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Our Science – Pommier Website

Yves Pommier, M.D., Ph.D.

Selected Publications
1)  Zhao XZ, Semenova EA, Vu BC, Maddali K, Marchand C, Hughes SH, Pommier Y, Burke TR.
2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors.
J. Med. Chem. 51: 251-9, 2008. [Journal]
2)  McLean L, Soto U, Agama K, Francis J, Jimenez R, Pommier Y, Sowers L, Brantley E.
Aminoflavone induces oxidative DNA damage and reactive oxidative species-mediated apoptosis in breast cancer cells.
Int. J. Cancer. 122: 1665-74, 2008. [Journal]
3)  Shimura T, Torres MJ, Martin MM, Rao VA, Pommier Y, Katsura M, Miyagawa K, Aladjem MI.
Bloom's syndrome helicase and Mus81 are required to induce transient double-strand DNA breaks in response to DNA replication stress.
J. Mol. Biol. 375: 1152-64, 2008. [Journal]
4)  Kohn KW, Aladjem MI, Weinstein JN, Pommier Y.
Chromatin Challenges during DNA Replication: A Systems Representation.
Mol. Biol. Cell. 19: 1-7, 2008. [Journal]
5)  Marinello J, Marchand C, Mott BT, Bain A, Thomas CJ, Pommier Y.
Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants.
Biochemistry. 47: 9345-54, 2008. [Journal]
6)  Meng LH, Meng Z, Miao ZH, Veenstra TD, Pommier Y.
Cytokeratin-RNA cross-linking mediated by the antitumor aminoflavone, 5-amino-2,3-fluorophenyl-6,8-difluoro-7-methyl-4H-1-benzopyran-4-one.
J. Pharmacol. Exp. Ther. 325: 674-80, 2008. [Journal]
7)  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.
J. Med. Chem. 2008. [Journal]
8)  Semenova EA, Marchand C, Pommier Y.
HIV-1 integrase inhibitors: update and perspectives.
Adv. Pharmacol. 56: 199-228, 2008. [Journal]
9)  Evans JW, Chernikova SB, Kachnic LA, Banath JP, Sordet O, Delahoussaye YM, Treszezamsky A, Chon BH, Feng Z, Gu Y, Wilson WR, Pommier Y, Olive PL, Powell SN, Brown JM.
Homologous recombination is the principal pathway for the repair of DNA damage induced by tirapazamine in mammalian cells.
Cancer Res. 68: 257-65, 2008. [Journal]
10)  Sordet O, Larochelle S, Nicolas E, Stevens EV, Zhang C, Shokat KM, Fisher RP, Pommier Y.
Hyperphosphorylation of RNA polymerase II in response to topoisomerase I cleavage complexes and its association with transcription- and BRCA1-dependent degradation of topoisomerase I.
J. Mol. Biol. 381: 540-9, 2008. [Journal]
11)  Marchand C, Beutler JA, Wamiru A, Budihas S, Möllmann U, Heinisch L, Mellors JW, Le Grice SF, Pommier Y.
Madurahydroxylactone derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and RNase H.
Antimicrob. Agents Chemother. 52: 361-4, 2008. [Journal]
12)  Diaz-González R, Pérez-Pertejo Y, Pommier Y, Balaña-Fouce R, Reguera RM.
Mutational study of the.
Biochem. Pharmacol. 2008. [Journal]
13)  Di Santo R, Costi R, Roux A, Miele G, Crucitti GC, Iacovo A, Rosi F, Lavecchia A, Marinelli L, Di Giovanni C, Novellino E, Palmisano L, Andreotti M, Amici R, Galluzzo CM, Nencioni L, Palamara AT, Pommier Y, Marchand C.
Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities.
J. Med. Chem. 2008. [Journal]
14)  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 Res. 68: 6190-8, 2008. [Journal]
15)  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. [Journal]
16)  Liao Z, Robey RW, Guirouilh-Barbat J, To KK, Polgar O, Bates SE, Pommier Y.
Reduced expression of DNA topoisomerase I in SF295 human glioblastoma cells selected for resistance to homocamptothecin and diflomotecan.
Mol. Pharmacol. 73: 490-7, 2008. [Journal]
17)  Laco GS, Pommier Y.
Role of a tryptophan anchor in human topoisomerase I structure, function and inhibition.
Biochem. J. 411: 523-30, 2008. [Journal]
18)  Kitagaki J, Agama KK, Pommier Y, Yang Y, Weissman AM.
Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2.
Mol. Cancer Ther. 7: 2445-54, 2008. [Journal]
19)  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 Res. 36: 4128-36, 2008. [Journal]
20)  Sordet O, Goldman A, Redon C, Solier S, Rao AV, Pommier Y.
Topoisomerase I requirement for death receptor-induced apoptotic nuclear fission.
J. Biol. Chem. 2008. [Journal]
21)  Guirouilh-Barbat J, Redon C, Pommier Y.
Transcription-coupled DNA Double-Strand Breaks Are Mediated via the Nucleotide Excision Repair and the Mre11-Rad50-Nbs1 Complex.
Mol. Biol. Cell. 2008. [Journal]
22)  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, 2008. [Journal]
23)  Chi G, Nair V, Semenova E, Pommier Y.
A novel diketo phosphonic acid that exhibits specific, strand-transfer inhibition of HIV integrase and anti-HIV activity.
Bioorg. Med. Chem. Lett. 17: 1266-9, 2007. [Journal]
24)  Rao VA, Agama K, Holbeck S, Pommier Y.
Batracylin (NSC 320846), a dual inhibitor of DNA topoisomerases I and II induces histone gamma-H2AX as a biomarker of DNA damage.
Cancer Res. 67: 9971-9, 2007. [Journal]
25)  Wang Y, Miao ZH, Pommier Y, Kawasaki ES, Player A.
Characterization of mismatch and high-signal intensity probes associated with Affymetrix genechips.
Bioinformatics. 23: 2088-95, 2007. [Journal]
26)  Reinhold WC, Reimers MA, Maunakea AK, Kim S, Lababidi S, Scherf U, Shankavaram UT, Ziegler MS, Stewart C, Kouros-Mehr H, Cui H, Dolginow D, Scudiero DA, Pommier YG, Munroe DJ, Feinberg AP, Weinstein JN.
Detailed DNA methylation profiles of the E-cadherin promoter in the NCI-60 cancer cells.
Mol. Cancer Ther. 6: 391-403, 2007. [Journal]
27)  Zhou M, Meng Z, Jobson AG, Pommier Y, Veenstra TD.
Detection of in vitro kinase generated protein phosphorylation sites using gamma[18O4]-ATP and mass spectrometry.
Anal. Chem. 79: 7603-10, 2007. [Journal]
28)  Meng LH, Kohn KW, Pommier Y.
Dose-response transition from cell cycle arrest to apoptosis with selective degradation of Mdm2 and p21WAF1/CIP1 in response to the novel anticancer agent, aminoflavone (NSC 686,288).
Oncogene. 26: 4806-16, 2007. [Journal]
29)  Rao VA, Conti C, Guirouilh-Barbat J, Nakamura A, Miao ZH, Davies SL, Saccá B, Hickson ID, Bensimon A, Pommier Y.
