Search Results - "Witmer, Marc V"

Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection by Summa, Vincenzo, Petrocchi, Alessia, Bonelli, Fabio, Crescenzi, Benedetta, Donghi, Monica, Ferrara, Marco, Fiore, Fabrizio, Gardelli, Cristina, Gonzalez Paz, Odalys, Hazuda, Daria J, Jones, Philip, Kinzel, Olaf, Laufer, Ralph, Monteagudo, Edith, Muraglia, Ester, Nizi, Emanuela, Orvieto, Federica, Pace, Paola, Pescatore, Giovanna, Scarpelli, Rita, Stillmock, Kara, Witmer, Marc V, Rowley, Michael

“…Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for…”
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A Naphthyridine Carboxamide Provides Evidence for Discordant Resistance between Mechanistically Identical Inhibitors of HIV-1 Integrase by Hazuda, Daria J., Anthony, Neville J., Gomez, Robert P., Jolly, Samson M., Wai, John S., Zhuang, Linghang, Fisher, Thorsten E., Embrey, Mark, Guare, James P., Egbertson, Melissa S., Vacca, Joseph P., Huff, Joel R., Felock, Peter J., Witmer, Marc V., Stillmock, Kara A., Danovich, Robert, Grobler, Jay, Miller, Michael D., Espeseth, Amy S., Jin, Lixia, I-Wu Chen, Lin, Jiunn H., Kassahun, Kelem, Ellis, Joan D., Wong, Bradley K., Xu, Wei, Pearson, Paul G., Schleif, William A., Cortese, Riccardo, Emini, Emilio, Summa, Vincenzo, Holloway, M. Katharine, Young, Steven D., Coffin, John M.

“…The increasing incidence of resistance to current HIV-1 therapy underscores the need to develop antiretroviral agents with new mechanisms of action. Integrase,…”
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Design and Synthesis of 8-Hydroxy-[1,6]Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells by Zhuang, Linghang, Wai, John S, Embrey, Mark W, Fisher, Thorsten E, Egbertson, Melissa S, Payne, Linda S, Guare, James P, Vacca, Joseph P, Hazuda, Daria J, Felock, Peter J, Wolfe, Abigail L, Stillmock, Kara A, Witmer, Marc V, Moyer, Gregory, Schleif, William A, Gabryelski, Lori J, Leonard, Yvonne M, Lynch, Joseph J, Michelson, Stuart R, Young, Steven D

“…Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1…”
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Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold by Williams, Peter D., Staas, Donnette D., Venkatraman, Shankar, Loughran, H. Marie, Ruzek, Rowena D., Booth, Theresa M., Lyle, Terry A., Wai, John S., Vacca, Joseph P., Feuston, Bradley P., Ecto, Linda T., Flynn, Jessica A., DiStefano, Daniel J., Hazuda, Daria J., Bahnck, Carolyn M., Himmelberger, Amy L., Dornadula, Geetha, Hrin, Renee C., Stillmock, Kara A., Witmer, Marc V., Miller, Michael D., Grobler, Jay A.

“…Optimization studies using an HIV RNase H active site inhibitor containing a 1-hydroxy-1,8-naphthyridin-2(1H)-one core identified 4-position substituents that…”
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Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase by Melamed, Jeffrey Y., Egbertson, Melissa S., Varga, Sandor, Vacca, Joseph P., Moyer, Greg, Gabryelski, Lori, Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Schleif, William, Hazuda, Daria J., Leonard, Yvonne, Jin, Lixia, Ellis, Joan D., Young, Steven D.

“…HIV-1 integrase catalyzes the insertion of viral DNA into the genome of the host cell. Integrase inhibitor…”
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Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5- a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors by Langford, H. Marie, Williams, Peter D., Homnick, Carl F., Vacca, Joseph P., Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Hazuda, Daria J., Gabryelski, Lori J., Schleif, William A.

