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Novel fluoroindenoisoquinoline non-camptothecin topoisomerase I inhibitors.

Marzi L, Agama K, Murai J, Difilippantonio S, James A, Peer CJ, Figg WD, Beck D, Elsayed MSA, Cushman M, Pommier Y.

Mol Cancer Ther. 2018 May 10. pii: molcanther.0028.2018. doi: 10.1158/1535-7163.MCT-18-0028. [Epub ahead of print]


Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2).

Yu LM, Hu Z, Chen Y, Ravji A, Lopez S, Plescia CB, Yu Q, Yang H, Abdelmalak M, Saha S, Agama K, Kiselev E, Marchand C, Pommier Y, An LK.

Eur J Med Chem. 2018 May 10;151:777-796. doi: 10.1016/j.ejmech.2018.04.024. Epub 2018 Apr 12.


Mitochondrial tyrosyl-DNA phosphodiesterase 2 and its TDP2S short isoform.

Huang SN, Dalla Rosa I, Michaels SA, Tulumello DV, Agama K, Khiati S, Jean SR, Baechler SA, Factor VM, Varma S, Murai J, Miller Jenkins LM, Kelley SO, Pommier Y.

EMBO Rep. 2018 Mar;19(3). pii: e42139. doi: 10.15252/embr.201642139. Epub 2018 Feb 9.


ALC1/CHD1L, a chromatin-remodeling enzyme, is required for efficient base excision repair.

Tsuda M, Cho K, Ooka M, Shimizu N, Watanabe R, Yasui A, Nakazawa Y, Ogi T, Harada H, Agama K, Nakamura J, Asada R, Fujiike H, Sakuma T, Yamamoto T, Murai J, Hiraoka M, Koike K, Pommier Y, Takeda S, Hirota K.

PLoS One. 2017 Nov 17;12(11):e0188320. doi: 10.1371/journal.pone.0188320. eCollection 2017.


Distribution bias and biochemical characterization of TOP1MT single nucleotide variants.

Zhang H, Seol Y, Agama K, Neuman KC, Pommier Y.

Sci Rep. 2017 Aug 17;7(1):8614. doi: 10.1038/s41598-017-09258-2.


Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.

Elsayed MSA, Su Y, Wang P, Sethi T, Agama K, Ravji A, Redon CE, Kiselev E, Horzmann KA, Freeman JL, Pommier Y, Cushman M.

J Med Chem. 2017 Jul 13;60(13):5364-5376. doi: 10.1021/acs.jmedchem.6b01870. Epub 2017 Jun 28.


Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).

Wang P, Elsayed MSA, Plescia CB, Ravji A, Redon CE, Kiselev E, Marchand C, Zeleznik O, Agama K, Pommier Y, Cushman M.

J Med Chem. 2017 Apr 27;60(8):3275-3288. doi: 10.1021/acs.jmedchem.6b01565. Epub 2017 Apr 18.


Phenanthriplatin Acts As a Covalent Poison of Topoisomerase II Cleavage Complexes.

Riddell IA, Agama K, Park GY, Pommier Y, Lippard SJ.

ACS Chem Biol. 2016 Nov 18;11(11):2996-3001. Epub 2016 Oct 6.


Design, Synthesis, and Biological Evaluation of Potential Prodrugs Related to the Experimental Anticancer Agent Indotecan (LMP400).

Lv PC, Elsayed MS, Agama K, Marchand C, Pommier Y, Cushman M.

J Med Chem. 2016 May 26;59(10):4890-9. doi: 10.1021/acs.jmedchem.6b00220. Epub 2016 Apr 20.


Investigation of the Structure-Activity Relationships of Aza-A-Ring Indenoisoquinoline Topoisomerase I Poisons.

Beck DE, Reddy PV, Lv W, Abdelmalak M, Tender GS, Lopez S, Agama K, Marchand C, Pommier Y, Cushman M.

J Med Chem. 2016 Apr 28;59(8):3840-53. doi: 10.1021/acs.jmedchem.6b00003. Epub 2016 Apr 12.


Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a new pair of resistance-associated mutations.

Jensen NF, Agama K, Roy A, Smith DH, Pfister TD, Rømer MU, Zhang HL, Doroshow JH, Knudsen BR, Stenvang J, Brünner N, Pommier Y.