Endogenous gamma-H2AX-ATM-Chk2 checkpoint activation in Bloom's syndrome helicase deficient cells is related to DNA replication arrested forks.
Mol. Cancer Res. 5: 713-24, 2007. [Journal]
30)  Pommier Y.
Finding the interface: more than an image.
Cancer Biol. Ther. 6: 620-3, 2007. [Journal]
31)  Jobson AG, Cardellina Ii JH, Scudiero D, Kondapaka S, Zhang H, Kim H, Shoemaker R, Pommier YG.
Identification of a bis-guanylhydrazone (NSC 109555) as a novel chemotype for inhibition of Chk2 kinase.
Mol Pharmacol. 2007. [Journal]
32)  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]
33)  Zhang H, Meng LH, Pommier Y.
Mitochondrial topoisomerases and alternative splicing of the human TOP1mt gene.
Biochimie. 89: 474-81, 2007. [Journal]
34)  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: 4419-4430, 2007. [Journal]
35)  Miao ZH, Player A, Shankavaram U, Wang YH, Zimonjic DB, Lorenzi PL, Liao ZY, Liu H, Shimura T, Zhang HL, Meng LH, Zhang YW, Kawasaki ES, Popescu NC, Aladjem MI, Goldstein DJ, Weinstein JN, Pommier Y.
Nonclassic functions of human topoisomerase I: genome-wide and pharmacologic analyses.
Cancer Res. 67: 8752-61, 2007. [Journal]
36)  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.
Mol. Cancer Ther. 6: 3229-38, 2007. [Journal]
37)  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]
38)  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]
39)  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: 4388-4404, 2007. [Journal]
40)  Johnson AA, Marchand C, Patil SS, Costi R, Di Santo R, Burke TR, Pommier Y.
Probing HIV-1 integrase inhibitor binding sites with position-specific integrase-DNA cross-linking assays.
Mol. Pharmacol. 71: 893-901, 2007. [Journal]
41)  Conti C, Saccà B, Herrick J, Lalou C, Pommier Y, Bensimon A.
Replication fork velocities at adjacent replication origins are coordinately modified during DNA replication in human cells.
Mol. Biol. Cell. 18: 3059-67, 2007. [Journal]
42)  Díaz González R, Pérez Pertejo Y, Redondo CM, Pommier Y, Balaña-Fouce R, Reguera RM.
Structural insights on the small subunit of DNA topoisomerase I from the unicellular parasite Leishmania donovani.
Biochimie. 89: 1517-27, 2007. [Journal]
43)  Shults EE, Semenova EA, Johnson AA, Bondarenko SP, Bagryanskaya IY, Gatilov YV, Tolstikov GA, Pommier Y.
Synthesis and HIV-1 integrase inhibitory activity of spiroundecane(ene) derivatives.
Bioorg. Med. Chem. Lett. 17: 1362-8, 2007. [Journal]
44)  Seiler JA, Conti C, Syed A, Aladjem MI, Pommier Y.
The intra-S-phase checkpoint affects both DNA replication initiation and elongation: single-cell and -DNA fiber analyses.
Mol. Cell. Biol. 27: 5806-18, 2007. [Journal]
45)  Conti C, Seiler JA, Pommier Y.
The mammalian DNA replication elongation checkpoint: implication of Chk1 and relationship with origin firing as determined by single DNA molecule and single cell analyses.
Cell Cycle. 6: 2760-7, 2007. [Journal]
46)  Liao C, Karki RG, Marchand C, Pommier Y, Nicklaus MC.
Virtual screening application of a model of full-length HIV-1 integrase complexed with viral DNA.
Bioorg Med Chem Lett. 2007. [Journal]
47)  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]
48)  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]
49)  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]
50)  Meng LH, Shankavaram U, Chen C, Agama K, Fu HQ, Gonzalez FJ, Weinstein J, Pommier Y.
Activation of Aminoflavone (NSC 686288) by a Sulfotransferase Is Required for the Antiproliferative Effect of the Drug and for Induction of Histone {gamma}-H2AX.
Cancer Res. 66: 9656-64, 2006. [Journal]
51)  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]
52)  Zhao XZ, Semenova EA, Liao C, Nicklaus M, Pommier Y, Burke TR.
Biotinylated biphenyl ketone-containing 2,4-dioxobutanoic acids designed as HIV-1 integrase photoaffinity ligands.
Bioorg Med Chem. 2006. [Journal]
53)  Antony S, Agama KK, Miao Z, Hollingshead M, Holbeck SL, Wright MH, Varticovski L, Nagarajan M, Morrell A, Cushman M, Pommier YG.
Bisindenoisoquinoline NSC 727357, a DNA intercalator and topoisomerase inhibitor with antitumor activity.
Mol Pharmacol. 70: 1109-20, 2006. Full Text Article. [Journal]
54)  Adams DJ, da Silva MW, Flowers JL, Kohlhagen G, Pommier Y, Colvin OM, Manikumar G, Wani MC.
Camptothecin analogs with enhanced activity against human breast cancer cells. I. Correlation of potency with lipophilicity and persistence in the cleavage complex.
Cancer Chemother. Pharmacol. 57: 135-44, 2006. [Journal]
55)  Pommier Y, Weinstein JN, Aladjem MI, Kohn KW.
Chk2 molecular interaction map and rationale for Chk2 inhibitors.
Clin. Cancer Res. 12: 2657-61, 2006. [Journal]
56)  Weinstein JN, Pommier Y.
Connecting genes, drugs and diseases.
Nat. Biotechnol. 24: 1365-6, 2006. [Journal]
57)  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. 2006. [Journal]
58)  Takemura H, Rao VA, Sordet O, Furuta T, Miao ZH, Meng L, Zhang H, Pommier Y.
Defective MRE11-dependent activation of CHK2 by ATM in colorectal carcinoma cells in response toreplication-dependent DNA double-strand breaks.
J Biol Chem. 2006. [Journal]
59)  Kohn KW, Aladjem MI, Kim S, Weinstein JN, Pommier Y.
Depicting combinatorial complexity with the molecular interaction map notation.
Mol. Syst. Biol. 2: 51, 2006. [Journal]
60)  Bona R, Andreotti M, Buffa V, Leone P, Galluzzo CM, Amici R, Palmisano L, Mancini MG, Michelini Z, Di Santo R, Costi R, Roux A, Pommier Y, Marchand C, Vella S, Cara A.
Development of a human immunodeficiency virus vector-based, single-cycle assay for evaluation of anti-integrase compounds.
Antimicrob. Agents Chemother. 50: 3407-17, 2006. [Journal]
61)  Johnson AA, Sayer JM, Yagi H, Patil SS, Debart F, Maier MA, Corey DR, Vasseur JJ, Burke TR, Marquez VE, Jerina DM, Pommier Y.
Effect of DNA modifications on DNA processing by HIV-1 integrase and inhibitor binding: role of DNA backbone flexibility and an open catalytic site.
J Biol Chem. 2006. [Journal]
62)  Kim Y, Sun Y, Chow C, Pommier YG, Simons SS.
Effects of acetylation, polymerase phosphorylation, and DNA unwinding in glucocorticoid receptor transactivation.
. 2006. [Journal]
63)  Yoshida A, Pommier Y, Ueda T.
