Yves Pommier

Yves Pommier

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Yves Pommier

Publications by authors named "Yves Pommier"

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Excision repair of topoisomerase DNA-protein crosslinks (TOP-DPC).

DNA Repair (Amst) 2020 Mar 7;89:102837. Epub 2020 Mar 7.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, United States. Electronic address:

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http://dx.doi.org/10.1016/j.dnarep.2020.102837DOI Listing
March 2020

Chromatin Remodeling and Immediate Early Gene Activation by SLFN11 in Response to Replication Stress.

Cell Rep 2020 Mar;30(12):4137-4151.e6

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2020.02.117DOI Listing
March 2020

Novel deazaflavin tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors.

DNA Repair (Amst) 2020 01 6;85:102747. Epub 2019 Nov 6.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, United States. Electronic address:

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http://dx.doi.org/10.1016/j.dnarep.2019.102747DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6952553PMC
January 2020

The antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitor.

J Enzyme Inhib Med Chem 2019 Dec;34(1):818-822

a School of Pharmaceutical Sciences , Sun Yat-sen University , Guangzhou , China.

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http://dx.doi.org/10.1080/14756366.2018.1516651DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6442119PMC
December 2019

Targeting Topoisomerase I in the Era of Precision Medicine.

Clin Cancer Res 2019 Nov 21;25(22):6581-6589. Epub 2019 Jun 21.

Developmental Therapeutics Branch, Center for Cancer Research, NCI, NIH, Bethesda, Maryland.

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http://dx.doi.org/10.1158/1078-0432.CCR-19-1089DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6858945PMC
November 2019

Beyond the unwinding: role of TOP1MT in mitochondrial translation.

Cell Cycle 2019 Oct 9;18(19):2377-2384. Epub 2019 Aug 9.

Laboratory of Molecular Pharmacology, Developmental Therapeutics Branch, Center for Cancer Research, National Cancer Institute, NIH , Bethesda , MD , USA.

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http://dx.doi.org/10.1080/15384101.2019.1646563DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6739053PMC
October 2019

Discovery of Novel Integrase Inhibitors Acting outside the Active Site Through High-Throughput Screening.

Molecules 2019 Oct 12;24(20). Epub 2019 Oct 12.

Laboratoire MFP, CNRS UMR5234, Université de Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux CEDEX, France.

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http://dx.doi.org/10.3390/molecules24203675DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6832134PMC
October 2019

Schlafen 11 (SLFN11), a restriction factor for replicative stress induced by DNA-targeting anti-cancer therapies.

Pharmacol Ther 2019 09 23;201:94-102. Epub 2019 May 23.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, Bethesda, MD, USA. Electronic address:

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http://dx.doi.org/10.1016/j.pharmthera.2019.05.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6708787PMC
September 2019

Synthesis and biological evaluation of 5-aminoethyl benzophenanthridone derivatives as DNA topoisomerase IB inhibitors.

Eur J Med Chem 2019 Sep 30;178:81-92. Epub 2019 May 30.

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China; Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, Guangzhou, 510006, China. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2019.05.074DOI Listing
September 2019

Dual Processing of R-Loops and Topoisomerase I Induces Transcription-Dependent DNA Double-Strand Breaks.

Cell Rep 2019 Sep;28(12):3167-3181.e6

Cancer Research Center of Toulouse, INSERM, Université de Toulouse, Université Toulouse III Paul Sabatier, CNRS, 31037 Toulouse, France. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2019.08.041DOI Listing
September 2019

RNA Sequencing of the NCI-60: Integration into CellMiner and CellMiner CDB.

Cancer Res 2019 07 21;79(13):3514-3524. Epub 2019 May 21.

Developmental Therapeutic Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland.

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http://dx.doi.org/10.1158/0008-5472.CAN-18-2047DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6615556PMC
July 2019

Mammalian Tyrosyl-DNA Phosphodiesterases in the Context of Mitochondrial DNA Repair.

Int J Mol Sci 2019 Jun 20;20(12). Epub 2019 Jun 20.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.

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http://dx.doi.org/10.3390/ijms20123015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6628236PMC
June 2019

Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide.

J Med Chem 2019 May 30;62(9):4669-4682. Epub 2019 Apr 30.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research , National Cancer Institute, National Institutes of Health , Bethesda , Maryland 20892 , United States.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00274
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http://dx.doi.org/10.1021/acs.jmedchem.9b00274DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6624171PMC
May 2019

Phosphatase 1 Nuclear Targeting Subunit, a Novel DNA Repair Partner of PARP1.

Cancer Res 2019 05;79(10):2460-2461

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, Maryland.

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http://cancerres.aacrjournals.org/lookup/doi/10.1158/0008-54
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http://dx.doi.org/10.1158/0008-5472.CAN-19-0798DOI Listing
May 2019

Acquired SETD2 mutation and impaired CREB1 activation confer cisplatin resistance in metastatic non-small cell lung cancer.

Oncogene 2019 01 9;38(2):180-193. Epub 2018 Aug 9.

Lombardi Comprehensive Cancer Center, Georgetown University, Washington, DC, 20057, USA.

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http://dx.doi.org/10.1038/s41388-018-0429-3DOI Listing
January 2019

Characterization and structure-activity relationships of indenoisoquinoline-derived topoisomerase I inhibitors in unsilencing the dormant gene associated with Angelman syndrome.

Mol Autism 2018 17;9:45. Epub 2018 Aug 17.

1Department of Cell Biology and Physiology, University of North Carolina School of Medicine, Neuroscience Research Building, Room 5119 115 Mason Farm Rd., Campus Box 7545, Chapel Hill, NC 27599-7545 USA.

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http://dx.doi.org/10.1186/s13229-018-0228-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6098585PMC
December 2018

Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.

J Med Chem 2018 12 21;61(23):10440-10462. Epub 2018 Nov 21.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University , West Lafayette , Indiana 47907 , United States.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00510
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http://dx.doi.org/10.1021/acs.jmedchem.8b00510DOI Listing
December 2018

Novel screen for anti-cancer drugs that elevate chromosome instability (CIN) using human artificial chromosome (HAC).

Oncotarget 2018 Dec 7;9(96):36833-36835. Epub 2018 Dec 7.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.

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http://dx.doi.org/10.18632/oncotarget.26406DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6305142PMC
December 2018

Novel clinical indenoisoquinoline topoisomerase I inhibitors: a twist around the camptothecins.

Oncotarget 2018 Dec 18;9(99):37286-37288. Epub 2018 Dec 18.

Yves Pommier: Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, Division of Cancer Treatment and Diagnosis, National Cancer Institute, NIH, Bethesda, Maryland, USA.

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http://www.oncotarget.com/fulltext/26466
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http://dx.doi.org/10.18632/oncotarget.26466DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6324668PMC
December 2018

Probing the evolutionary conserved residues Y204, F259, S400 and W590 that shape the catalytic groove of human TDP1 for 3'- and 5'-phosphodiester-DNA bond cleavage.

DNA Repair (Amst) 2018 Jun - Jul;66-67:64-71. Epub 2018 May 2.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA. Electronic address:

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http://dx.doi.org/10.1016/j.dnarep.2018.05.001DOI Listing
October 2018

TDP1 suppresses mis-joining of radiomimetic DNA double-strand breaks and cooperates with Artemis to promote optimal nonhomologous end joining.

Nucleic Acids Res 2018 09;46(17):8926-8939

Department of Pharmacology and Toxicology and Massey Cancer Center, Virginia Commonwealth University, Richmond, VA 23298, USA.

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http://dx.doi.org/10.1093/nar/gky694DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6158748PMC
September 2018

Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors.

Mol Cancer Ther 2018 08 10;17(8):1694-1704. Epub 2018 May 10.

Developmental Therapeutics Branch & Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, Maryland.

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http://mct.aacrjournals.org/lookup/doi/10.1158/1535-7163.MCT
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http://dx.doi.org/10.1158/1535-7163.MCT-18-0028DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072611PMC
August 2018

Phase I Study of ATR Inhibitor M6620 in Combination With Topotecan in Patients With Advanced Solid Tumors.

J Clin Oncol 2018 06 18;36(16):1594-1602. Epub 2017 Dec 18.

Anish Thomas, Christophe E. Redon, Linda Sciuto, Emerson Padiernos, Min-Jung Lee, Akira Yuno, Sunmin Lee, Arun Rajan, Udayan Guha, Haobin Chen, Raffit Hassan, Christine C. Alewine, Eva Szabo, Seth M. Steinberg, James H. Doroshow, Mirit I. Aladjem, Jane B. Trepel, and Yves Pommier, National Cancer Institute, Bethesda; Jiuping Ji, Yiping Zhang, Lan Tran, William Yutzy, and Robert J. Kinders, Frederick National Laboratory for Cancer Research, Frederick, MD; and Susan E. Bates, Columbia University Medical Center, New York, NY.

