E. Kiselev

发表

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

Y. Pommier, S. Hughes, M. Métifiot, 2016, Nucleic acids research.

Exploring a 2-Naphthoic Acid Template for the Structure-Based Design of P2Y14 Receptor Antagonist Molecular Probes

Kyle A. Brown, R. Stevens, K. Jacobson, 2014, ACS chemical biology.

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

Steven M. Moss, Hualiang Jiang, R. Stevens, 2014, Nature.

Two disparate ligand-binding sites in the human P2Y1 receptor

Hualiang Jiang, R. Stevens, K. Jacobson, 2015, Nature.

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

Kyle A. Brown, K. Jacobson, T. K. Harden, 2016, Journal of medicinal chemistry.

Identification of a ligand binding hot spot and structural motifs replicating aspects of tyrosyl-DNA phosphodiesterase I (TDP1) phosphoryl recognition by crystallographic fragment cocktail screening.

Y. Pommier, J. Tropea, D. Waugh, 2019, Nucleic acids research.

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.

Y. Pommier, Shar-yin N. Huang, C. Marchand, 2018, DNA repair.

Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.

K. Jacobson, Zhang-Guo Gao, E. Kiselev, 2014, Biochemical pharmacology.

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

Y. Pommier, K. Shi, E. Kiselev, 2018, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

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

Muthana Al Abo, Y. Pommier, V. Rajapakse, 2017, Molecular Cancer Therapeutics.

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

Y. Pommier, Shar-yin N. Huang, H. Sasanuma, 2016, ACS chemical biology.

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

Y. Pommier, M. Cushman, K. Agama, 2012, Journal of medicinal chemistry.

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.

Y. Pommier, C. Marchand, K. Agama, 2018, Journal of medicinal chemistry.

An unexpected synthesis of 3,5-diaryl-1,2,4-thiadiazoles from thiobenzamides and methyl bromocyanoacetate.

M. Cushman, E. Kiselev, Abdelrahman S. Mayhoub, 2011, Tetrahedron letters.

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

Y. Pommier, J. Balzarini, S. Noppen, 2015, European journal of medicinal chemistry.

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

Taresh K. Sethi, J. Freeman, Y. Pommier, 2017, Journal of medicinal chemistry.

Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.

Y. Pommier, T. Dexheimer, M. Cushman, 2010, Journal of medicinal chemistry.

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

Y. Pommier, M. Cushman, K. Agama, 2012, The Journal of organic chemistry.

Induction of Retinoid X Receptor Activity and Consequent Upregulation of p21WAF1/CIP1 by Indenoisoquinolines in MCF7 Cells

J. Pezzuto, M. Conda-Sheridan, R. V. van Breemen, 2011, Cancer Prevention Research.

Optimization of the Lactam Side Chain of 7-Azaindenoisoquinoline Topoisomerase I Inhibitors and Mechanism of Action Studies in Cancer Cells

Y. Pommier, M. Cushman, K. Agama, 2014, Journal of medicinal chemistry.

Renal Intercalated Cells Sense and Mediate Inflammation via the P2Y14 Receptor

K. Jacobson, M. Pittet, Dennis Brown, 2015, PloS one.

Induction of apoptosis by 3-amino-6-(3-aminopropyl)-5,6-dihydro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline via modulation of MAPKs (p38 and c-Jun N-terminal kinase) and c-Myc in HL-60 human leukemia cells.

J. Pezzuto, M. Conda-Sheridan, M. Cushman, 2012, Journal of natural products.

7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.

Y. Pommier, T. Dexheimer, M. Cushman, 2011, Journal of medicinal chemistry.

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

Y. Pommier, C. Marchand, K. Agama, 2018, European journal of medicinal chemistry.

Topoisomerase I (TOP1) dynamics: conformational transition from open to closed states

Y. Pommier, P. Forterre, Hongliang Zhang, 2022, Nature communications.

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

Y. Pommier, C. Redon, C. Marchand, 2017, Journal of medicinal chemistry.

Interfacial inhibitors.

Y. Pommier, C. Marchand, E. Kiselev, 2015, Bioorganic & medicinal chemistry letters.

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

Y. Pommier, Jiashu Xie, E. Kiselev, 2019, Journal of medicinal chemistry.

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

Y. Pommier, Jiashu Xie, E. Kiselev, 2019, DNA repair.

Small molecule microarray identifies inhibitors of tyrosyl-DNA phosphodiesterase 1 that simultaneously access the catalytic pocket and two substrate binding sites†

Y. Pommier, J. Tropea, D. Waugh, 2021, Chemical science.

Induction of Retinoid X Receptor Activity and Consequent Upregulation of p21 by Indenoisoquinolines in MCF7 Cells

J. Pezzuto, M. Conda-Sheridan, T. Kondratyuk, 2011 .

Nucleotides Acting at P2Y Receptors: Connecting Structure and Function

R. Stevens, K. Jacobson, V. Katritch, 2015, Molecular Pharmacology.

Identification of multidentate tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors that simultaneously access the DNA, protein and catalytic-binding sites by oxime diversification

Y. Pommier, J. Tropea, T. Burke, 2023, RSC chemical biology.

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

Y. Pommier, M. Métifiot, M. Kvaratskhelia, 2018, Molecules.

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

Kyle A. Brown, R. Stevens, K. Jacobson, 2015, Bioorganic & medicinal chemistry letters.

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

K. Jacobson, E. Kiselev, S. Paoletta, 2015, Bioorganic & medicinal chemistry.

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

K. Jacobson, Zhang-Guo Gao, E. Kiselev, 2014, Computational and structural biotechnology journal.

Nucleotides Acting at P 2 Y Receptors : Connecting Structure and Function

R. Stevens, K. Jacobson, V. Katritch, 2015 .

Design, Synthesis and Pharmacological Characterization of a Fluorescent Agonist of the P2Y 14 Receptor

Kyle A. Brown, R. Stevens, K. Jacobson, 2015 .

Optimization of the Lactam Side Chain of 7-Azaindenoisoquinoline Topoisomerase I Inhibitors and Mechanism of Action Studies in Cancer Cells

M. Cushman, K. Agama, E. Kiselev, 2014, Journal of medicinal chemistry.