Endonuclease activation and chromosomal DNA fragmentation during apoptosis in leukemia cells.
Int. J. Hematol. 84: 31-7, 2006. [Journal]
64)  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.
. 2006. [Journal]
65)  Miao ZH, Agama K, Sordet O, Povirk L, Kohn KW, Pommier Y.
Hereditary ataxia SCAN1 cells are defective for the repair of transcription-dependent topoisomerase I cleavage complexes.
DNA Repair (Amst). 2006. [Journal]
66)  Liao Z, Thibaut L, Jobson A, Pommier Y.
Inhibition of Human Tyrosyl-DNA Phosphodiesterase by Aminoglycoside Antibiotics and Ribosome Inhibitors.
Mol. Pharmacol. 70: 366-72, 2006. [Journal]
67)  Johnson AA, Santos W, Pais GC, Marchand C, Amin R, Burke TR, Verdine G, Pommier Y.
Integration requires a specific interaction of the donor DNA terminal 5'-cytosine with glutamine 148 of the HIV-1 integrase flexible loop.
J. Biol. Chem. 281: 461-7, 2006. [Journal]
68)  Deng J, Kelley JA, Barchi JJ, Sanchez T, Dayam R, Pommier Y, Neamati N.
Mining the NCI antiviral compounds for HIV-1 integrase inhibitors.
Bioorg. Med. Chem. 14: 3785-92, 2006. [Journal]
69)  Kohn KW, Aladjem MI, Weinstein JN, Pommier Y.
Molecular interaction maps of bioregulatory networks: a general rubric for systems biology.
Mol. Biol. Cell. 17: 1-13, 2006. [Journal]
70)  Di Santo R, Costi R, Roux A, Artico M, Lavecchia A, Marinelli L, Novellino E, Palmisano L, Andreotti M, Amici R, Galluzzo CM, Nencioni L, Palamara AT, Pommier Y, Marchand C.
Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action.
J. Med. Chem. 49: 1939-45, 2006. [Journal]
71)  Furuta T, Hayward RL, Meng LH, Takemura H, Aune GJ, Bonner WM, Aladjem MI, Kohn KW, Pommier Y.
p21CDKN1A allows the repair of replication-mediated DNA double-strand breaks induced by topoisomerase I and is inactivated by the checkpoint kinase inhibitor 7-hydroxystaurosporine.
Oncogene. 25: 2839-49, 2006. [Journal]
72)  Semenova EA, Johnson AA, Marchand C, Davis DA, Yarchoan R, Pommier Y.
Preferential inhibition of the magnesium-dependent strand transfer reaction of HIV-1 integrase by alpha-hydroxytropolones.
Mol. Pharmacol. 69: 1454-60, 2006. [Journal]
73)  Stagliano KW, Emadi A, Lu Z, Malinakova HC, Twenter B, Yu M, Holland LE, Rom AM, Harwood JS, Amin R, Johnson AA, Pommier Y.
Regiocontrolled synthesis and HIV inhibitory activity of unsymmetrical binaphthoquinone and trimeric naphthoquinone derivatives of conocurvone.
. 2006. [Journal]
74)  Pommier Y, Barcelo JM, Rao VA, Sordet O, Jobson AG, Thibaut L, Miao ZH, Seiler JA, Zhang H, Marchand C, Agama K, Nitiss JL, Redon C.
Repair of topoisomerase I-mediated DNA damage.
Prog. Nucleic Acid Res. Mol. Biol. 81: 179-229, 2006. [Journal]
75)  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.
. 2006. [Journal]
76)  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. [Journal]
77)  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]
78)  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]
79)  Pommier Y.
Topoisomerase I inhibitors: camptothecins and beyond.
Nat. Rev. Cancer. 6: 789-802, 2006. [Journal]
80)  Sordet O, Goldman A, Pommier Y.
Topoisomerase II and tubulin inhibitors both induce the formation of apoptotic topoisomerase I cleavage complexes.
Mol. Cancer Ther. 5: 3139-44, 2006. [Journal]
81)  Xiao X, Antony S, Pommier Y, Cushman M.
Total synthesis and biological evaluation of 22-hydroxyacuminatine.
J. Med. Chem. 49: 1408-12, 2006. [Journal]
82)  Chen C, Meng LH, Ma X, Krausz KW, Pommier Y, Idle JR, Gonzalez FJ.
Urinary Metabolite Profiling Reveals CYP1A2-mediated Metabolism of Aminoflavone (NSC 686288).
. 2006. [Journal]
83)  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. [Journal]
84)  Arimondo PB, Laco GS, Thomas CJ, Halby L, Pez D, Schmitt P, Boutorine A, Garestier T, Pommier Y, Hecht SM, Sun JS, Bailly C.
Activation of camptothecin derivatives by conjugation to triple helix-forming oligonucleotides.
Biochemistry. 44: 4171-80, 2005. [Journal]
85)  Brantley E, Antony S, Kohlhagen S, Meng L, Agama K, Stinson S, Sausville EA, Pommier Y.
Antitumor drug candidate 2-(4-amino-3-methylphenyl0-5-fluorobenzothiazole induces single-strand breaks and DNA-protein crosslinks in sensitive MCF-7 breast cancer cells.
Cancer Chemotherapy Pharmacol. In press, 2005. [Journal]
86)  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. [Journal]
87)  Di Santo R, Costi R, Artico M, Ragno R, Greco G, Novellino E, Marchand C, Pommier Y.
Design, synthesis and biological evaluation of heteroaryl diketohexenoic and diketobutanoic acids as HIV-1 integrase inhibitors endowed with antiretroviral activity.
Farmaco. 60: 409-17, 2005. [Journal]
88)  Xiao X, Miao ZH, Antony S, Pommier Y, Cushman M.
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
Bioorg Med Chem Lett. 15: 2795-8, 2005. [Journal]
89)  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]
90)  .
Effect of dimerization and tetramerization on the potency of HIV-1 integrase inhibitory peptides.
Biopolymers. 80: 557, 2005. [Journal]
91)  Pommier Y, Johnson AA, Marchand C.
Integrase inhibitors to treat HIV/AIDS.
Nat Rev Drug Discov. 4: 236-48, 2005. [Journal]
92)  Pommier Y, Cherfils J.
Interfacial inhibition of macromolecular interactions: nature's paradigm for drug discovery.
Trends Pharmacol Sci. 26: 138-45, 2005. [Journal]
93)  Pommier Y, Marchand C.
Interfacial inhibitors of protein-nucleic acid interactions.
Curr Med Chem Anti-Canc Agents. 5: 421-9, 2005. [Journal]
94)  Kohn KW, Pommier Y.
Molecular interaction map of the p53 and Mdm2 logic elements, which control the Off-On switch of p53 in response to DNA damage.
Biochem Biophys Res Commun. 331: 816-27, 2005. [Journal]
95)  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. [Journal]
96)  Rao VA, Fan AM, Meng L, Doe CF, North PS, Hickson ID, Pommier Y.
Phosphorylation of BLM, dissociation from topoisomerase IIIalpha and colocalization with gamma-H2AX after topoisomerase I-induced replication damage.
Mol. Cell. Biol. in press, 2005. [Journal]
97)  Rehman A, Chahal MS, Tang X, Bruce JE, Pommier Y, Daoud SS.