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http://dx.doi.org/10.1200/JCO.2017.76.6915DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5978471PMC
June 2018

PRMT5-mediated arginine methylation of TDP1 for the repair of topoisomerase I covalent complexes.

Nucleic Acids Res 2018 06;46(11):5601-5617

Laboratory of Molecular Biology, Department of Biological Chemistry, Indian Association for the Cultivation of Science, 2A & B, Raja S.C. Mullick Road, Jadavpur, Kolkata 700032, India.

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http://dx.doi.org/10.1093/nar/gky291DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009676PMC
June 2018

Overcoming Resistance to DNA-Targeted Agents by Epigenetic Activation of Schlafen 11 ( Expression with Class I Histone Deacetylase Inhibitors.

Clin Cancer Res 2018 04 1;24(8):1944-1953. Epub 2018 Feb 1.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, Maryland.

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http://clincancerres.aacrjournals.org/lookup/doi/10.1158/107
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http://dx.doi.org/10.1158/1078-0432.CCR-17-0443DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5899656PMC
April 2018

SLFN11 Blocks Stressed Replication Forks Independently of ATR.

Mol Cell 2018 02;69(3):371-384.e6

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S10972765183004
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http://dx.doi.org/10.1016/j.molcel.2018.01.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5802881PMC
February 2018

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

Eur J Pharm Sci 2018 Jan 13;111:337-348. Epub 2017 Oct 13.

Department of Radiation Oncology, Stanford University, 3165 Porter Drive, Palo Alto, CA 94304, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ejps.2017.10.017DOI Listing
January 2018

Transcription profiling suggests that mitochondrial topoisomerase IB acts as a topological barrier and regulator of mitochondrial DNA transcription.

J Biol Chem 2017 12 11;292(49):20162-20172. Epub 2017 Oct 11.

From the Laboratory of Molecular Pharmacology, Developmental Therapeutics Branch, Center for Cancer Research, NCI, National Institutes of Health, Bethesda, Maryland 20892 and

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http://dx.doi.org/10.1074/jbc.M117.815241DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5724003PMC
December 2017

TDP1 is Critical for the Repair of DNA Breaks Induced by Sapacitabine, a Nucleoside also Targeting ATM- and BRCA-Deficient Tumors.

Mol Cancer Ther 2017 11 11;16(11):2543-2551. Epub 2017 Aug 11.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, NCI, NIH, Bethesda, Maryland.

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http://dx.doi.org/10.1158/1535-7163.MCT-17-0110DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5971110PMC
November 2017

Effects of camptothecin or TOP1 overexpression on genetic stability in Saccharomyces cerevisiae.

DNA Repair (Amst) 2017 11 18;59:69-75. Epub 2017 Sep 18.

Department of Molecular Genetics and Microbiology, Duke University Medical Center, Durham, NC 27710, United States. Electronic address:

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http://dx.doi.org/10.1016/j.dnarep.2017.09.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5691608PMC
November 2017

Structure-Guided Optimization of HIV Integrase Strand Transfer Inhibitors.

J Med Chem 2017 09 10;60(17):7315-7332. Epub 2017 Aug 10.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health , Bethesda, Maryland 20892, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.7b00596DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5601359PMC
September 2017

Distribution bias and biochemical characterization of TOP1MT single nucleotide variants.

Sci Rep 2017 08 17;7(1):8614. Epub 2017 Aug 17.

Laboratory of Molecular Pharmacology, Developmental Therapeutics Branch, Center for Cancer Research, NCI, National Institutes of Health, Bethesda, MD, 20892, USA.

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http://dx.doi.org/10.1038/s41598-017-09258-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5561071PMC
August 2017

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

J Med Chem 2017 07 28;60(13):5364-5376. Epub 2017 Jun 28.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01870DOI Listing
July 2017

Identification of Natural Products That Inhibit the Catalytic Function of Human Tyrosyl-DNA Phosphodiesterase (TDP1).

SLAS Discov 2017 Jul 1:2472555217717200. Epub 2017 Jul 1.

1 Molecular Targets Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, USA.

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http://dx.doi.org/10.1177/2472555217717200DOI Listing
July 2017

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

J Med Chem 2017 04 18;60(8):3275-3288. Epub 2017 Apr 18.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01565DOI Listing
April 2017

Topoisomerase I-mediated cleavage at unrepaired ribonucleotides generates DNA double-strand breaks.

EMBO J 2017 02 8;36(3):361-373. Epub 2016 Dec 8.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD, USA

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http://dx.doi.org/10.15252/embj.201592426DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5286372PMC
February 2017

Temozolomide in the Era of Precision Medicine.

Cancer Res 2017 02 3;77(4):823-826. Epub 2017 Feb 3.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, NCI, Bethesda, Maryland.

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http://dx.doi.org/10.1158/0008-5472.CAN-16-2983DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5313339PMC
February 2017

DNA-Targeted Precision Medicine; Have we Been Caught Sleeping?

Trends Cancer 2017 01;3(1):2-6

Developmental Therapeutics Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892.

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http://dx.doi.org/10.1016/j.trecan.2016.11.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5461960PMC
January 2017

Novel TDP2-ubiquitin interactions and their importance for the repair of topoisomerase II-mediated DNA damage.

Nucleic Acids Res 2016 12 19;44(21):10201-10215. Epub 2016 Aug 19.

Department of Biochemistry, Molecular Biology and Biophysics, University of Minnesota, Minneapolis, MN 55455, USA

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http://dx.doi.org/10.1093/nar/gkw719DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5137425PMC
December 2016

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

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

Department of Chemistry, Massachusetts Institute of Technology , Cambridge, Massachusetts 02139, United States.

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http://dx.doi.org/10.1021/acschembio.6b00565DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5248983PMC
November 2016

Resistance to PARP inhibitors by SLFN11 inactivation can be overcome by ATR inhibition.

Oncotarget 2016 Nov;7(47):76534-76550

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.

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http://dx.doi.org/10.18632/oncotarget.12266DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5340226PMC
November 2016

Roles of eukaryotic topoisomerases in transcription, replication and genomic stability.

Nat Rev Mol Cell Biol 2016 11 21;17(11):703-721. Epub 2016 Sep 21.

College of Pharmacy, University of Illinois, Rockford, Illinois 61107, USA.

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http://dx.doi.org/10.1038/nrm.2016.111DOI Listing
November 2016

F10 cytotoxicity via topoisomerase I cleavage complex repair consistent with a unique mechanism for thymineless death.

Future Oncol 2016 Oct 22;12(19):2183-8. Epub 2016 Jun 22.

University of North Carolina, Chapel Hill, NC 27599, USA.

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http://dx.doi.org/10.2217/fon-2016-0127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5551924PMC
October 2016

Laying a trap to kill cancer cells: PARP inhibitors and their mechanisms of action.

Sci Transl Med 2016 10;8(362):362ps17

Drug Development Unit, Institute of Cancer Research and Royal Marsden National Health Service Foundation Trust, London SM2 5PT, U.K.

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http://stm.sciencemag.org/content/scitransmed/8/362/362ps17.
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http://dx.doi.org/10.1126/scitranslmed.aaf9246DOI Listing
October 2016

Parallel analysis of ribonucleotide-dependent deletions produced by yeast Top1 in vitro and in vivo.

Nucleic Acids Res 2016 09 1;44(16):7714-21. Epub 2016 Jun 1.

Department of Molecular Genetics and Microbiology, Duke University Medical Center, Durham, NC 27710, USA

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http://dx.doi.org/10.1093/nar/gkw495DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5027487PMC
September 2016

Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site.

Nucleic Acids Res 2016 08 1;44(14):6896-906. Epub 2016 Jul 1.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, 37 Convent Drive, Bethesda, MD 20892, USA

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http://dx.doi.org/10.1093/nar/gkw592DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5001616PMC
August 2016

Deazaflavin Inhibitors of Tyrosyl-DNA Phosphodiesterase 2 (TDP2) Specific for the Human Enzyme and Active against Cellular TDP2.

ACS Chem Biol 2016 07 11;11(7):1925-33. Epub 2016 May 11.

Developmental Therapeutics Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health , Bethesda, Maryland 20892, United States.

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http://dx.doi.org/10.1021/acschembio.5b01047DOI Listing
July 2016

Chromatin Regulators as a Guide for Cancer Treatment Choice.

Mol Cancer Ther 2016 07 16;15(7):1768-77. Epub 2016 May 16.

