Sort by
Items per page

Send to

Choose Destination

Search results

Items: 49


Identifying chemopreventive agents for obesity-associated cancers using an efficient, 3D high-throughput transformation assay.

Benham V, Bullard B, Dexheimer TS, Bernard MP, Neubig RR, Liby KT, Bernard JJ.

Sci Rep. 2019 Jul 16;9(1):10278. doi: 10.1038/s41598-019-46531-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.

Kiselev E, Dexheimer TS, Marchand C, Huang SN, Pommier Y.

DNA Repair (Amst). 2018 Jun - Jul;66-67:64-71. doi: 10.1016/j.dnarep.2018.05.001. Epub 2018 May 2.


Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy.

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, Maloney DJ, Jadhav A, Simeonov A, Linder S, Arnér ESJ.

Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444. doi: 10.1126/scitranslmed.aaf7444.


Synthesis, anti-cancer screening and tyrosyl-DNA phosphodiesterase 1 (Tdp1) inhibition activity of novel piperidinyl sulfamides.

Jun JH, Kumar V, Dexheimer TS, Wedlich I, Nicklaus MC, Pommier Y, Malhotra SV.

Eur J Pharm Sci. 2018 Jan 1;111:337-348. doi: 10.1016/j.ejps.2017.10.017. Epub 2017 Oct 13.


Small Molecule Enhancement of 20S Proteasome Activity Targets Intrinsically Disordered Proteins.

Jones CL, Njomen E, Sjögren B, Dexheimer TS, Tepe JJ.

ACS Chem Biol. 2017 Sep 15;12(9):2240-2247. doi: 10.1021/acschembio.7b00489. Epub 2017 Aug 1.


Chemerin-induced arterial contraction is Gi- and calcium-dependent.

Ferland DJ, Darios ES, Neubig RR, Sjögren B, Truong N, Torres R, Dexheimer TS, Thompson JM, Watts SW.

Vascul Pharmacol. 2017 Jan;88:30-41. doi: 10.1016/j.vph.2016.11.009. Epub 2016 Nov 24.


A Platform to Enable the Pharmacological Profiling of Small Molecules in Gel-Based Electrophoretic Mobility Shift Assays.

Foley TL, Dorjsuren D, Dexheimer TS, Burkart MD, Wight WC, Simeonov A.

J Biomol Screen. 2016 Dec;21(10):1125-1131. doi: 10.1177/1087057116652895. Epub 2016 Jul 10.


Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays.

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, Cox K, Austin CP, Simeonov A, Sittampalam GS, Husain S, Franklin N, Wild DJ, Yang JJ, Sutherland JJ, Thomas CJ.

PLoS One. 2015 Jul 15;10(7):e0130796. doi: 10.1371/journal.pone.0130796. eCollection 2015.


Discovery of ML323 as a Novel Inhibitor of the USP1/UAF1 Deubiquitinase Complex.

Dexheimer TS, Rosenthal AS, Liang Q, Chen J, Villamil MA, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Oct 23 [updated 2014 Sep 18].


Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition.

Gormally MV, Dexheimer TS, Marsico G, Sanders DA, Lowe C, Matak-Vinković D, Michael S, Jadhav A, Rai G, Maloney DJ, Simeonov A, Balasubramanian S.

Nat Commun. 2014 Nov 12;5:5165. doi: 10.1038/ncomms6165.


Neuroprotection and repair of 3'-blocking DNA ends by glaikit (gkt) encoding Drosophila tyrosyl-DNA phosphodiesterase 1 (TDP1).

Guo D, Dexheimer TS, Pommier Y, Nash HA.

Proc Natl Acad Sci U S A. 2014 Nov 4;111(44):15816-20. doi: 10.1073/pnas.1415011111. Epub 2014 Oct 20.


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.

Dexheimer TS, Rosenthal AS, Luci DK, Liang Q, Villamil MA, Chen J, Sun H, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ.

J Med Chem. 2014 Oct 9;57(19):8099-110. doi: 10.1021/jm5010495. Epub 2014 Sep 17.


A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein.

Carver J, Dexheimer TS, Hsu D, Weng MT, Smith JL, Guha R, Jadhav A, Simeonov A, Luo J.

PLoS One. 2014 Aug 5;9(8):e103836. doi: 10.1371/journal.pone.0103836. eCollection 2014.


Biochemical assays for the discovery of TDP1 inhibitors.

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, Simeonov A, Pommier Y.

Mol Cancer Ther. 2014 Aug;13(8):2116-26. doi: 10.1158/1535-7163.MCT-13-0952. Epub 2014 Jul 14.


A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.

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, Wang Y, Maloney DJ, Zhuang Z.

Nat Chem Biol. 2014 Apr;10(4):298-304. doi: 10.1038/nchembio.1455. Epub 2014 Feb 16.


Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity.

Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U, Jadhav A, Simeonov A, Kristie TM, Maloney DJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 17 [updated 2013 Sep 16].


Discovery of ML216, a Small Molecule Inhibitor of Bloom (BLM) Helicase.