J Exp Clin Cancer Res. 2016 Mar 31;35:56. doi: 10.1186/s13046-016-0335-x.


Analogs of the novel phytohormone, strigolactone, trigger apoptosis and synergize with PARP inhibitors by inducing DNA damage and inhibiting DNA repair.

Croglio MP, Haake JM, Ryan CP, Wang VS, Lapier J, Schlarbaum JP, Dayani Y, Artuso E, Prandi C, Koltai H, Agama K, Pommier Y, Chen Y, Tricoli L, LaRocque JR, Albanese C, Yarden RI.

Oncotarget. 2016 Mar 22;7(12):13984-4001. doi: 10.18632/oncotarget.7414.


Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.

Beck DE, Lv W, Abdelmalak M, Plescia CB, Agama K, Marchand C, Pommier Y, Cushman M.

Bioorg Med Chem. 2016 Apr 1;24(7):1469-79. doi: 10.1016/j.bmc.2016.02.015. Epub 2016 Feb 9.


Single-Molecule Supercoil Relaxation Assay as a Screening Tool to Determine the Mechanism and Efficacy of Human Topoisomerase IB Inhibitors.

Seol Y, Zhang H, Agama K, Lorence N, Pommier Y, Neuman KC.

Mol Cancer Ther. 2015 Nov;14(11):2552-9. doi: 10.1158/1535-7163.MCT-15-0454. Epub 2015 Sep 8.


Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.

Beck DE, Abdelmalak M, Lv W, Reddy PV, Tender GS, O'Neill E, Agama K, Marchand C, Pommier Y, Cushman M.

J Med Chem. 2015 May 14;58(9):3997-4015. doi: 10.1021/acs.jmedchem.5b00303. Epub 2015 Apr 24.


Synthesis and biological evaluation of nitrated 7-, 8-, 9-, and 10-hydroxyindenoisoquinolines as potential dual topoisomerase I (Top1)-tyrosyl-DNA phosphodiesterase I (TDP1) inhibitors.

Nguyen TX, Abdelmalak M, Marchand C, Agama K, Pommier Y, Cushman M.

J Med Chem. 2015 Apr 9;58(7):3188-208. doi: 10.1021/acs.jmedchem.5b00136. Epub 2015 Mar 26.


Synthesis and evaluation of new antitumor 3-aminomethyl-4,11-dihydroxynaphtho[2,3-f]indole-5,10-diones.

Shchekotikhin AE, Glazunova VA, Dezhenkova LG, Luzikov YN, Buyanov VN, Treshalina HM, Lesnaya NA, Romanenko VI, Kaluzhny DN, Balzarini J, Agama K, Pommier Y, Shtil AA, Preobrazhenskaya MN.

Eur J Med Chem. 2014 Oct 30;86:797-805. doi: 10.1016/j.ejmech.2014.09.021. Epub 2014 Sep 8.


Poisoning of mitochondrial topoisomerase I by lamellarin D.

Khiati S, Seol Y, Agama K, Dalla Rosa I, Agrawal S, Fesen K, Zhang H, Neuman KC, Pommier Y.

Mol Pharmacol. 2014 Aug;86(2):193-9. doi: 10.1124/mol.114.092833. Epub 2014 Jun 2.


Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.

Lv PC, Agama K, Marchand C, Pommier Y, Cushman M.

J Med Chem. 2014 May 22;57(10):4324-36. doi: 10.1021/jm500294a. Epub 2014 May 6.


Mapping topoisomerase sites in mitochondrial DNA with a poisonous mitochondrial topoisomerase I (Top1mt).

Dalla Rosa I, Huang SY, Agama K, Khiati S, Zhang H, Pommier Y.

J Biol Chem. 2014 Jun 27;289(26):18595-602. doi: 10.1074/jbc.M114.555367. Epub 2014 May 5.


Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.

Kiselev E, Sooryakumar D, Agama K, Cushman M, Pommier Y.

J Med Chem. 2014 Feb 27;57(4):1289-98. doi: 10.1021/jm401471v. Epub 2014 Feb 6.


Epigenetic and genetic inactivation of tyrosyl-DNA-phosphodiesterase 1 (TDP1) in human lung cancer cells from the NCI-60 panel.

Gao R, Das BB, Chatterjee R, Abaan OD, Agama K, Matuo R, Vinson C, Meltzer PS, Pommier Y.

