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Our Science – Antony Website

Smitha Antony, Ph.D.

Selected Publications

1)  Wu Y, Antony S, Juhasz A, Lu J, Ge Y, Jiang G, Roy K, Doroshow JH.
Up-regulation and Sustained Activation of Stat1 Are Essential for Interferon-{gamma} (IFN-{gamma})-induced Dual Oxidase 2 (Duox2) and Dual Oxidase A2 (DuoxA2) Expression in Human Pancreatic Cancer Cell Lines.
J. Biol. Chem. 286: 12245-56, 2011.
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2)  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.
Bioorg. Med. Chem. 18: 182-9, 2010.
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3)  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.
J. Med. Chem. 52: 7122-31, 2009.
[Journal]
4)  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.
EMBO J. 28: 3667-80, 2009.
[Journal]
5)  Guirouilh-Barbat J, Antony S, Pommier Y.
Zalypsis (PM00104) is a potent inducer of gamma-H2AX foci and reveals the importance of the C ring of trabectedin for transcription-coupled repair inhibition.
Mol. Cancer Ther. 8: 2007-14, 2009.
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6)  Stevens EV, Nishizuka S, Antony S, Reimers M, Varma S, Young L, Munson PJ, Weinstein JN, Kohn EC, Pommier Y.
Predicting cisplatin and trabectedin drug sensitivity in ovarian and colon cancers.
Mol. Cancer Ther. 7: 10-8, 2008.
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7)  Dexheimer TS, Antony S, Marchand C, Pommier Y.
Tyrosyl-DNA phosphodiesterase as a target for anticancer therapy.
Anticancer Agents Med Chem. 8: 381-9, 2008.
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8)  Aune GJ, Takagi K, Sordet O, Guirouilh-Barbat J, Antony S, Bohr VA, Pommier Y.
Von Hippel-Lindau-coupled and transcription-coupled nucleotide excision repair-dependent degradation of RNA polymerase II in response to trabectedin.
Clin. Cancer Res. 14: 6449-55, 2008.
[Journal]
9)  Morrell A, Placzek MS, Steffen JD, Antony S, Agama K, Pommier Y, Cushman M.
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
J. Med. Chem. 50: 2040-8, 2007.
[Journal]
10)  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.
J. Med. Chem. 50: 4419-30, 2007.
[Journal]
11)  Antony S, Marchand C, Stephen AG, Thibaut L, Agama KK, Fisher RJ, Pommier Y.
Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1.
Nucleic Acids Res. 35: 4474-84, 2007.
[Journal]
12)  Antony S, Agama KK, Miao ZH, Takagi K, Wright MH, Robles AI, Varticovski L, Nagarajan M, Morrell A, Cushman M, Pommier Y.
Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistance.
Cancer Res. 67: 10397-405, 2007.
[Journal]
13)  Morrell A, Placzek M, Parmley S, Grella B, Antony S, Pommier Y, Cushman M.
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
J. Med. Chem. 50: 4388-404, 2007.
[Journal]
14)  Miao ZH, Rao VA, Agama K, Antony S, Kohn KW, Pommier Y.
4-nitroquinoline-1-oxide induces the formation of cellular topoisomerase I-DNA cleavage complexes.
Cancer Res. 66: 6540-5, 2006.
[Journal]
15)  Marchand C, Antony S, Kohn KW, Cushman M, Ioanoviciu A, Staker BL, Burgin AB, Stewart L, Pommier Y.
A novel norindenoisoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex.
Mol. Cancer Ther. 5: 287-95, 2006.
[Journal]
16)  Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M.
A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor.
J. Med. Chem. 49: 7740-53, 2006.
[Journal]
17)  Brantley E, Antony S, Kohlhagen G, Meng L, Agama K, Stinson SF, Sausville EA, Pommier Y.
Anti-tumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces single-strand breaks and DNA-protein cross-links in sensitive MCF-7 breast cancer cells.
Cancer Chemother. Pharmacol. 58: 62-72, 2006.
