| Year |
Citation |
Score |
| 2023 |
Dexheimer TS, Coussens NP, Silvers T, Wright J, Morris J, Doroshow JH, Teicher BA. Multicellular Complex Tumor Spheroid Response to DNA Repair Inhibitors in Combination with DNA-damaging Drugs. Cancer Research Communications. 3: 1648-1661. PMID 37637936 DOI: 10.1158/2767-9764.CRC-23-0193 |
0.407 |
|
| 2020 |
Liu M, Sui D, Dexheimer T, Hovde S, Deng X, Wang KW, Lin HL, Chien HT, Kweon HK, Kuo NS, Ayoub CA, Jimenez-Harrison D, Andrews PC, Kwok R, Bochar DA, et al. Hyperphosphorylation Renders Tau Prone to Aggregate and to Cause Cell Death. Molecular Neurobiology. PMID 32780352 DOI: 10.1007/S12035-020-02034-W |
0.557 |
|
| 2019 |
Sommers JA, Kulikowicz T, Croteau DL, Dexheimer T, Dorjsuren D, Jadhav A, Maloney DJ, Simeonov A, Bohr VA, Brosh RM. A high-throughput screen to identify novel small molecule inhibitors of the Werner Syndrome Helicase-Nuclease (WRN). Plos One. 14: e0210525. PMID 30625228 DOI: 10.1371/Journal.Pone.0210525 |
0.515 |
|
| 2018 |
Kiselev E, Dexheimer TS, Marchand C, Huang SN, Pommier Y. Probing the evolutionary conserved residues Y204, F259, S400 and W590 that shape the catalytic groove of human TDP1 for 3'- and 5'-phosphodiester-DNA bond cleavage. Dna Repair. 66: 64-71. PMID 29747024 DOI: 10.1016/J.Dnarep.2018.05.001 |
0.397 |
|
| 2018 |
Stafford WC, Peng X, Olofsson MH, Zhang X, Luci DK, Lu L, Cheng Q, Trésaugues L, Dexheimer TS, Coussens NP, Augsten M, Ahlzén HM, Orwar O, Östman A, Stone-Elander S, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy. Science Translational Medicine. 10. PMID 29444979 DOI: 10.1126/Scitranslmed.Aaf7444 |
0.391 |
|
| 2017 |
Jun JH, Kumar V, Dexheimer TS, Wedlich I, Nicklaus MC, Pommier Y, Malhotra SV. Synthesis, anti-cancer screening and tyrosyl-DNA phosphodiesterase 1 (Tdp1) inhibition activity of novel piperidinyl sulfamides. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation For Pharmaceutical Sciences. PMID 29037996 DOI: 10.1016/J.Ejps.2017.10.017 |
0.434 |
|
| 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 |
0.33 |
|
| 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 |
0.432 |
|
| 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 |
0.446 |
|
| 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 |
0.443 |
|
| 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 |
0.31 |
|
| 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 |
0.465 |
|
| 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 |
0.485 |
|
| 2014 |
Dexheimer TS, Rosenthal AS, Luci D, Liang Q, Villamil MA, Jadhav A, Simeonov A, Zhuang Z, Maloney DJ. Abstract LB-11: Discovery, synthesis, and structure-activity relationship of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against non-small cell lung cancer Cancer Research. 74. DOI: 10.1158/1538-7445.Am2014-Lb-11 |
0.435 |
|
| 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 |
0.346 |
|
| 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 |
0.536 |
|
| 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 |
0.436 |
|
| 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 |
0.439 |
|
| 2013 |
Huang SN, Murai J, Rosa ID, Dexheimer TS, Gmeiner WH, Pommier Y. Abstract C79: TDP1 repairs nuclear and mitochondrial DNA damage induced by chain-terminating anticancer and antiviral nucleoside analogs. Molecular Cancer Therapeutics. 12. DOI: 10.1158/1535-7163.Targ-13-C79 |
0.439 |
|
| 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 |
0.463 |
|
| 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 |
0.419 |
|
| 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 |
0.495 |
|
| 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 |
0.429 |
|
| 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 |
0.319 |
|
| 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 |
0.462 |
|
| 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 |
0.401 |
|
| 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). Bioorganic & Medicinal Chemistry. 18: 2347-2355. PMID 30025429 DOI: 10.1016/J.Bmc.2010.02.009 |
0.461 |
|
| 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 |
0.468 |
|
| 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 |
0.444 |
|
| 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 |
0.414 |
|
| 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 |
0.404 |
|
| 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 |
0.512 |
|
| 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 |
0.446 |
|
| 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 |
0.458 |
|
| 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 |
0.37 |
|
| 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 |
0.42 |
|
| 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 |
0.517 |
|
| 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 |
0.451 |
|
| 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 |
0.383 |
|
| 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 |
0.561 |
|
| 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 |
0.493 |
|
| 2009 |
Sooryakumar D, Dexheimer T, Teicher BA, Pommier Y. Abstract C219: Molecular and cellular pharmacology of the novel non‐camptothecin topoisomerase I inhibitor, GENZ644282 Molecular Cancer Therapeutics. 8. DOI: 10.1158/1535-7163.Targ-09-C219 |
0.395 |
|
| 2009 |
Stephen AG, Dexheimer TS, Marchand C, Pommier Y, Fisher RJ. Tyrosyl-DNA Phosphodiesterase Binds Nucleic Acids Preferentially At The 3′ End Biophysical Journal. 96: 417a. DOI: 10.1016/J.Bpj.2008.12.2132 |
0.373 |
|
| 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 |
0.51 |
|
| 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 |
0.469 |
|
| 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 |
0.443 |
|
| 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 |
0.378 |
|
| 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 |
0.493 |
|
| 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 |
0.421 |
|
| 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 |
0.354 |
|
| 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 |
0.507 |
|
| 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 |
0.329 |
|
| 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 |
0.517 |
|
| 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 |
0.598 |
|
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