Výsledky vyhledávání

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

Zobrazit plný text záznamu

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

Zobrazit plný text záznamu

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df736ec299e4d25ad33f97274f0768a6
https://doi.org/10.1128/aac.41.5.1058

Zobrazit plný text záznamu

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

Zobrazit plný text záznamu

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

Zobrazit plný text záznamu

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0824a7c79ecad1e41d45e4d2330c1f5e
https://doi.org/10.1021/bi9516440

Zobrazit plný text záznamu

U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication

Autor: Mariano Busso, Donna Lee Romero, T J Dueweke, Kathleen M. Downey, S. M. Swaney, Lionel Resnick, S M Poppe, Fritz Reusser, Antero G. So, Irene W. Althaus

Publikováno v: Antimicrobial Agents and Chemotherapy. 37:1127-1131

Bisheteroarylpiperazines are potent inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). We describe a novel bisheteroarylpiperazine, U-90152 [1-(5-methanesulfonamido-1H-indol-2-yl-carbonyl)-4-[3-(1-methyl eth yl-amin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5071316058796b443c9e591414b0d9af
https://doi.org/10.1128/aac.37.5.1127

Zobrazit plný text záznamu

The differential processing of homodimers of reverse transcriptases from human immunodeficiency viruses type 1 and 2 is a consequence of the distinct specificities of the viral proteases

Autor: N, Fan, K B, Rank, J W, Leone, R L, Heinrikson, C A, Bannow, C W, Smith, D B, Evans, S M, Poppe, W G, Tarpley, D J, Rothrock

Publikováno v: The Journal of biological chemistry. 270(22)

Active, recombinant p68 reverse transcriptase (RT) from human immunodeficiency virus type 2 (HIV-2), with an NH2-terminal extension containing a hexahistidine sequence was isolated from extracts of Escherichia coli by immobilized metal affinity chrom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::708dbafc0a6f8d85ef250ff2406f87ac
https://pubmed.ncbi.nlm.nih.gov/7539431

Zobrazit plný text záznamu

A mutation in reverse transcriptase of bis(heteroaryl)piperazine-resistant human immunodeficiency virus type 1 that confers increased sensitivity to other nonnucleoside inhibitors

Autor: W. G. Tarpley, J. Q. Zhao, S M Poppe, I. S. Y. Chen, T J Dueweke, Mario Stevenson, S. M. Swaney, T. Pushkarskaya

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America. 90(10)

Several nonnucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) have been described, including Nevirapine, thiobenzimidazolone (TIBO) derivatives, pyridinone derivatives such as L-697,661, and the bis(hetero

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aad357fc0ee363cdf6a79598ee994af4
https://pubmed.ncbi.nlm.nih.gov/7685109

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání