Výsledky vyhledávání - "W G, Tarpley"

Oxazolidinones: a new class of antibacterials

Autor: W G Tarpley, C W Ford, G E Zurenko, D L Shinabarger, J K Gibson, P A Aristoff

Publikováno v: Current Opinion in Pharmacology. 1:470-476

The oxazolidinones represent the first truly new class of antibacterial agents to reach the marketplace in several decades. They have a unique mechanism of action involving inhibition of the initiation step of protein synthesis and are not cross-resi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f94776151bdf003ff58f5d14abde43f
https://doi.org/10.1016/s1471-4892(01)00082-0

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Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives

Autor: S M Swaney, Michael J. Genin, S M Poppe, Donna L. Romero, Carolyn Biles, Keiser Bj, Y. Yagi, W G Tarpley

Publikováno v: Journal of Medicinal Chemistry. 43:1034-1040

Through computationally directed broad screening, a novel 1, 5-diphenylpyrazole (DPP) class of HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) has been discovered. Compound 2 (PNU-32945) was found to have good activity versus wild-type

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88d4a28c47aced1fff65c6eded613496
https://doi.org/10.1021/jm990383f

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Pyrimidine Thioethers: A Novel Class of HIV-1 Reverse Transcriptase Inhibitors with Activity Against BHAP-Resistant HIV

Autor: Stephen T. Schlachter, Richard C. Thomas, T. J. Poel, David R. Graber, Robert A. Olmsted, Laurice A. Kopta, Megan Murphy, Richard A. Nugent, S M Swaney, Keiser Bj, Joel Morris, Y. Yagi, Cleek Gary J, W G Tarpley, S M Poppe, Donn G. Wishka

Publikováno v: Journal of Medicinal Chemistry. 41:3793-3803

A series of pyrimidine thioethers was synthesized and evaluated for inhibitory properties against wild-type HIV-1 reverse transcriptase (RT) and an RT carrying the resistance-conferring mutation P236L. Modifications of both the pyrimidine and the fun

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4261683cacd8cb18181116f242af220
https://doi.org/10.1021/jm9800806

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Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor

Autor: D D Ho, P J Pagano, K T Chong, W. G. Tarpley, T J Dueweke, D E Slade, rd R R Gorman, S M Poppe, M Markowitz, S Thaisrivongs, R. R. Hinshaw, H Mo

Publikováno v: Antimicrobial Agents and Chemotherapy. 41:1058-1063

PNU-140690 is a member of a new class of nonpeptidic human immunodeficiency virus (HIV) protease inhibitors (sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones) discovered by structure-based design. PNU-140690 has excellent potency against a vari

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https://doi.org/10.1128/aac.41.5.1058

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(Alkylamino) piperidine bis(heteroaryl)piperizine analogs are potent, broad-spectrum nonnucleoside reverse transcriptase inhibitors of drug-resistant isolates of human immunodeficiency virus type 1 (HIV-1) and select for drug-resistant variants of HIV-1IIIB with reduced replication phenotypes

Autor: T J Poel, Richard C. Thomas, K B Rank, R A Morge, S W Newport, Y Yagi, C Biles, T J Dueweke, D. L. Romero, R A Olmsted, L A Kopta, S K Sharma, D E Slade, W. G. Tarpley, S M Poppe

Publikováno v: Journal of Virology. 70:3698-3705

The (alkylamino)piperidine bis(heteroaryl)piperizines (AAP-BHAPs) are a new class of human immunodeficiency virus type 1 (HIV-1)-specific inhibitors which were identified by targeted screening of recombinant reverse transcriptase (RT) enzymes carryin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::612cc6a32e010235b307f7e0c1f8b224
https://doi.org/10.1128/jvi.70.6.3698-3705.1996

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Validation of a quantitative RNA PCR assay for HIV-1 in human plasma

Autor: K. W. Nuorala, K. S. Krieger, S. M. Poppe, D. J. Crampton, K. A. Re, R. K. Patel, T. J. Dueweke, W. G. Tarpley, L. K. Wathen

Publikováno v: Journal of Clinical Laboratory Analysis. 10:262-268

A quantitative human immunodeficiency virus type 1 (HIV-1) RNA polymerase chain reaction assay has been validated analytically and clinically in > 13,000 samples. The assay is highly reproducible with intra- and inter-assay precision of 16% and 19%,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8d8c87803009d644b6efb65b9c80ac94
https://doi.org/10.1002/(sici)1098-2825(1996)10:5<262::aid-jcla6>3.0.co

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Targeting Delavirdine/Atevirdine Resistant HIV-1: Identification of (Alkylamino)piperidine-Containing Bis(heteroaryl)piperazines as Broad Spectrum HIV-1 Reverse Transcriptase Inhibitors

Publikováno v: Journal of Medicinal Chemistry. 39:3769-3789

A novel class of bis(heteroaryl)piperazine (BHAP) analogs which possesses the ability to inhibit NNRTI (non-nucleoside reverse transcriptase inhibitor) resistant recombinant HIV-1 reverse transcriptase (RT) and NNRTI resistant variants of HIV-1 has b

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https://doi.org/10.1021/jm960158n

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A Drug Resistance Mutation in the Inhibitor Binding Pocket of Human Immunodeficiency Virus Type 1 Reverse Transcriptase Impairs DNA Synthesis and RNA Degradation

Autor: Naisheng Fan, S K Sharma, S M Poppe, Richard C. Thomas, David B. Evans, K B Rank, L A Kopta, D E Slade, W. G. Tarpley, R A Olmsted

Publikováno v: Biochemistry. 35:9737-9745

Selection of the IIIB strain of human immunodeficiency virus type (HIV-1) resistant to the (alkylamino)piperidine-bis(heteroaryl)piperazine (AAP-BHAP) U-104489 results in substitution of a glycine to glutamate at residue 190 (G190E) of reverse transc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ff6ed3622d40bbd08fdaebc441b3eb0
https://doi.org/10.1021/bi9600308

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Characterization of the p68/p58 Heterodimer of Human Immunodeficiency Virus Type 2 Reverse Transcriptase

Autor: Naisheng Fan, S K Sharma, W. G. Tarpley, S M Poppe, K B Rank

Publikováno v: Biochemistry. 35:1911-1917

Recently we demonstrated that the p58 subunit of p68/p58 HIV-2 reverse transcriptase (RT) heterodimer, produced by processing of p68/p68 homodimer with recombinant HIV-2 protease, terminates at Met484 [Fan, N., et al. (1995) J. Biol. Chem. 270, 13573

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https://doi.org/10.1021/bi9516440

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