[Journal]
18)  Antony S, Agama KK, Miao ZH, Hollingshead M, Holbeck SL, Wright MH, Varticovski L, Nagarajan M, Morrell A, Cushman M, Pommier Y.
Bisindenoisoquinoline bis-1,3-{(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity.
Mol. Pharmacol. 70: 1109-20, 2006.
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19)  Marchand C, Krajewski K, Lee HF, Antony S, Johnson AA, Amin R, Roller P, Kvaratskhelia M, Pommier Y.
Covalent binding of the natural antimicrobial peptide indolicidin to DNA abasic sites.
Nucleic Acids Res. 34: 5157-65, 2006.
[Journal]
20)  Morrell A, Jayaraman M, Nagarajan M, Fox BM, Meckley MR, Ioanoviciu A, Pommier Y, Antony S, Hollingshead M, Cushman M.
Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
Bioorg. Med. Chem. Lett. 16: 4395-9, 2006.
[Journal]
21)  Tangirala RS, Antony S, Agama K, Pommier Y, Anderson BD, Bevins R, Curran DP.
Synthesis and biological assays of E-ring analogs of camptothecin and homocamptothecin.
Bioorg. Med. Chem. 14: 6202-12, 2006.
[Journal]
22)  Nagarajan M, Morrell A, Antony S, Kohlhagen G, Agama K, Pommier Y, Ragazzon PA, Garbett NC, Chaires JB, Hollingshead M, Cushman M.
Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors.
J. Med. Chem. 49: 5129-40, 2006.
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23)  Nagarajan M, Morrell A, Ioanoviciu A, Antony S, Kohlhagen G, Agama K, Hollingshead M, Pommier Y, Cushman M.
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
J. Med. Chem. 49: 6283-9, 2006.
[Journal]
24)  Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M.
Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors.
Bioorg. Med. Chem. Lett. 16: 1846-9, 2006.
[Journal]
25)  Xiao X, Antony S, Pommier Y, Cushman M.
Total synthesis and biological evaluation of 22-hydroxyacuminatine.
J. Med. Chem. 49: 1408-12, 2006.
[Journal]
26)  Liao ZY, Sordet O, Zhang HL, Kohlhagen G, Antony S, Gmeiner WH, Pommier Y.
A novel polypyrimidine antitumor agent FdUMP[10] induces thymineless death with topoisomerase I-DNA complexes.
Cancer Res. 65: 4844-51, 2005.
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27)  Antony S, Kohlhagen G, Agama K, Jayaraman M, Cao S, Durrani FA, Rustum YM, Cushman M, Pommier Y.
Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison.
Mol. Pharmacol. 67: 523-30, 2005.
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28)  Xiao X, Miao ZH, Antony S, Pommier Y, Cushman M.
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
Bioorg. Med. Chem. Lett. 15: 2795-8, 2005.
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29)  Meng LH, Kohlhagen G, Liao ZY, Antony S, Sausville E, Pommier Y.
DNA-protein cross-links and replication-dependent histone H2AX phosphorylation induced by aminoflavone (NSC 686288), a novel anticancer agent active against human breast cancer cells.
Cancer Res. 65: 5337-43, 2005.
[Journal]
30)  Xiao X, Antony S, Pommier Y, Cushman M.
On the binding of indeno[1,2-c]isoquinolines in the DNA-topoisomerase I cleavage complex.
J. Med. Chem. 48: 3231-8, 2005.
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31)  Ioanoviciu A, Antony S, Pommier Y, Staker BL, Stewart L, Cushman M.
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
J. Med. Chem. 48: 4803-14, 2005.
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32)  Tangirala RS, Dixon R, Yang D, Ambrus A, Antony S, Agama K, Pommier Y, Curran DP.
Total and semisynthesis and in vitro studies of both enantiomers of 20-fluorocamptothecin.
Bioorg. Med. Chem. Lett. 15: 4736-40, 2005.
