 Sooryakumar D, Dexheimer TS, Teicher BA, Pommier Y. Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282. Molecular Cancer Therapeutics. 10: 1490-9. PMID 21636699 DOI: 10.1158/1535-7163.MCT-10-1043  0.52
2011 Prast-Nielsen S, Dexheimer TS, Schultz L, Stafford WC, Cheng Q, Xu J, Jadhav A, Arnér ES, Simeonov A. Inhibition of thioredoxin reductase 1 by porphyrins and other small molecules identified by a high-throughput screening assay. Free Radical Biology & Medicine. 50: 1114-23. PMID 21262347 DOI: 10.1016/j.freeradbiomed.2011.01.020  0.52
2010 Kiselev E, Dexheimer TS, Pommier Y, Cushman M. Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents. Journal of Medicinal Chemistry. 53: 8716-26. PMID 21090809 DOI: 10.1021/jm101048k  0.52
2010 Das BB, Dexheimer TS, Maddali K, Pommier Y. Role of tyrosyl-DNA phosphodiesterase (TDP1) in mitochondria. Proceedings of the National Academy of Sciences of the United States of America. 107: 19790-5. PMID 21041670 DOI: 10.1073/pnas.1009814107  0.52
2010 Cinelli MA, Morrell AE, Dexheimer TS, Agama K, Agrawal S, Pommier Y, Cushman M. The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode. Bioorganic & Medicinal Chemistry. 18: 5535-52. PMID 20630766 DOI: 10.1016/j.bmc.2010.06.040  0.52
2010 Song Y, Shao Z, Dexheimer TS, Scher ES, Pommier Y, Cushman M. Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors. Journal of Medicinal Chemistry. 53: 1979-89. PMID 20155916 DOI: 10.1021/jm901649x  0.52
2010 Gheeya J, Johansson P, Chen QR, Dexheimer T, Metaferia B, Song YK, Wei JS, He J, Pommier Y, Khan J. Expression profiling identifies epoxy anthraquinone derivative as a DNA topoisomerase inhibitor Cancer Letters. 293: 124-131. PMID 20133050 DOI: 10.1016/j.canlet.2010.01.004  0.52
2010 Dexheimer TS, Stephen AG, Fivash MJ, Fisher RJ, Pommier Y. The DNA binding and 3'-end preferential activity of human tyrosyl-DNA phosphodiesterase. Nucleic Acids Research. 38: 2444-52. PMID 20097655 DOI: 10.1093/nar/gkp1206  0.52
2010 Weidlich IE, Dexheimer T, Marchand C, Antony S, Pommier Y, Nicklaus MC. Inhibitors of human tyrosyl-DNA phospodiesterase (hTdp1) developed by virtual screening using ligand-based pharmacophores. Bioorganic & Medicinal Chemistry. 18: 182-9. PMID 19963390 DOI: 10.1016/j.bmc.2009.11.008  0.52
2010 Weidlich IE, Dexheimer TS, Marchand C, Antony S, Pommier Y, Nicklaus MC. Virtual screening using ligand-based pharmacophores for inhibitors of human tyrosyl-DNA phospodiesterase (hTdp1) (DOI:10.1016/j.bmc.2010.02.008) Bioorganic and Medicinal Chemistry. 18: 2347-2355. DOI: 10.1016/j.bmc.2010.02.009  0.52
2010 Weidlich IE, Dexheimer T, Marchand C, Antony S, Pommier Y, Nicklaus MC. Corrigendum to "Inhibitors of human tyrosyl-DNA phospodiesterase (hTdp1) developed by virtual screening using ligand-based pharmacophores" [Bioorg. Med. Chem. 18 (2010) 182-189] Bioorganic and Medicinal Chemistry. 18: 2346. DOI: 10.1016/j.bmc.2010.02.008  0.52
2009 Dexheimer TS, Gediya LK, Stephen AG, Weidlich I, Antony S, Marchand C, Interthal H, Nicklaus M, Fisher RJ, Njar VC, Pommier Y. 4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors. Journal of Medicinal Chemistry. 52: 7122-31. PMID 19883083 DOI: 10.1021/jm901061s  0.52
2009 Das BB, Antony S, Gupta S, Dexheimer TS, Redon CE, Garfield S, Shiloh Y, Pommier Y. Optimal function of the DNA repair enzyme TDP1 requires its phosphorylation by ATM and/or DNA-PK. The Embo Journal. 28: 3667-80. PMID 19851285 DOI: 10.1038/emboj.2009.302  0.52
2009 Cinelli MA, Cordero B, Dexheimer TS, Pommier Y, Cushman M. Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships. Bioorganic & Medicinal Chemistry. 17: 7145-55. PMID 19783447 DOI: 10.1016/j.bmc.2009.08.066  0.52
