Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Robert P. Gomez"'
Autor:
Sarah L. Huszar, Thomas W. Rosahl, Sophie Parmentier-Batteur, H. Fauré, Thomas J. Tucker, Craig A. Stump, Emannuel Le Poul, Richard Hargreaves, Brian C. Magliaro, Xu-Fang Zhang, Neville J. Anthony, Thomas Forest, Theresa M. Williams, Jason M. Uslaner, Nathalie Lambeng, Julie A. O'Brien, Robert P. Gomez, Robert M. Tynebor, Peter H. Hutson, Sonia Poli, Jean-Philippe Rocher, Britta A. Mattson, Karsten Menzel
Publikováno v:
Neuropharmacology. 82:161-173
Previous work has suggested that activation of mGlu5 receptor augments NMDA receptor function and thereby may constitute a rational approach addressing glutamate hypofunction in schizophrenia and a target for novel antipsychotic drug development. Her
Autor:
Robert P. Gomez, Ming-Tain Lai, Jay A. Grobler, Peter J. Felock, Renee Hrin, Meiqing Lu, Daria J. Hazuda, Michael D. Miller, Philip M. McKenna, Vandna Munshi, Georgia B. McGaughey, Youwei Yan, Neville J. Anthony, Sanjeev Munshi, Theresa M. Williams, Ying-Jie Wang
Publikováno v:
Antimicrobial Agents and Chemotherapy. 56:3324-3335
MK-6186 is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) which displays subnanomolar potency against wild-type (WT) virus and the two most prevalent NNRTI-resistant RT mutants (K103N and Y181C) in biochemical assays. In addition, it s
Autor:
Yuexia Liang, Daniel DeStefano, Samson M. Jolly, Georgia B. McGaughey, Joe P. Vacca, Bang-Lin Wan, Michael W. Miller, Robert P. Gomez, Youwei Yan, Sinoeun Touch, Neville J. Anthony, Robert M. Tynebor, Ming-Tain Lai, Rosa I. Sanchez, Vandna Munshi, Thomas J. Tucker, Theresa M. Williams, Peter J. Felock, Brenda Paton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7344-7350
Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constrain
Autor:
Nancy E. Kohl, Charles A. Omer, Michael W. Conner, Neville J. Anthony, Joseph P. Davide, S. Jane Desolms, Elizabeth A. Giuliani, Robert P. Gomez, Samuel L. Graham, Kelly Hamilton, Laurence K. Handt, George D. Hartman, Kenneth S. Koblan, Astrid M. Kral, Patricia J. Miller, Scott D. Mosser, Timothy J. O'Neill, Elaine Rands, Michael D. Schaber, Jackson B. Gibbs, Allen Oliff
Publikováno v:
Nature Medicine. 1:792-797
For Ras oncoproteins to transform mammalian cells, they must be post-translationally modified with a farnesyl group in a reaction catalysed by the enzyme farnesyl-protein transferase (FPTase). Inhibitors of FPTase have therefore been proposed as anti
Publikováno v:
Tetrahedron Letters. 36:3821-3824
The synthesis of methylene-oxy dipeptide isosteres has been achieved by stereoselective functionalisation of the acylmorpholinone 3 .
Autor:
Lee Ta Jyh, Neville J. Anthony, Robert P. Gomez, S D Mosser, Michael W. Conner, Nancy E. Kohl, W. J. Holtz, F R Wilson, E A Giuliani, S J deSolms
Publikováno v:
Proceedings of the National Academy of Sciences. 91:9141-9145
The posttranslational addition of a farnesyl moiety to the Ras oncoprotein is essential for its transforming activity. Cell-active inhibitors of the enzyme that catalyzes this reaction, protein farnesyltransferase, have been shown to selectively bloc
Autor:
Michael W. Miller, Yuexia Liang, Ming-Tain Lai, Georgia B. McGaughey, Bang-Lin Wan, Maricel Torrent, Rosa I. Sanchez, Daniel J. DiStefano, John C. Reid, Peter J. Felock, Robert P. Gomez, Theresa M. Williams, Brenda Paton, Joseph P. Vacca, Youwei Yan, Jessica A. Flynn, Samson J. Jolly, Neville J. Anthony, Vandna Munshi
Publikováno v:
Journal of medicinal chemistry. 54(22)
Highly active antiretroviral therapy (HAART) significantly reduces human immunodeficiency virus (HIV) viral load and has led to a dramatic decrease in acquired immunodeficiency syndrome (AIDS) related mortality. Despite this success, there remains a
Publikováno v:
ChemInform. 26
The synthesis of methylene-oxy dipeptide isosteres has been achieved by stereoselective functionalisation of the acylmorpholinone 3 .
Autor:
William A. Schleif, Lori J. Gabryelski, Amanda R. Cortes, James P. Guare, Steven D. Young, I.-W. Chen, John S. Wai, Samson M. Jolly, Daria J. Hazuda, Gregory Moyer, Robert P. Gomez, Peter J. Felock, Lixia Jin, Neville J. Anthony, Kara A. Stillmock, Joseph P. Vacca
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(11)
A series of 5-amino derivatives of 8-hydroxy[1,6]-naphthyridine-7-carboxamide exhibiting sub-micromolar potency against replication of HIV-1 in cell culture was identified. One of these analogs, compound 12, displayed excellent pharmacokinetic proper
Autor:
Daria J. Hazuda, John S. Wai, Lynda Tussey, Neville J. Anthony, Geethanjali Dornadula, Michael D. Miller, John W. Shiver, Joseph P. Vacca, Sherri L. Motzel, Lixia Jin, Robert M. Danovich, Marc V. Witmer, Larry Handt, James P. Guare, Danilo R. Casimiro, Steven D. Young, Lori S. Gabryelski, Hilton J. Klein, Robert P. Gomez, Keith A. Wilson, William A. Schleif, Emilio A. Emini
Publikováno v:
Science (New York, N.Y.). 305(5683)
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) 89.6P. When initiated before CD4 cell depletion, L-870812 therapy mediated a sustained supp