DNA Repair (Amst). 2014 Jan;13:1-9. doi: 10.1016/j.dnarep.2013.09.001. Epub 2013 Dec 16.


Development of purely structure-based pharmacophores for the topoisomerase I-DNA-ligand binding pocket.

Drwal MN, Agama K, Pommier Y, Griffith R.

J Comput Aided Mol Des. 2013 Dec;27(12):1037-49. doi: 10.1007/s10822-013-9695-x. Epub 2013 Dec 1.


Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

Taliani S, Pugliesi I, Barresi E, Salerno S, Marchand C, Agama K, Simorini F, La Motta C, Marini AM, Di Leva FS, Marinelli L, Cosconati S, Novellino E, Pommier Y, Di Santo R, Da Settimo F.

J Med Chem. 2013 Sep 26;56(18):7458-62. doi: 10.1021/jm400932c. Epub 2013 Sep 16.


Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1).

Conda-Sheridan M, Reddy PV, Morrell A, Cobb BT, Marchand C, Agama K, Chergui A, Renaud A, Stephen AG, Bindu LK, Pommier Y, Cushman M.

J Med Chem. 2013 Jan 10;56(1):182-200. doi: 10.1021/jm3014458. Epub 2012 Dec 21.


Correction to Synthesis and Biological Evaluation of the First Dual Tyrosyl-DNA Phosphodiesterase I (Tdp1)-Topoisomerase I (Top1) Inhibitors.

Nguyen TX, Morrell A, Conda-Sheridan M, Marchand C, Agama K, Bermingham A, Stephen AG, Chergui A, Naumova A, Fisher R, O'Keefe BR, Pommier Y, Cushman M.

J Med Chem. 2012 Aug 23;55(16):7297. Epub 2012 Aug 14. No abstract available.


Dibenzo[c,h][1,5]naphthyridinediones as topoisomerase I inhibitors: design, synthesis, and biological evaluation.

Kiselev E, Empey N, Agama K, Pommier Y, Cushman M.

J Org Chem. 2012 Jun 1;77(11):5167-72. doi: 10.1021/jo3006039. Epub 2012 May 15.


Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase I (Tdp1)-topoisomerase I (Top1) inhibitors.

Nguyen TX, Morrell A, Conda-Sheridan M, Marchand C, Agama K, Bermingham A, Stephen AG, Chergui A, Naumova A, Fisher R, O'Keefe BR, Pommier Y, Cushman M.

J Med Chem. 2012 May 10;55(9):4457-78. doi: 10.1021/jm300335n. Epub 2012 Apr 26. Erratum in: J Med Chem. 2012 Aug 23;55(16):7297. Bermingam, Alun [corrected to Bermingham, Alun].


Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.

Kiselev E, Agama K, Pommier Y, Cushman M.

J Med Chem. 2012 Feb 23;55(4):1682-97. doi: 10.1021/jm201512x. Epub 2012 Feb 13.


Mus81-mediated DNA cleavage resolves replication forks stalled by topoisomerase I-DNA complexes.

Regairaz M, Zhang YW, Fu H, Agama KK, Tata N, Agrawal S, Aladjem MI, Pommier Y.

J Cell Biol. 2011 Nov 28;195(5):739-49. doi: 10.1083/jcb.201104003.


Exploring DNA topoisomerase I ligand space in search of novel anticancer agents.

Drwal MN, Agama K, Wakelin LP, Pommier Y, Griffith R.

PLoS One. 2011;6(9):e25150. doi: 10.1371/journal.pone.0025150. Epub 2011 Sep 22.


Schedule-dependent synergy of histone deacetylase inhibitors with DNA damaging agents in small cell lung cancer.

Luchenko VL, Salcido CD, Zhang Y, Agama K, Komlodi-Pasztor E, Murphy RF, Giaccone G, Pommier Y, Bates SE, Varticovski L.

Cell Cycle. 2011 Sep 15;10(18):3119-28. Epub 2011 Sep 15.


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.


Poly(ADP-ribose) polymerase and XPF-ERCC1 participate in distinct pathways for the repair of topoisomerase I-induced DNA damage in mammalian cells.

Zhang YW, Regairaz M, Seiler JA, Agama KK, Doroshow JH, Pommier Y.

Nucleic Acids Res. 2011 May;39(9):3607-20. doi: 10.1093/nar/gkq1304. Epub 2011 Jan 11.