Proteomic identification of heat shock protein 90 as a candidate target for p53 mutation reactivation by PRIMA-1 in breast cancer cells.
Breast Cancer Res. 7: R765-74, 2005. [Journal]
98)  Staker BL, Feese MD, Cushman M, Pommier Y, Zembower D, Stewart L, Burgin AB.
Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.
J Med Chem. 48: 2336-45, 2005. [Journal]
99)  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. [Journal]
100)  Pommier Y, Sordet O, Rao VA, Zhang H, Kohn KW.
Targeting chk2 kinase: molecular interaction maps and therapeutic rationale.
Curr Pharm Des. 11: 2855-72, 2005. [Journal]
101)  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. [Journal]
102)  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]
103)  Candeil L, Gourdier I, Peyron D, Vezzio N, Copois V, Bibeau F, Orsetti B, Scheffer GL, Ychou M, Khan QA, Pommier Y, Pau B, Martineau P, Del Rio M.
ABCG2 overexpression in colon cancer cells resistant to SN38 and in irinotecan-treated metastases.
Int J Cancer. 109: 848-54, 2004. [Journal]
104)  Shao RG, Cao CX, Pommier Y.
Abrogation of Chk1-mediated S/G2 checkpoint by UCN-01 enhances ara-C-induced cytotoxicity in human colon cancer cells.
Acta Pharmacol Sin. 25: 756-62, 2004. [Journal]
105)  Annereau JP, Szakács G, Tucker CJ, Arciello A, Cardarelli C, Collins J, Grissom S, Zeeberg BR, Reinhold W, Weinstein JN, Pommier Y, Paules RS, Gottesman MM.
Analysis of ABC transporter expression in drug-selected cell lines by a microarray dedicated to multidrug resistance.
Mol Pharmacol. 2004. [Journal]
106)  Laco GS, Du W, Kohlhagen G, Sayer JM, Jerina DM, Burke TG, Curran DP, Pommier Y.
Analysis of human topoisomerase I inhibition and interaction with the cleavage site +1 deoxyguanosine, via in vitro experiments and molecular modeling studies.
Bioorg Med Chem. 12: 5225-35, 2004. [Journal]
107)  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. [Journal]
108)  Sordet O, Khan QA, Pommier Y.
Apoptotic Topoisomerase I-DNA Complexes Induced by Oxygen Radicals and Mitochondrial Dysfunction.
Cell Cycle. 3, 2004. [Journal]
109)  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. 2004. [Journal]
110)  Svarovskaia ES, Barr R, Zhang X, Pais GC, Marchand C, Pommier Y, Burke TR, Pathak VK.
Azido-containing diketo acid derivatives inhibit human immunodeficiency virus type 1 integrase in vivo and influence the frequency of deletions at two-long-terminal-repeat-circle junctions.
J Virol. 78: 3210-22, 2004. [Journal]
111)  Svarovskaia ES, Barr R, Zhang X, Pais GC, Marchand C, Pommier Y, Burke TR, Pathak VK.
Azido-containing diketo acid derivatives inhibit human immunodeficiency virus type 1 integrase in vivo and influence the frequency of deletions at two-long-terminal-repeat-circle junctions.
J Virol. 78: 3210-22, 2004. [Journal]
112)  Pommier Y.
Camptothecins and topoisomerase I: a foot in the door. Targeting the genome beyond topoisomerase I with camptothecins and novel anticancer drugs: importance of DNA replication, repair and cell cycle checkpoints.
Curr Med Chem Anti-Canc Agents. 4: 429-34, 2004. [Journal]
113)  Farrell N, Povirk LF, Dange Y, DeMasters G, Gupta MS, Kohlhagen G, Khan QA, Pommier Y, Gewirtz DA.
Cytotoxicity, DNA strand breakage and DNA-protein crosslinking by a novel transplatinum compound in human A2780 ovarian and MCF-7 breast carcinoma cells.
Biochem Pharmacol. 68: 857-66, 2004. [Journal]
114)  Zhang X, Marchand C, Pommier Y, Burke TR.
Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes.
Bioorg Med Chem Lett. 14: 1205-7, 2004. [Journal]
115)  Zhang X, Marchand C, Pommier Y, Burke TR.
Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes.
Bioorg Med Chem Lett. 14: 1205-7, 2004. [Journal]
116)  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. [Journal]
117)  Johnson AA, Marchand C, Pommier Y.
HIV-1 integrase inhibitors: a decade of research and two drugs in clinical trial.
Curr Top Med Chem. 4: 1059-77, 2004. [Journal]
118)  Mertins SD, Myers TG, Holbeck SL, Medina-Perez W, Wang E, Kohlhagen G, Pommier Y, Bates SE.
In vitro evaluation of dimethane sulfonate analogues with potential alkylating activity and selective renal cell carcinoma cytotoxicity.
Mol Cancer Ther. 3: 849-60, 2004. [Journal]
119)  Chrencik JE, Staker BL, Burgin AB, Pourquier P, Pommier Y, Stewart L, Redinbo MR.
Mechanisms of camptothecin resistance by human topoisomerase I mutations.
J Mol Biol. 339: 773-84, 2004. [Journal]
120)  Aladjem MI, Pasa S, Parodi S, Weinstein JN, Pommier Y, Kohn KW.
Molecular interaction maps--a diagrammatic graphical language for bioregulatory networks.
Sci STKE. 2004: pe8, 2004. [Journal]
121)  Yu D, Khan E, Khaleque MA, Lee J, Laco G, Kohlhagen G, Kharbanda S, Cheng YC, Pommier Y, Bharti A.
Phosphorylation of DNA topoisomerase l by the c-Abl tyrosine kinase confers camptothecin sensitivity.
J Biol Chem. 2004. [Journal]
122)  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. [Journal]
123)  Johnson AA, Sayer JM, Yagi H, Kalena GP, Amin R, Jerina DM, Pommier Y.
Position-specific suppression and enhancement of HIV-1 integrase reactions by minor groove benzo[a]pyrene diol epoxide deoxyguanine adducts: implications for molecular interactions between integrase and substrates.
J Biol Chem. 279: 7947-55, 2004. [Journal]
124)  Kohn KW, Riss J, Aprelikova O, Weinstein JN, Pommier Y, Barrett JC.
Properties of switch-like bioregulatory networks studied by simulation of the hypoxia response control system.
Mol Biol Cell. 15: 3042-52, 2004. [Journal]
125)  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. [Journal]
126)  Meng LH, Zhang H, Hayward L, Takemura H, Shao RG, Pommier Y.
Tetrandrine induces early G1 arrest in human colon carcinoma cells by down-regulating the activity and inducing the degradation of G1-S-specific cyclin-dependent kinases and by inducing p53 and p21Cip1.
Cancer Res. 64: 9086-92, 2004. [Journal]
127)  Zhang H, Meng LH, Zimonjic DB, Popescu NC, Pommier Y.
Thirteen-exon-motif signature for vertebrate nuclear and mitochondrial type IB topoisomerases.
Nucleic Acids Res. 32: 2087-92, 2004. [Journal]
128)  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. [Journal]
129)  Rapisarda A, Uranchimeg B, Sordet O, Pommier Y, Shoemaker RH, Melillo G.