Institut Curie, PSL Research University, CNRS, UMR3664, Equipe Labellisée Ligue contre le Cancer, Paris, France. Sorbonne Universités, UPMC Universite Paris 06, CNRS, UMR3664, Paris, France.

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http://dx.doi.org/10.1158/1535-7163.MCT-15-1008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4936925PMC
July 2016

RNA topoisomerase is prevalent in all domains of life and associates with polyribosomes in animals.

Nucleic Acids Res 2016 07 1;44(13):6335-49. Epub 2016 Jun 1.

Genome Instability and Chromatin Remodeling Section, Lab of Genetics, National Institute on Aging, National Institutes of Health, 251 Bayview Boulevard, Baltimore, MD 21224, USA

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http://dx.doi.org/10.1093/nar/gkw508DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4994864PMC
July 2016

Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft.

Bioorg Med Chem Lett 2016 07 24;26(14):3232-3236. Epub 2016 May 24.

Department of Chemistry, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30302, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.05.065DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4939481PMC
July 2016

Small cell lung cancer: Time to revisit DNA-damaging chemotherapy.

Sci Transl Med 2016 07;8(346):346fs12

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892, USA.

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http://dx.doi.org/10.1126/scitranslmed.aaf6282DOI Listing
July 2016

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

J Med Chem 2016 05 20;59(10):4890-9. Epub 2016 Apr 20.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States .

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http://dx.doi.org/10.1021/acs.jmedchem.6b00220DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5317102PMC
May 2016

rcellminer: exploring molecular profiles and drug response of the NCI-60 cell lines in R.

Bioinformatics 2016 04 3;32(8):1272-4. Epub 2015 Dec 3.

Developmental Therapeutic Branch, Center for Cancer Research, NCI, NIH, Bethesda, MD 20892, USA.

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http://dx.doi.org/10.1093/bioinformatics/btv701DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4907377PMC
April 2016

HIV-1 Integrase Strand Transfer Inhibitors with Reduced Susceptibility to Drug Resistant Mutant Integrases.

ACS Chem Biol 2016 Apr 5;11(4):1074-81. Epub 2016 Feb 5.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health , Bethesda, Maryland 20892, United States.

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http://dx.doi.org/10.1021/acschembio.5b00948DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4836387PMC
April 2016

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

Bioorg Med Chem 2016 Apr 9;24(7):1469-79. Epub 2016 Feb 9.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2016.02.015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4789169PMC
April 2016

topIb, a phylogenetic hallmark gene of Thaumarchaeota encodes a functional eukaryote-like topoisomerase IB.

Nucleic Acids Res 2016 Apr 22;44(6):2795-805. Epub 2016 Feb 22.

Sorbonne Universités, Université Pierre et Marie Curie (UPMC), CNRS, Institut de Biologie Paris-Seine (IBPS), Unité Evolution Paris-Seine (UMR 7138), F-75005 Paris, France

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http://dx.doi.org/10.1093/nar/gkw097DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4824112PMC
April 2016

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

J Med Chem 2016 04 12;59(8):3840-53. Epub 2016 Apr 12.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b00003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5317104PMC
April 2016

Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2).

J Med Chem 2016 Mar 7;59(6):2734-46. Epub 2016 Mar 7.

Center for Drug Design, Academic Health Center, University of Minnesota , Minneapolis, Minnesota 55455, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01973DOI Listing
March 2016

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

J Exp Clin Cancer Res 2016 Mar 31;35:56. Epub 2016 Mar 31.

National Institutes of Health, National Cancer Institute, Center for Cancer Research, Laboratory of Molecular Pharmacology, 37 Convent Drive, Building 37, Room 5068, Bethesda, MD, 20892-4255, USA.

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http://dx.doi.org/10.1186/s13046-016-0335-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4815242PMC
March 2016

Molecular characterization of irinotecan (SN-38) resistant human breast cancer cell lines.

BMC Cancer 2016 Jan 22;16:34. Epub 2016 Jan 22.

Faculty of Health and Medical Sciences, Department of Veterinary Disease Biology, Section for Molecular Disease Biology and Sino-Danish Breast Cancer Research Centre, University of Copenhagen, Strandboulevarden 49, DK-2100, Copenhagen, Denmark.

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http://dx.doi.org/10.1186/s12885-016-2071-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4722663PMC
January 2016