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Discovery, Synthesis, and Evaluation of Oxynitidine Derivatives as Dual Inhibitors of DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1), and Potential Antitumor Agents.

Zhang XR, Wang HW, Tang WL, Zhang Y, Yang H, Hu DX, Ravji A, Marchand C, Kiselev E, Ofori-Atta K, Agama K, Pommier Y, An LK.

J Med Chem. 2018 Nov 21;61(22):9908-9930. doi: 10.1021/acs.jmedchem.8b00639. Epub 2018 Oct 31.


HIV-1 Integrase-Targeted Short Peptides Derived from a Viral Protein R Sequence.

Zhao XZ, Métifiot M, Kiselev E, Kessl JJ, Maddali K, Marchand C, Kvaratskhelia M, Pommier Y, Burke TR Jr.

Molecules. 2018 Jul 26;23(8). pii: E1858. doi: 10.3390/molecules23081858.


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

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

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


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

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

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


New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2).

Ribeiro CJA, Kankanala J, Shi K, Kurahashi K, Kiselev E, Ravji A, Pommier Y, Aihara H, Wang Z.

Eur J Pharm Sci. 2018 Jun 15;118:67-79. doi: 10.1016/j.ejps.2018.03.021. Epub 2018 Mar 21.


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

Al Abo M, Sasanuma H, Liu X, Rajapakse VN, Huang SY, Kiselev E, Takeda S, Plunkett W, Pommier Y.

Mol Cancer Ther. 2017 Nov;16(11):2543-2551. doi: 10.1158/1535-7163.MCT-17-0110. Epub 2017 Aug 11.


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

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

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


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

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

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


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.

Métifiot M, Johnson BC, Kiselev E, Marler L, Zhao XZ, Burke TR Jr, Marchand C, Hughes SH, Pommier Y.

Nucleic Acids Res. 2016 Aug 19;44(14):6896-906. doi: 10.1093/nar/gkw592. Epub 2016 Jul 1.


Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.

Junker A, Balasubramanian R, Ciancetta A, Uliassi E, Kiselev E, Martiriggiano C, Trujillo K, Mtchedlidze G, Birdwell L, Brown KA, Harden TK, Jacobson KA.

J Med Chem. 2016 Jul 14;59(13):6149-68. doi: 10.1021/acs.jmedchem.6b00044. Epub 2016 Jun 22.


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

Marchand C, Abdelmalak M, Kankanala J, Huang SY, Kiselev E, Fesen K, Kurahashi K, Sasanuma H, Takeda S, Aihara H, Wang Z, Pommier Y.

ACS Chem Biol. 2016 Jul 15;11(7):1925-33. doi: 10.1021/acschembio.5b01047. Epub 2016 May 11.


Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers.

Rivero-Buceta E, Carrero P, Casanova E, Doyagüez EG, Madrona A, Quesada E, Peréz-Pérez MJ, Mateos R, Bravo L, Mathys L, Noppen S, Kiselev E, Marchand C, Pommier Y, Liekens S, Balzarini J, Camarasa MJ, San-Félix A.

Eur J Med Chem. 2015 Dec 1;106:132-43. doi: 10.1016/j.ejmech.2015.10.027. Epub 2015 Oct 21.


Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor.

Kiselev E, Balasubramanian R, Uliassi E, Brown KA, Trujillo K, Katritch V, Hammes E, Stevens RC, Harden TK, Jacobson KA.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4733-4739. doi: 10.1016/j.bmcl.2015.08.021. Epub 2015 Aug 10.


Interfacial inhibitors.

Pommier Y, Kiselev E, Marchand C.

Bioorg Med Chem Lett. 2015 Sep 15;25(18):3961-5. doi: 10.1016/j.bmcl.2015.07.032. Epub 2015 Jul 18. Review.


John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors.

Jacobson KA, Gao ZG, Paoletta S, Kiselev E, Chakraborty S, Jayasekara PS, Balasubramanian R, Tosh DK.

Comput Struct Biotechnol J. 2014 Oct 16;13:286-98. doi: 10.1016/j.csbj.2014.10.004. eCollection 2015. Review.


Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands.

Trujillo K, Paoletta S, Kiselev E, Jacobson KA.

Bioorg Med Chem. 2015 Jul 15;23(14):4056-64. doi: 10.1016/j.bmc.2015.03.042. Epub 2015 Mar 21.


Nucleotides Acting at P2Y Receptors: Connecting Structure and Function.

Jacobson KA, Paoletta S, Katritch V, Wu B, Gao ZG, Zhao Q, Stevens RC, Kiselev E.

Mol Pharmacol. 2015 Aug;88(2):220-30. doi: 10.1124/mol.114.095711. Epub 2015 Apr 2. Review.


Two disparate ligand-binding sites in the human P2Y1 receptor.

Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B.

Nature. 2015 Apr 16;520(7547):317-21. doi: 10.1038/nature14287. Epub 2015 Mar 30.


Renal intercalated cells sense and mediate inflammation via the P2Y14 receptor.

Azroyan A, Cortez-Retamozo V, Bouley R, Liberman R, Ruan YC, Kiselev E, Jacobson KA, Pittet MJ, Brown D, Breton S.

PLoS One. 2015 Mar 23;10(3):e0121419. doi: 10.1371/journal.pone.0121419. eCollection 2015.


Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes.

Kiselev E, Barrett MO, Katritch V, Paoletta S, Weitzer CD, Brown KA, Hammes E, Yin AL, Zhao Q, Stevens RC, Harden TK, Jacobson KA.

ACS Chem Biol. 2014 Dec 19;9(12):2833-42. doi: 10.1021/cb500614p. Epub 2014 Oct 20.

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