“…A series of 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5- a]pyrazine-2-carboxamides was synthesized and tested for their inhibition of HIV-1 integrase catalytic…”
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10-Hydroxy-7,8-dihydropyrazino[1′,2′:1,5]pyrrolo[2,3- d]pyridazine-1,9(2 H,6 H)-diones: Potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants by Wiscount, Catherine M., Williams, Peter D., Tran, Lekhanh O., Embrey, Mark W., Fisher, Thorsten E., Sherman, Vanessa, Homnick, Carl F., Donnette Staas, D., Lyle, Terry A., Wai, John S., Vacca, Joseph P., Wang, ZiQiang, Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Miller, Michael D., Hazuda, Daria J., Day, Alysha M., Gabryelski, Lori J., Ecto, Linda T., Schleif, William A., DiStefano, Daniel J., Kochansky, Christopher J., Reza Anari, M.

“…[Display omitted] A series of 10-hydroxy-7,8-dihydropyrazino[1′,2′:1,5]pyrrolo[2,3- d]pyridazine-1,9(2 H,6 H)-diones was synthesized and tested for their…”
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A potent and orally active HIV-1 integrase inhibitor by Egbertson, Melissa S., Moritz, H. Marie, Melamed, Jeffrey Y., Han, Wei, Perlow, Debra S., Kuo, Michelle S., Embrey, Mark, Vacca, Joseph P., Zrada, Matthew M., Cortes, Amanda R., Wallace, Audrey, Leonard, Yvonne, Hazuda, Daria J., Miller, Michael D., Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Schleif, William, Gabryelski, Lori J., Moyer, Gregory, Ellis, Joan D., Jin, Lixia, Xu, Wei, Braun, Matthew P., Kassahun, Kellem, Tsou, Nancy N., Young, Steven D.

“…A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent…”
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Integrase Inhibitors and Cellular Immunity Suppress Retroviral Replication in Rhesus Macaques by Hazuda, Daria J., Young, Steven D., Guare, James P., Anthony, Neville J., Gomez, Robert P., Wai, John S., Vacca, Joseph P., Handt, Larry, Motzel, Sherri L., Klein, Hilton J., Dornadula, Geethanjali, Danovich, Robert M., Witmer, Marc V., Keith A. A. Wilson, Tussey, Lynda, Schleif, William A., Gabryelski, Lori S., Jin, Lixia, Miller, Michael D., Casimiro, Danilo R., Emini, Emilio A., Shiver, John W.

“…We describe the efficacy of L-870812, an inhibitor of HIV-1 and SIV integrase, in rhesus macaques infected with the simian-human immunodeficiency virus (SHIV)…”
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A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells by Embrey, Mark W., Wai, John S., Funk, Timothy W., Homnick, Carl F., Perlow, Debbie S., Young, Steven D., Vacca, Joseph P., Hazuda, Daria J., Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Moyer, Gregory, Schleif, William A., Gabryelski, Lori J., Jin, Lixia, Chen, I-Wu, Ellis, Joan D., Wong, Bradley K., Lin, Jiunn H., Leonard, Yvonne M., Tsou, Nancy N., Zhuang, Linghang

“…Introduction of a 5,6-dihydrouracil functionality in the 5-position of N-(4-fluorobenzyl)-8-hydroxy-[1,6]naphthyridine-7-carboxamide 1 led to a series of…”
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Increased sensitivity to DNA-alkylating agents in CHO mutants with decreased poly(ADP-ribose) polymerase activity by Witmer, M V, Aboul-Ela, N, Jacobson, M K, Stamato, T D

“…Using a replica-plating procedure and a 32P-NAD+ permeable cell-screening assay, we have isolated a CHO mutant, PADR-9, which displays approximately 17% of the…”
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Isolation of Chinese hamster ovary cells with reduced poly(ADP-ribose) polymerase activity by MacLaren, R A, Witmer, M V, Richardson, E, Stamato, T D

“…The biological function of poly(ADP-ribose) polymerase in DNA repair, cell-cycle regulation and cellular differentiation has yet to be defined. Isolation of…”
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