A novel DNA topoisomerase I inhibitor with different mechanism from camptothecin induces G2/M phase cell cycle arrest to K562 cells.

Wu N, Wu XW, Agama K, Pommier Y, Du J, Li D, Gu LQ, Huang ZS, An LK.

Biochemistry. 2010 Nov 30;49(47):10131-6. doi: 10.1021/bi1009419. Epub 2010 Nov 8.


Rif1 provides a new DNA-binding interface for the Bloom syndrome complex to maintain normal replication.

Xu D, Muniandy P, Leo E, Yin J, Thangavel S, Shen X, Ii M, Agama K, Guo R, Fox D 3rd, Meetei AR, Wilson L, Nguyen H, Weng NP, Brill SJ, Li L, Vindigni A, Pommier Y, Seidman M, Wang W.

EMBO J. 2010 Sep 15;29(18):3140-55. doi: 10.1038/emboj.2010.186. Epub 2010 Aug 13.


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.


Collaborative action of Brca1 and CtIP in elimination of covalent modifications from double-strand breaks to facilitate subsequent break repair.

Nakamura K, Kogame T, Oshiumi H, Shinohara A, Sumitomo Y, Agama K, Pommier Y, Tsutsui KM, Tsutsui K, Hartsuiker E, Ogi T, Takeda S, Taniguchi Y.

PLoS Genet. 2010 Jan 22;6(1):e1000828. doi: 10.1371/journal.pgen.1000828.


Interaction of DNA topoisomerase 1 with DNA intermediates and proteins of base excision repair.

Lebedeva NA, Rechkunova NI, Agama K, Pommier Y, Lavrik OI.

Biochemistry (Mosc). 2009 Nov;74(11):1278-84.


Topoisomerase I levels in the NCI-60 cancer cell line panel determined by validated ELISA and microarray analysis and correlation with indenoisoquinoline sensitivity.

Pfister TD, Reinhold WC, Agama K, Gupta S, Khin SA, Kinders RJ, Parchment RE, Tomaszewski JE, Doroshow JH, Pommier Y.

Mol Cancer Ther. 2009 Jul;8(7):1878-84. doi: 10.1158/1535-7163.MCT-09-0016. Epub 2009 Jul 7.


The iron chelator Dp44mT causes DNA damage and selective inhibition of topoisomerase IIalpha in breast cancer cells.

Rao VA, Klein SR, Agama KK, Toyoda E, Adachi N, Pommier Y, Shacter EB.

Cancer Res. 2009 Feb 1;69(3):948-57. doi: 10.1158/0008-5472.CAN-08-1437. Epub 2009 Jan 27.


The 5' Third of Cauliflower mosaic virus Gene VI Conditions Resistance Breakage in Arabidopsis Ecotype Tsu-0.

Agama K, Beach S, Schoelz J, Leisner SM.

Phytopathology. 2002 Feb;92(2):190-6. doi: 10.1094/PHYTO.2002.92.2.190.


Cauliflower mosaic virus gene VI product N-terminus contains regions involved in resistance-breakage, self-association and interactions with movement protein.

Hapiak M, Li Y, Agama K, Swade S, Okenka G, Falk J, Khandekar S, Raikhy G, Anderson A, Pollock J, Zellner W, Schoelz J, Leisner SM.

Virus Res. 2008 Dec;138(1-2):119-29. doi: 10.1016/j.virusres.2008.09.002. Epub 2008 Oct 28.


Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2.

Kitagaki J, Agama KK, Pommier Y, Yang Y, Weissman AM.

Mol Cancer Ther. 2008 Aug;7(8):2445-54. doi: 10.1158/1535-7163.MCT-08-0063.


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.


Aminoflavone induces oxidative DNA damage and reactive oxidative species-mediated apoptosis in breast cancer cells.

McLean L, Soto U, Agama K, Francis J, Jimenez R, Pommier Y, Sowers L, Brantley E.

Int J Cancer. 2008 Apr 1;122(7):1665-74.


Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistance.

Antony S, Agama KK, Miao ZH, Takagi K, Wright MH, Robles AI, Varticovski L, Nagarajan M, Morrell A, Cushman M, Pommier Y.

Cancer Res. 2007 Nov 1;67(21):10397-405. Erratum in: Cancer Res. 2007 Dec 15;67(24):12034.

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