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33)  Bates SE, Medina-Pérez WY, Kohlhagen G, Antony S, Nadjem T, Robey RW, Pommier Y.
ABCG2 mediates differential resistance to SN-38 (7-ethyl-10-hydroxycamptothecin) and homocamptothecins.
J. Pharmacol. Exp. Ther. 310: 836-42, 2004.
[Journal]
34)  Pommier Y, Sordet O, Antony S, Hayward RL, Kohn KW.
Apoptosis defects and chemotherapy resistance: molecular interaction maps and networks.
Oncogene. 23: 2934-49, 2004.
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35)  Sordet O, Khan QA, Plo I, Pourquier P, Urasaki Y, Yoshida A, Antony S, Kohlhagen G, Solary E, Saparbaev M, Laval J, Pommier Y.
Apoptotic topoisomerase I-DNA complexes induced by staurosporine-mediated oxygen radicals.
J. Biol. Chem. 279: 50499-504, 2004.
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36)  Xiao X, Antony S, Kohlhagen G, Pommier Y, Cushman M.
Design, synthesis, and biological evaluation of cytotoxic 11-aminoalkenylindenoisoquinoline and 11-diaminoalkenylindenoisoquinoline topoisomerase I inhibitors.
Bioorg. Med. Chem. 12: 5147-60, 2004.
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37)  Antony S, Theruvathu JA, Brooks PJ, Lesher DT, Redinbo M, Pommier Y.
Enhancement of camptothecin-induced topoisomerase I cleavage complexes by the acetaldehyde adduct N2-ethyl-2'-deoxyguanosine.
Nucleic Acids Res. 32: 5685-92, 2004.
[Journal]
38)  Xiao X, Antony S, Kohlhagen G, Pommier Y, Cushman M.
Novel autoxidative cleavage reaction of 9-fluoredenes discovered during synthesis of a potential DNA-threading indenoisoquinoline.
J. Org. Chem. 69: 7495-501, 2004.
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39)  Antony S, Arimondo PB, Sun JS, Pommier Y.
Position- and orientation-specific enhancement of topoisomerase I cleavage complexes by triplex DNA structures.
Nucleic Acids Res. 32: 5163-73, 2004.
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40)  Nagarajan M, Morrell A, Fort BC, Meckley MR, Antony S, Kohlhagen G, Pommier Y, Cushman M.
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
J. Med. Chem. 47: 5651-61, 2004.
[Journal]
41)  Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M.
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
Bioorg. Med. Chem. Lett. 14: 3659-63, 2004.
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42)  Sordet O, Liao Z, Liu H, Antony S, Stevens EV, Kohlhagen G, Fu H, Pommier Y.
Topoisomerase I-DNA complexes contribute to arsenic trioxide-induced apoptosis.
J. Biol. Chem. 279: 33968-75, 2004.
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43)  Fox BM, Xiao X, Antony S, Kohlhagen G, Pommier Y, Staker BL, Stewart L, Cushman M.
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
J. Med. Chem. 46: 3275-82, 2003.
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44)  Nagarajan M, Xiao X, Antony S, Kohlhagen G, Pommier Y, Cushman M.
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
J. Med. Chem. 46: 5712-24, 2003.
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45)  Antony S, Jayaraman M, Laco G, Kohlhagen G, Kohn KW, Cushman M, Pommier Y.
Differential induction of topoisomerase I-DNA cleavage complexes by the indenoisoquinoline MJ-III-65 (NSC 706744) and camptothecin: base sequence analysis and activity against camptothecin-resistant topoisomerases I.
Cancer Res. 63: 7428-35, 2003.
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46)  Pommier Y, Redon C, Rao VA, Seiler JA, Sordet O, Takemura H, Antony S, Meng L, Liao Z, Kohlhagen G, Zhang H, Kohn KW.
Repair of and checkpoint response to topoisomerase I-mediated DNA damage.
Mutat. Res. 532: 173-203, 2003.
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This page was last updated on 5/18/2011.