Rosenthal AS, Dexheimer TS, Nguyen G, Gileadi O, Vindigni A, Simeonov A, Jadhav A, Hickson I, Maloney DJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 15 [updated 2013 Feb 28].


Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.

Rosenthal AS, Dexheimer TS, Gileadi O, Nguyen GH, Chu WK, Hickson ID, Jadhav A, Simeonov A, Maloney DJ.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5660-6. doi: 10.1016/j.bmcl.2013.08.025. Epub 2013 Aug 13.


TDP1 repairs nuclear and mitochondrial DNA damage induced by chain-terminating anticancer and antiviral nucleoside analogs.

Huang SY, Murai J, Dalla Rosa I, Dexheimer TS, Naumova A, Gmeiner WH, Pommier Y.

Nucleic Acids Res. 2013 Sep;41(16):7793-803. doi: 10.1093/nar/gkt483. Epub 2013 Jun 17.


A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells.

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, Gileadi O, Maloney DJ, Simeonov A, Hickson ID.

Chem Biol. 2013 Jan 24;20(1):55-62. doi: 10.1016/j.chembiol.2012.10.016.


Tyrosyl-DNA phosphodiesterase 1 (TDP1) repairs DNA damage induced by topoisomerases I and II and base alkylation in vertebrate cells.

Murai J, Huang SY, Das BB, Dexheimer TS, Takeda S, Pommier Y.

J Biol Chem. 2012 Apr 13;287(16):12848-57. doi: 10.1074/jbc.M111.333963. Epub 2012 Feb 27.


Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells.

Chen J, Dexheimer TS, Ai Y, Liang Q, Villamil MA, Inglese J, Maloney DJ, Jadhav A, Simeonov A, Zhuang Z.

Chem Biol. 2011 Nov 23;18(11):1390-400. doi: 10.1016/j.chembiol.2011.08.014.


7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.

Kiselev E, DeGuire S, Morrell A, Agama K, Dexheimer TS, Pommier Y, Cushman M.

J Med Chem. 2011 Sep 8;54(17):6106-16. doi: 10.1021/jm200719v. Epub 2011 Aug 8.


Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.

Peterson KE, Cinelli MA, Morrell AE, Mehta A, Dexheimer TS, Agama K, Antony S, Pommier Y, Cushman M.

J Med Chem. 2011 Jul 28;54(14):4937-53. doi: 10.1021/jm101338z. Epub 2011 Jun 28.


Exploratory analysis of kinetic solubility measurements of a small molecule library.

Guha R, Dexheimer TS, Kestranek AN, Jadhav A, Chervenak AM, Ford MG, Simeonov A, Roth GP, Thomas CJ.

Bioorg Med Chem. 2011 Jul 1;19(13):4127-34. doi: 10.1016/j.bmc.2011.05.005. Epub 2011 May 13.


Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282.

Sooryakumar D, Dexheimer TS, Teicher BA, Pommier Y.

Mol Cancer Ther. 2011 Aug;10(8):1490-9. doi: 10.1158/1535-7163.MCT-10-1043. Epub 2011 Jun 2.


Inhibition of thioredoxin reductase 1 by porphyrins and other small molecules identified by a high-throughput screening assay.

Prast-Nielsen S, Dexheimer TS, Schultz L, Stafford WC, Cheng Q, Xu J, Jadhav A, Arnér ES, Simeonov A.

Free Radic Biol Med. 2011 May 1;50(9):1114-23. doi: 10.1016/j.freeradbiomed.2011.01.020. Epub 2011 Jan 22.


Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.

Kiselev E, Dexheimer TS, Pommier Y, Cushman M.

J Med Chem. 2010 Dec 23;53(24):8716-26. doi: 10.1021/jm101048k. Epub 2010 Nov 23.


Role of tyrosyl-DNA phosphodiesterase (TDP1) in mitochondria.

Das BB, Dexheimer TS, Maddali K, Pommier Y.

Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):19790-5. doi: 10.1073/pnas.1009814107. Epub 2010 Nov 1.


The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.

Cinelli MA, Morrell AE, Dexheimer TS, Agama K, Agrawal S, Pommier Y, Cushman M.

Bioorg Med Chem. 2010 Aug 1;18(15):5535-52. doi: 10.1016/j.bmc.2010.06.040. Epub 2010 Jun 20.


Virtual screening using ligand-based pharmacophores for inhibitors of human tyrosyl-DNA phospodiesterase (hTdp1).

Weidlich IE, Dexheimer TS, Marchand C, Antony S, Pommier Y, Nicklaus MC.

Bioorg Med Chem. 2010 Mar 15;18(6):2347-2355. doi: 10.1016/j.bmc.2010.02.009. Epub 2010 Mar 2.


Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.

Song Y, Shao Z, Dexheimer TS, Scher ES, Pommier Y, Cushman M.

J Med Chem. 2010 Mar 11;53(5):1979-89. doi: 10.1021/jm901649x.


The DNA binding and 3'-end preferential activity of human tyrosyl-DNA phosphodiesterase.

Dexheimer TS, Stephen AG, Fivash MJ, Fisher RJ, Pommier Y.

Nucleic Acids Res. 2010 Apr;38(7):2444-52. doi: 10.1093/nar/gkp1206. Epub 2010 Jan 21.


4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors.

Dexheimer TS, Gediya LK, Stephen AG, Weidlich I, Antony S, Marchand C, Interthal H, Nicklaus M, Fisher RJ, Njar VC, Pommier Y.

J Med Chem. 2009 Nov 26;52(22):7122-31. doi: 10.1021/jm901061s.


Optimal function of the DNA repair enzyme TDP1 requires its phosphorylation by ATM and/or DNA-PK.

Das BB, Antony S, Gupta S, Dexheimer TS, Redon CE, Garfield S, Shiloh Y, Pommier Y.

EMBO J. 2009 Dec 2;28(23):3667-80. doi: 10.1038/emboj.2009.302. Epub 2009 Oct 22.


Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.

Cinelli MA, Cordero B, Dexheimer TS, Pommier Y, Cushman M.

Bioorg Med Chem. 2009 Oct 15;17(20):7145-55. doi: 10.1016/j.bmc.2009.08.066. Epub 2009 Sep 6.


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).

Dexheimer TS, Carey SS, Zuohe S, Gokhale VM, Hu X, Murata LB, Maes EM, Weichsel A, Sun D, Meuillet EJ, Montfort WR, Hurley LH.

Mol Cancer Ther. 2009 May;8(5):1363-77. doi: 10.1158/1535-7163.MCT-08-1093. Epub 2009 May 12.


Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay.

Marchand C, Lea WA, Jadhav A, Dexheimer TS, Austin CP, Inglese J, Pommier Y, Simeonov A.

Mol Cancer Ther. 2009 Jan;8(1):240-8. doi: 10.1158/1535-7163.MCT-08-0878.


DNA cleavage assay for the identification of topoisomerase I inhibitors.

Dexheimer TS, Pommier Y.

Nat Protoc. 2008;3(11):1736-50. doi: 10.1038/nprot.2008.174.


Par-4 binds to topoisomerase 1 and attenuates its DNA relaxation activity.

Goswami A, Qiu S, Dexheimer TS, Ranganathan P, Burikhanov R, Pommier Y, Rangnekar VM.

Cancer Res. 2008 Aug 1;68(15):6190-8. doi: 10.1158/0008-5472.CAN-08-0831.


Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.

Cinelli MA, Morrell A, Dexheimer TS, Scher ES, Pommier Y, Cushman M.

J Med Chem. 2008 Aug 14;51(15):4609-19. doi: 10.1021/jm800259e. Epub 2008 Jul 17.


The modulation of topoisomerase I-mediated DNA cleavage and the induction of DNA-topoisomerase I crosslinks by crotonaldehyde-derived DNA adducts.

Dexheimer TS, Kozekova A, Rizzo CJ, Stone MP, Pommier Y.

Nucleic Acids Res. 2008 Jul;36(12):4128-36. doi: 10.1093/nar/gkn334. Epub 2008 Jun 10.


Tyrosyl-DNA phosphodiesterase as a target for anticancer therapy.

Dexheimer TS, Antony S, Marchand C, Pommier Y.

Anticancer Agents Med Chem. 2008 May;8(4):381-9. Review.


Novel E-ring camptothecin keto analogues (S38809 and S39625) are stable, potent, and selective topoisomerase I inhibitors without being substrates of drug efflux transporters.

Takagi K, Dexheimer TS, Redon C, Sordet O, Agama K, Lavielle G, Pierré A, Bates SE, Pommier Y.

Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3229-38.


Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.

Morrell A, Placzek M, Parmley S, Antony S, Dexheimer TS, Pommier Y, Cushman M.

J Med Chem. 2007 Sep 6;50(18):4419-30. Epub 2007 Aug 15.


An intramolecular G-quadruplex structure with mixed parallel/antiparallel G-strands formed in the human BCL-2 promoter region in solution.

Dai J, Dexheimer TS, Chen D, Carver M, Ambrus A, Jones RA, Yang D.

J Am Chem Soc. 2006 Feb 1;128(4):1096-8.


Determination of the importance of the stereochemistry of psorospermin in topoisomerase II-induced alkylation of DNA and in vitro and in vivo biological activity.

Fellows IM, Schwaebe M, Dexheimer TS, Vankayalapati H, Gleason-Guzman M, Whitten JP, Hurley LH.

Mol Cancer Ther. 2005 Nov;4(11):1729-39.


Conformationally restricted analogues of psorospermin: design, synthesis, and bioactivity of natural-product-related bisfuranoxanthones.

Heald RA, Dexheimer TS, Vankayalapati H, Siddiqui-Jain A, Szabo LZ, Gleason-Guzman MC, Hurley LH.

J Med Chem. 2005 Apr 21;48(8):2993-3004.


Supplemental Content

Loading ...
Support Center