Topoisomerase I-mediated inhibition of hypoxia-inducible factor 1: mechanism and therapeutic implications.
Cancer Res. 64: 1475-82, 2004. [Journal]
130)  Pommier Y, Kohn KW.
[Cell cycle and checkpoints in oncology: new therapeutic targets].
Med Sci (Paris). 19: 173-86, 2003. [Journal]
131)  Sordet O, Khan QA, Kohn KW, Pommier Y.
Apoptosis induced by topoisomerase inhibitors.
Curr Med Chem Anti-Canc Agents. 3: 271-90, 2003. [Journal]
132)  Reinhold WC, Kouros-Mehr H, Kohn KW, Maunakea AK, Lababidi S, Roschke A, Stover K, Alexander J, Pantazis P, Miller L, Liu E, Kirsch IR, Urasaki Y, Pommier Y, Weinstein JN.
Apoptotic susceptibility of cancer cells selected for camptothecin resistance: gene expression profiling, functional analysis, and molecular interaction mapping.
Cancer Res. 63: 1000-11, 2003. [Journal]
133)  Zhang X, Pais GC, Svarovskaia ES, Marchand C, Johnson AA, Karki RG, Nicklaus MC, Pathak VK, Pommier Y, Burke TR.
Azido-Containing aryl beta-Diketo acid HIV-1 integrase inhibitors.
Bioorg Med Chem Lett. 13: 1215-9, 2003. [Journal]
134)  Fan Z, Beresford PJ, Zhang D, Xu Z, Novina CD, Yoshida A, Pommier Y, Lieberman J.
Cleaving the oxidative repair protein Ape1 enhances cell death mediated by granzyme A.
Nat Immunol. 4: 145-53, 2003. [Journal]
135)  Krajewski K, Long YQ, Marchand C, Pommier Y, Roller PP.
Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.
Bioorg Med Chem Lett. 13: 3203-3205, 2003. [Journal]
136)  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. [Journal]
137)  Yoshida A, Urasaki Y, Waltham M, Bergman AC, Pourquier P, Rothwell DG, Inuzuka M, Weinstein JN, Ueda T, Appella E, Hickson ID, Pommier Y.
Human AP endonuclease (Ape1) and its N-terminal truncated form (AN34) are involved in DNA fragmentation during apoptosis.
J Biol Chem. 2003. [Journal]
138)  Yoshida A, Urasaki Y, Waltham M, Bergman AC, Pourquier P, Rothwell DG, Inuzuka M, Weinstein JN, Ueda T, Appella E, Hickson ID, Pommier Y.
Human apurinic/apyrimidinic endonuclease (Ape1) and its N-terminal truncated form (AN34) are involved in DNA fragmentation during apoptosis.
J Biol Chem. 278: 37768-76, 2003. [Journal]
139)  Daoud SS, Munson PJ, Reinhold W, Young L, Prabhu VV, Yu Q, LaRose J, Kohn KW, Weinstein JN, Pommier Y.
Impact of p53 knockout and topotecan treatment on gene expression profiles in human colon carcinoma cells: a pharmacogenomic study.
Cancer Res. 63: 2782-93, 2003. [Journal]
140)  Marchand C, Johnson AA, Karki RG, Pais GC, Zhang X, Cowansage K, Patel TA, Nicklaus MC, Burke TR, Pommier Y.
Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble double-mutant (F185K/C280S).
Mol Pharmacol. 64: 600-9, 2003. [Journal]
141)  Meng LH, Liao ZY, Pommier Y.
Non-camptothecin DNA topoisomerase I inhibitors in cancer therapy.
Curr Top Med Chem. 3: 305-20, 2003. [Journal]
142)  Furuta T, Takemura H, Liao ZY, Aune GJ, Redon C, Sedelnikova OA, Pilch DR, Rogakou EP, Celeste A, Chen HT, Nussenzweig A, Aladjem MI, Bonner WM, Pommier Y.
Phosphorylation of histone H2AX and activation of Mre11, Rad50, and Nbs1 in response to replication-dependent DNA double-strand breaks induced by mammalian DNA topoisomerase I cleavage complexes.
J Biol Chem. 278: 20303-12, 2003. [Journal]
143)  Khan QA, Kohlhagen G, Marshall R, Austin CA, Kalena GP, Kroth H, Sayer JM, Jerina DM, Pommier Y.
Position-specific trapping of topoisomerase II by benzo[a]pyrene diol epoxide adducts: implications for interactions with intercalating anticancer agents.
Proc Natl Acad Sci U S A. 100: 12498-503, 2003. [Journal]
144)  Chrencik JE, Burgin AB, Pommier Y, Stewart L, Redinbo MR.
Structural impact of the leukemia drug 1-beta-D-arabinofuranosylcytosine (Ara-C) on the covalent human topoisomerase I-DNA complex.
J Biol Chem. 278: 12461-6, 2003. [Journal]
145)  Wall NR, O'Connor DS, Plescia J, Pommier Y, Altieri DC.
Suppression of survivin phosphorylation on Thr34 by flavopiridol enhances tumor cell apoptosis.
Cancer Res. 63: 230-5, 2003. [Journal]
146)  Lesher DT, Pommier Y, Stewart L, Redinbo MR.
8-Oxoguanine rearranges the active site of human topoisomerase I.
Proc Natl Acad Sci U S A. 99: 12102-7, 2002. [Journal]
147)  Xu L, Yang L, Hashimoto K, Anderson M, Kohlhagen G, Pommier Y, D'Arpa P.
Characterization of BTBD1 and BTBD2, two similar BTB-domain-containing Kelch-like proteins that interact with Topoisomerase I.
BMC Genomics. 3: 1, 2002. [Journal]
148)  Pommier Y, Kohlhagen G, Laco GS, Kroth H, Sayer JM, Jerina DM.
Different effects on human topoisomerase I by minor groove and intercalated deoxyguanosine adducts derived from two polycyclic aromatic hydrocarbon diol epoxides at or near a normal cleavage site.
J Biol Chem. 277: 13666-72, 2002. [Journal]
149)  Gourdier I, Del Rio M, Crabbé L, Candeil L, Copois V, Ychou M, Auffray C, Martineau P, Mechti N, Pommier Y, Pau B.
Drug specific resistance to oxaliplatin is associated with apoptosis defect in a cellular model of colon carcinoma.
FEBS Lett. 529: 232-6, 2002. [Journal]
150)  Aune GJ, Furuta T, Pommier Y.
Ecteinascidin 743: a novel anticancer drug with a unique mechanism of action.
Anticancer Drugs. 13: 545-55, 2002. [Journal]
151)  Melek M, Jones JM, O'Dea MH, Pais G, Burke TR, Pommier Y, Neamati N, Gellert M.
Effect of HIV integrase inhibitors on the RAG1/2 recombinase.
Proc Natl Acad Sci U S A. 99: 134-7, 2002. [Journal]
152)  Pourquier P, Gioffre C, Kohlhagen G, Urasaki Y, Goldwasser F, Hertel LW, Yu S, Pon RT, Gmeiner WH, Pommier Y.
Gemcitabine (2',2'-difluoro-2'-deoxycytidine), an antimetabolite that poisons topoisomerase I.
Clin Cancer Res. 8: 2499-504, 2002. [Journal]
153)  Laco GS, Collins JR, Luke BT, Kroth H, Sayer JM, Jerina DM, Pommier Y.