2009 Dexheimer TS, Carey SS, Zuohe S, Gokhale VM, Hu X, Murata LB, Maes EM, Weichsel A, Sun D, Meuillet EJ, Montfort WR, Hurley LH. NM23-H2 may play an indirect role in transcriptional activation of c-myc gene expression but does not cleave the nuclease hypersensitive element III(1). Molecular Cancer Therapeutics. 8: 1363-77. PMID 19435876 DOI: 10.1158/1535-7163.MCT-08-1093  0.52
2009 Marchand C, Lea WA, Jadhav A, Dexheimer TS, Austin CP, Inglese J, Pommier Y, Simeonov A. Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay. Molecular Cancer Therapeutics. 8: 240-8. PMID 19139134 DOI: 10.1158/1535-7163.MCT-08-0878  0.52
2008 Dexheimer TS, Pommier Y. DNA cleavage assay for the identification of topoisomerase I inhibitors. Nature Protocols. 3: 1736-50. PMID 18927559 DOI: 10.1038/nprot.2008.174  0.52
2008 Goswami A, Qiu S, Dexheimer TS, Ranganathan P, Burikhanov R, Pommier Y, Rangnekar VM. Par-4 binds to topoisomerase 1 and attenuates its DNA relaxation activity. Cancer Research. 68: 6190-8. PMID 18676842 DOI: 10.1158/0008-5472.CAN-08-0831  0.52
2008 Cinelli MA, Morrell A, Dexheimer TS, Scher ES, Pommier Y, Cushman M. Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors. Journal of Medicinal Chemistry. 51: 4609-19. PMID 18630891 DOI: 10.1021/jm800259e  0.52
2008 Dexheimer TS, Kozekova A, Rizzo CJ, Stone MP, Pommier Y. The modulation of topoisomerase I-mediated DNA cleavage and the induction of DNA-topoisomerase I crosslinks by crotonaldehyde-derived DNA adducts. Nucleic Acids Research. 36: 4128-36. PMID 18550580 DOI: 10.1093/nar/gkn334  0.52
2008 Dexheimer TS, Antony S, Marchand C, Pommier Y. Tyrosyl-DNA phosphodiesterase as a target for anticancer therapy. Anti-Cancer Agents in Medicinal Chemistry. 8: 381-9. PMID 18473723 DOI: 10.2174/187152008784220357  0.52
2007 Takagi K, Dexheimer TS, Redon C, Sordet O, Agama K, Lavielle G, Pierré A, Bates SE, Pommier Y. Novel E-ring camptothecin keto analogues (S38809 and S39625) are stable, potent, and selective topoisomerase I inhibitors without being substrates of drug efflux transporters. Molecular Cancer Therapeutics. 6: 3229-38. PMID 18089716 DOI: 10.1158/1535-7163.MCT-07-0441  0.52
2007 Morrell A, Placzek M, Parmley S, Antony S, Dexheimer TS, Pommier Y, Cushman M. Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization. Journal of Medicinal Chemistry. 50: 4419-30. PMID 17696418 DOI: 10.1021/jm070361q  0.52
2006 Dexheimer TS, Sun D, Hurley LH. Deconvoluting the structural and drug-recognition complexity of the G-quadruplex-forming region upstream of the bcl-2 P1 promoter. Journal of the American Chemical Society. 128: 5404-15. PMID 16620112 DOI: 10.1021/ja0563861  0.52
2006 Dai J, Dexheimer TS, Chen D, Carver M, Ambrus A, Jones RA, Yang D. An intramolecular G-quadruplex structure with mixed parallel/antiparallel G-strands formed in the human BCL-2 promoter region in solution. Journal of the American Chemical Society. 128: 1096-8. PMID 16433524 DOI: 10.1021/ja055636a  0.52
2005 Fellows IM, Schwaebe M, Dexheimer TS, Vankayalapati H, Gleason-Guzman M, Whitten JP, Hurley LH. Determination of the importance of the stereochemistry of psorospermin in topoisomerase II-induced alkylation of DNA and in vitro and in vivo biological activity. Molecular Cancer Therapeutics. 4: 1729-39. PMID 16275994 DOI: 10.1158/1535-7163.MCT-05-0183  0.52
2005 Heald RA, Dexheimer TS, Vankayalapati H, Siddiqui-Jain A, Szabo LZ, Gleason-Guzman MC, Hurley LH. Conformationally restricted analogues of psorospermin: design, synthesis, and bioactivity of natural-product-related bisfuranoxanthones. Journal of Medicinal Chemistry. 48: 2993-3004. PMID 15828838 DOI: 10.1021/jm049299c  0.52
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