Human topoisomerase I inhibition: docking camptothecin and derivatives into a structure-based active site model.
Biochemistry. 41: 1428-35, 2002. [Journal]
154)  Strumberg D, Nitiss JL, Dong J, Walker J, Nicklaus MC, Kohn KW, Heddle JG, Maxwell A, Seeber S, Pommier Y.
Importance of the fourth alpha-helix within the CAP homology domain of type II topoisomerase for DNA cleavage site recognition and quinolone action.
Antimicrob Agents Chemother. 46: 2735-46, 2002. [Journal]
155)  van Hattum AH, Hoogsteen IJ, Schlüper HM, Maliepaard M, Scheffer GL, Scheper RJ, Kohlhagen G, Pommier Y, Pinedo HM, Boven E.
Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity.
Br J Cancer. 87: 665-72, 2002. [Journal]
156)  Marchand C, Pourquier P, Laco GS, Jing N, Pommier Y.
Interaction of human nuclear topoisomerase I with guanosine quartet-forming and guanosine-rich single-stranded DNA and RNA oligonucleotides.
J Biol Chem. 277: 8906-11, 2002. [Journal]
157)  Neamati N, Lin Z, Karki RG, Orr A, Cowansage K, Strumberg D, Pais GC, Voigt JH, Nicklaus MC, Winslow HE, Zhao H, Turpin JA, Yi J, Skalka AM, Burke TR, Pommier Y.
Metal-dependent inhibition of HIV-1 integrase.
J Med Chem. 45: 5661-70, 2002. [Journal]
158)  Kanzaki A, Takebayashi Y, Ren XQ, Miyashita H, Mori S, Akiyama S, Pommier Y.
Overcoming multidrug drug resistance in P-glycoprotein/MDR1-overexpressing cell lines by ecteinascidin 743.
Mol Cancer Ther. 1: 1327-34, 2002. [Journal]
159)  Plo I, Hernandez H, Kohlhagen G, Lautier D, Pommier Y, Laurent G.
Overexpression of the atypical protein kinase C zeta reduces topoisomerase II catalytic activity, cleavable complexes formation, and drug-induced cytotoxicity in monocytic U937 leukemia cells.
J Biol Chem. 277: 31407-15, 2002. [Journal]
160)  Debéthune L, Kohlhagen G, Grandas A, Pommier Y.
Processing of nucleopeptides mimicking the topoisomerase I-DNA covalent complex by tyrosyl-DNA phosphodiesterase.
Nucleic Acids Res. 30: 1198-204, 2002. [Journal]
161)  Marchand C, Zhang X, Pais GC, Cowansage K, Neamati N, Burke TR, Pommier Y.
Structural determinants for HIV-1 integrase inhibition by beta-diketo acids.
J Biol Chem. 277: 12596-603, 2002. [Journal]
162)  Pais GC, Zhang X, Marchand C, Neamati N, Cowansage K, Svarovskaia ES, Pathak VK, Tang Y, Nicklaus M, Pommier Y, Burke TR.
Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors.
J Med Chem. 45: 3184-94, 2002. [Journal]
163)  Jayaraman M, Fox BM, Hollingshead M, Kohlhagen G, Pommier Y, Cushman M.
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
J Med Chem. 45: 242-9, 2002. [Journal]
164)  Xu G, Kannan A, Hartman TL, Wargo H, Watson K, Turpin JA, Buckheit RW, Johnson AA, Pommier Y, Cushman M.
Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents.
Bioorg Med Chem. 10: 2807-16, 2002. [Journal]
165)  Furuta T, Ueda T, Aune G, Sarasin A, Kraemer KH, Pommier Y.
Transcription-coupled nucleotide excision repair as a determinant of cisplatin sensitivity of human cells.
Cancer Res. 62: 4899-902, 2002. [Journal]
166)  Zhou Y, Gwadry FG, Reinhold WC, Miller LD, Smith LH, Scherf U, Liu ET, Kohn KW, Pommier Y, Weinstein JN.
Transcriptional regulation of mitotic genes by camptothecin-induced DNA damage: microarray analysis of dose- and time-dependent effects.
Cancer Res. 62: 1688-95, 2002. [Journal]
167)  Yu Q, La Rose J, Zhang H, Takemura H, Kohn KW, Pommier Y.
UCN-01 inhibits p53 up-regulation and abrogates gamma-radiation-induced G(2)-M checkpoint independently of p53 by targeting both of the checkpoint kinases, Chk2 and Chk1.
Cancer Res. 62: 5743-8, 2002. [Journal]
168)  Shao RG, Cao CX, Nieves-Neira W, Dimanche-Boitrel MT, Solary E, Pommier Y.
Activation of the Fas pathway independently of Fas ligand during apoptosis induced by camptothecin in p53 mutant human colon carcinoma cells.
Oncogene. 20: 1852-9, 2001. [Journal]
169)  Kreuzer KN, Freudenreich CH, Pommier Y.
Analysis of cleavage complexes using reactive inhibitor derivatives.
Methods Mol Biol. 95: 89-99, 2001. [Journal]
170)  Takebayashi Y, Pourquier P, Zimonjic DB, Nakayama K, Emmert S, Ueda T, Urasaki Y, Kanzaki A, Akiyama SI, Popescu N, Kraemer KH, Pommier Y.
Antiproliferative activity of ecteinascidin 743 is dependent upon transcription-coupled nucleotide-excision repair.
Nat Med. 7: 961-6, 2001. [Journal]
171)  Yu Q, Rose JH, Zhang H, Pommier Y.
Antisense inhibition of Chk2/hCds1 expression attenuates DNA damage-induced S and G2 checkpoints and enhances apoptotic activity in HEK-293 cells.
FEBS Lett. 505: 7-12, 2001. [Journal]
172)  Zhang X, Neamati N, Lee YK, Orr A, Brown RD, Whitaker N, Pommier Y, Burke TR.
Arylisothiocyanate-containing esters of caffeic acid designed as affinity ligands for HIV-1 integrase.
Bioorg Med Chem. 9: 1649-57, 2001. [Journal]
173)  Urasaki Y, Laco GS, Pourquier P, Takebayashi Y, Kohlhagen G, Gioffre C, Zhang H, Chatterjee D, Pantazis P, Pommier Y.
Characterization of a novel topoisomerase I mutation from a camptothecin-resistant human prostate cancer cell line.
Cancer Res. 61: 1964-9, 2001. [Journal]
174)  Taktakishvili M, Neamati N, Pommier Y, Nair V.
Discovery of a nuclease-resistant, non-natural dinucleotide that inhibits HIV-1 integrase.
Bioorg Med Chem Lett. 11: 1433-5, 2001. [Journal]
175)  Gamcsik MP, Kasibhatla MS, Adams DJ, Flowers JL, Colvin OM, Manikumar G, Wani M, Wall ME, Kohlhagen G, Pommier Y.
Dual role of glutathione in modulating camptothecin activity: depletion potentiates activity, but conjugation enhances the stability of the topoisomerase I-DNA cleavage complex.
Mol Cancer Ther. 1: 11-20, 2001. [Journal]
176)  Takebayashi Y, Goldwasser F, Urasaki Y, Kohlhagen G, Pommier Y.
Ecteinascidin 743 induces protein-linked DNA breaks in human colon carcinoma HCT116 cells and is cytotoxic independently of topoisomerase I expression.
Clin Cancer Res. 7: 185-91, 2001. [Journal]
177)  Lovett BD, Strumberg D, Blair IA, Pang S, Burden DA, Megonigal MD, Rappaport EF, Rebbeck TR, Osheroff N, Pommier YG, Felix CA.
Etoposide metabolites enhance DNA topoisomerase II cleavage near leukemia-associated MLL translocation breakpoints.
Biochemistry. 40: 1159-70, 2001. [Journal]
178)  Zhang H, Barceló JM, Lee B, Kohlhagen G, Zimonjic DB, Popescu NC, Pommier Y.
Human mitochondrial topoisomerase I.
Proc Natl Acad Sci U S A. 98: 10608-13, 2001. [Journal]
179)  Marchand C, Neamati N, Pommier Y.
In vitro human immunodeficiency virus type 1 integrase assays.
Methods Enzymol. 340: 624-33, 2001. [Journal]
180)  Takebayashi Y, Nakayama K, Kanzaki A, Miyashita H, Ogura O, Mori S, Mutoh M, Miyazaki K, Fukumoto M, Pommier Y.
Loss of heterozygosity of nucleotide excision repair factors in sporadic ovarian, colon and lung carcinomas: implication for their roles of carcinogenesis in human solid tumors.
Cancer Lett. 174: 115-25, 2001. [Journal]
181)  Fan Y, Shi LM, Kohn KW, Pommier Y, Weinstein JN.
Quantitative structure-antitumor activity relationships of camptothecin analogues: cluster analysis and genetic algorithm-based studies.
J Med Chem. 44: 3254-63, 2001. [Journal]
182)  Jing N, Marchand C, Guan Y, Liu J, Pallansch L, Lackman-Smith C, De Clercq E, Pommier Y.
Structure-activity of inhibition of HIV-1 integrase and virus replication by G-quartet oligonucleotides.
DNA Cell Biol. 20: 499-508, 2001. [Journal]
183)  Pourquier P, Waltman JL, Urasaki Y, Loktionova NA, Pegg AE, Nitiss JL, Pommier Y.
Topoisomerase I-mediated cytotoxicity of N-methyl-N'-nitro-N-nitrosoguanidine: trapping of topoisomerase I by the O6-methylguanine.
Cancer Res. 61: 53-8, 2001. [Journal]
184)  Pourquier P, Pommier Y.
Topoisomerase I-mediated DNA damage.
Adv Cancer Res. 80: 189-216, 2001. [Journal]
185)  Urasaki Y, Laco G, Takebayashi Y, Bailly C, Kohlhagen G, Pommier Y.
Use of camptothecin-resistant mammalian cell lines to evaluate the role of topoisomerase I in the antiproliferative activity of the indolocarbazole, NB-506, and its topoisomerase I binding site.
Cancer Res. 61: 504-8, 2001. [Journal]
186)  Scherf U, Ross DT, Waltham M, Smith LH, Lee JK, Tanabe L, Kohn KW, Reinhold WC, Myers TG, Andrews DT, Scudiero DA, Eisen MB, Sausville EA, Pommier Y, Botstein D, Brown PO, Weinstein JN.
A gene expression database for the molecular pharmacology of cancer.
Nat Genet. 24: 236-44, 2000. [Journal]
187)  Urasaki Y, Takebayashi Y, Pommier Y.
Activity of a novel camptothecin analogue, homocamptothecin, in camptothecin-resistant cell lines with topoisomerase I alterations.
Cancer Res. 60: 6577-80, 2000. [Journal]
188)  Pommier Y, Kohlhagen G, Pourquier P, Sayer JM, Kroth H, Jerina DM.
Benzo[a]pyrene diol epoxide adducts in DNA are potent suppressors of a normal topoisomerase I cleavage site and powerful inducers of other topoisomerase I cleavages.
Proc Natl Acad Sci U S A. 97: 2040-5, 2000. [Journal]
189)  Strumberg D, Pilon AA, Smith M, Hickey R, Malkas L, Pommier Y.
Conversion of topoisomerase I cleavage complexes on the leading strand of ribosomal DNA into 5'-phosphorylated DNA double-strand breaks by replication runoff.
Mol Cell Biol. 20: 3977-87, 2000. [Journal]
190)  Neamati N, Marchand C, Pommier Y.
HIV-1 integrase inhibitors: past, present, and future.
Adv Pharmacol. 49: 147-65, 2000. [Journal]
191)  Kohn KW, Shao RG, Pommier Y.
How do drug-induced topoisomerase I-DNA lesions signal to the molecular interaction network that regulates cell cycle checkpoints, DNA replication, and DNA repair?.
Cell Biochem Biophys. 33: 175-80, 2000. [Journal]
192)  Voeller DM, Grem JL, Pommier Y, Paull K, Allegra CJ.
Identification and proposed mechanism of action of thymidine kinase inhibition associated with cellular exposure to camptothecin analogs.
Cancer Chemother Pharmacol. 45: 409-16, 2000. [Journal]
193)  Chen IJ, Neamati N, Nicklaus MC, Orr A, Anderson L, Barchi JJ, Kelley JA, Pommier Y, MacKerell AD.
Identification of HIV-1 integrase inhibitors via three-dimensional database searching using ASV and HIV-1 integrases as targets.
Bioorg Med Chem. 8: 2385-98, 2000. [Journal]
194)  Pourquier P, Takebayashi Y, Urasaki Y, Gioffre C, Kohlhagen G, Pommier Y.
Induction of topoisomerase I cleavage complexes by 1-beta -D-arabinofuranosylcytosine (ara-C) in vitro and in ara-C-treated cells.
Proc Natl Acad Sci U S A. 97: 1885-90, 2000. [Journal]
195)  Rogakou EP, Nieves-Neira W, Boon C, Pommier Y, Bonner WM.
Initiation of DNA fragmentation during apoptosis induces phosphorylation of H2AX histone at serine 139.
J Biol Chem. 275: 9390-5, 2000. [Journal]
196)  Jing N, Marchand C, Liu J, Mitra R, Hogan ME, Pommier Y.
Mechanism of inhibition of HIV-1 integrase by G-tetrad-forming oligonucleotides in Vitro.
J Biol Chem. 275: 21460-7, 2000. [Journal]
197)  Kohn KW, Pommier Y.
Molecular and biological determinants of the cytotoxic actions of camptothecins. Perspective for the development of new topoisomerase I inhibitors.
Ann N Y Acad Sci. 922: 11-26, 2000. [Journal]
198)  Pilon AA, Marchand C, Kavlick MF, Bajaj K, Owen J, Mitsuya H, Pommier Y.
Mutations in the HIV type 1 integrase of patients receiving long-term dideoxynucleoside therapy do not confer resistance to zidovudine.
AIDS Res Hum Retroviruses. 16: 1417-22, 2000. [Journal]
199)  Pommier Y, Laco GS, Kohlhagen G, Sayer JM, Kroth H, Jerina DM.
Position-specific trapping of topoisomerase I-DNA cleavage complexes by intercalated benzo[a]- pyrene diol epoxide adducts at the 6-amino group of adenine.
Proc Natl Acad Sci U S A. 97: 10739-44, 2000. [Journal]
200)  Taktakishvili M, Neamati N, Pommier Y, Nair V.
Recognition and inhibition of HIV integrase by a novel dinucleotide.
Bioorg Med Chem Lett. 10: 249-51, 2000. [Journal]
201)  Pommier Y, Marchand C, Neamati N.
Retroviral integrase inhibitors year 2000: update and perspectives.
Antiviral Res. 47: 139-48, 2000. [Journal]
202)  Gharehbaghi K, Szekeres T, Yalowitz JA, Fritzer-Szekeres M, Pommier YG, Jayaram HN.
Sensitizing human colon carcinoma HT-29 cells to cisplatin by cyclopentenylcytosine, in vitro and in vivo.
Life Sci. 68: 1-11, 2000. [Journal]
203)  Fertala J, Vance JR, Pourquier P, Pommier Y, Bjornsti MA.
Substitutions of Asn-726 in the active site of yeast DNA topoisomerase I define novel mechanisms of stabilizing the covalent enzyme-DNA intermediate.
J Biol Chem. 275: 15246-53, 2000. [Journal]
204)  Cushman M, Jayaraman M, Vroman JA, Fukunaga AK, Fox BM, Kohlhagen G, Strumberg D, Pommier Y.
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
J Med Chem. 43: 3688-98, 2000. [Journal]
205)  Bom D, Curran DP, Kruszewski S, Zimmer SG, Thompson Strode J, Kohlhagen G, Du W, Chavan AJ, Fraley KA, Bingcang AL, Latus LJ, Pommier Y, Burke TG.
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
J Med Chem. 43: 3970-80, 2000. [Journal]
206)  Pluymers W, Neamati N, Pannecouque C, Fikkert V, Marchand C, Burke TR, Pommier Y, Schols D, De Clercq E, Debyser Z, Witvrouw M.
Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters.
Mol Pharmacol. 58: 641-8, 2000. [Journal]
207)  LeGrice S, Scott B, Marchand C, Pommier Y, inventor; DHHS, assignee.
Compounds and methods of treating retroviral infections such as AIDS.
Patent Pending, Filed in 2004. Application No. 60/515,987. Pending [Patent]
208)  Burke T, Zhang X, Pais G, Svarovskaia E, Pathak V, Marchand C, Pommier Y, inventor; DHHS, assignee.
Compounds to treat HIV infections and AIDS.
Patent Pending, Filed in 2002. Application No. 10/497,898. E-Number: E-039-2004/0-US-01. Pending [Patent]
209)  Pommier Y, Marchand C, inventor; DHHS, assignee.
Diamidines inhibitors of human tyrosyl-DNA phosphodiesterase (Tdp1) for the treatment of cancers.
Patent Pending, Filed in 2006. Application No. 60/786-604. E-Number: E-165-2006/0-US-01. Pending [Patent]
210)  Pommier Y, Semenova E, Marchand C, inventor; DHHS, assignee.
Discovery of tropolone inhibitors of HIV-1 integrase that can be used for treament of retroviral infection, including AIDS.
Patent Pending, Filed in 2005. Application No. 60/741,769. E-Number: E-308-2005/0-US-01. Pending [Patent]
211)  Pommier Y, Artico M, Di Santo R, Marchand C, inventor; DHHS, assignee.
Novel Inhibitors Of Hiv-1 Integrase.
Patent Pending, Filed in 2003. Application No. 10/591,679. E-Number: E-187-2003/0-US-03. Pending [Patent]
212)  Roller P, Marchand C, Krajewski K, Pathak V, Zhang Y, Pommier Y, inventor; DHHS, assignee.
Peptide inhibitors of HIV-1 integrase useful for the treatment of retroviral and HIV infections.
Patent Pending, Filed in 2004. Application No. 60/534,378. E-Number: E-039-2004/0-US-01. Pending [Patent]
213)  Pommier Y, inventor; DHHS, assignee.
Ribosome inhibitors as inhibitors of tyrosyl-DNA-phosphodiesterase.
Patent Pending, Filed in 2005. Application No. 60/661,306. Pending [Patent]
214)  Pommier Y, Marchand C, Semenova E, inventor; DHHS, assignee.
Stilbenedisulfonic acid derivatives as inhibitors of retroviral integrase.
Patent Pending, Filed in 2006. Application No. 60/849,718. E-Number: E-264-2006/0-PCT-02. Pending [Patent]
215)  Cushman M, Morrell A, Pommier Y, inventor; DHHS, assignee.
Synthesis Of Indenoisoquinolines.
Patent Pending, Filed in 2006. Application No. 11/125,723. E-Number: E-112-2006/1-US-01. Pending [Patent]
216)  Pommier Y, inventor; DHHS, assignee.
Synthesis of indenoisoquinolines.
Patent Pending, Filed in 2006. Application No. US-2006-0025595-A1. Pending [Patent]
217)  Cushman M, Ioanoviciu A, Pommier Y, inventor; DHHS, assignee.
Synthesis of indenoisoquinoliniums and methods of use.
Patent Pending, Filed in 2004. Application No. 60/553,837. Pending [Patent]
218)  Pommier Y, Thibaut L, Marchand C, inventor; DHHS, assignee.
Tetracycline inhibitors of human tyrosy-DNA phosphodiesterase (tdp1) for the treatment of cancers.
Patent Pending, Filed in 2006. Application No. 60/786,746. E-Number: E-097-2006/0-ZUS-01. Pending [Patent]
219)  Pommier Y, inventor; DHHS, assignee.
Use of Chk2 kinase inhibitors for cancer treatment.
Patent Pending, Filed in 2005. E-Number: E-211-2005/0-US-01. Pending [Patent]
220)  Pommier Y, Colvin M, Gamcsik M, inventor; DHHS, assignee.
Camptothecin Compounds With A Sulfhydryl Group.
US Patent: 6,825,206. 2004. [Patent]
221)  Cushman M, Pommier Y, inventor; DHHS, assignee.
Cytotoxic Indeno- And Isoindenoisoquinoline Compounds.
US Patent: 7,312,228. 2007. [Patent]
222)  Cushman M, Nagafumi P, Jayaraman M, Pommier Y, inventor; DHHS, assignee.
Indenoisoquinolines as antineoplastic agents.
US Patent: 6,509,344. 2003. [Patent]
223)  Cushman M, Jayaraman M, Nagafuji P, Pommier Y, inventor; DHHS, assignee.
Novel Indenoisoquinoline As Antineoplastic Agents.
US Patent: 6,509,344. 2003. [Patent]
224)  Pommier Y, Marchand C, Simeonov A, Dexheimer T, Lea W, Inglese J, Austin C, Jadhav A, inventor; DHHS, assignee.
Protein tyrosine phosphatase inhibitors of human tyrosyl-DNA phosphodiesterase (Tdp1) and methods of treating disorders.
US Patent: 61/042706. 2008. [Patent]
225)  Pommier Y, Neamati N, Garofalo A, Nacci V, inventor; DHHS, assignee.
Thiazepine inhibitors of HIV-1 integrase.
US Patent: 7,015,212. 2006. [Patent]

This page was last updated on 12/1/2008.