A novel mutation (F227L) arises in the reverse transcriptase of human immunodeficiency virus type 1 on dose-escalating treatment of HIV type 1-infected cell cultures with the nonnucleoside reverse transcriptase inhibitor thiocarboxanilide UC-781.

A novel mutation (F227L) arises in the reverse transcriptase of human immunodeficiency virus type 1 on dose-escalating treatment of HIV type 1-infected cell cultures with the nonnucleoside reverse transcriptase inhibitor thiocarboxanilide UC-781.

Treatment of wild-type human immunodeficiency virus [HIV-1(IIIB)]-infected cell cultures with the thiocarboxanilide UC-781 under low selective pressure (i.e., 0.01 microg/ml) resulted in the emergence of V106A RT mutant virus. On increasing drug concentrations (stepwise up to 30 microg/ml) the virus...

Descrizione completa

Dettagli Bibliografici
Autori principali:	Balzarini, J, Pelemans, H, Esnouf, R, De Clercq, E
Natura:	Journal article
Lingua:	English
Pubblicazione:	1998

Documenti analoghi

Mutational analysis of Tyr-318 within the non-nucleoside reverse transcriptase inhibitor binding pocket of human immunodeficiency virus type I reverse transcriptase.
di: Pelemans, H, et al.
Pubblicazione: (1998)

Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol.
di: Anna Figueiredo, et al.
Pubblicazione: (2006-11-01)

A mutation in the 3' region of the human immunodeficiency virus type 1 reverse transcriptase (Y318F) associated with nonnucleoside reverse transcriptase inhibitor resistance.
di: Harrigan, P, et al.
Pubblicazione: (2002)

Characteristics of the Pro225His mutation in human immunodeficiency virus type 1 (HIV-1) reverse transcriptase that appears under selective pressure of dose-escalating quinoxaline treatment of HIV-1.
di: Pelemans, H, et al.
Pubblicazione: (1997)

Assessment of Nonnucleoside Inhibitors Binding to HIV-1 Reverse Transcriptase Using HYDE Scoring
di: Agata Paneth, et al.
Pubblicazione: (2019-04-01)

A proline-to-histidine substitution at position 225 of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) sensitizes HIV-1 RT to BHAP U-90152.
di: Pelemans, H, et al.
Pubblicazione: (1998)

Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors.
di: Pelemans, H, et al.
Pubblicazione: (2000)

Discovery of diarylpyrimidine derivatives bearing piperazine sulfonyl as potent HIV-1 nonnucleoside reverse transcriptase inhibitors
di: Xiangyi Jiang, et al.
Pubblicazione: (2023-04-01)

Review The Emerging Profile of Cross-Resistance among the Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors
di: Nicolas Sluis-Cremer
Pubblicazione: (2014-07-01)

Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors.
di: Auwerx, J, et al.
Pubblicazione: (2004)

Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives.
di: Esnouf, R, et al.
Pubblicazione: (1997)

Mutations at amino acid positions 63, 189, and 396 of human immunodeficiency virus type 1 reverse transcriptase (RT) partially restore the DNA polymerase activity of a Trp229Tyr mutant RT.
di: Pelemans, H, et al.
Pubblicazione: (2001)

The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT.
di: Auwerx, J, et al.
Pubblicazione: (2004)

Pharmacokinetics of lopinavir-ritonavir with and without nonnucleoside reverse transcriptase inhibitors in Ugandan HIV-infected adults.
di: Kityo, C, et al.
Pubblicazione: (2010)

Crystal structures of HIV-1 reverse transcriptase in complex with carboxanilide derivatives.
di: Ren, J, et al.
Pubblicazione: (1998)

Pharmacokinetics and tolerability of the new second-generation nonnucleoside reverse- transcriptase inhibitor KM-023 in healthy subjects
di: Cha YJ, et al.
Pubblicazione: (2014-09-01)

Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine (BHAP) U-90152 explain resistance mutations for this nonnucleoside inhibitor.
di: Esnouf, R, et al.
Pubblicazione: (1997)

1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors with anti-HIV-1 activity.
di: Witvrouw, M, et al.
Pubblicazione: (1998)

Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors.
di: Esnouf, R, et al.
Pubblicazione: (1995)

The Molecular Docking of Specific Reverse Transcriptase Inhibitory Ligands onto the Molecular Model of HIV-1 Reverse Transcriptase
di: Roohallah Yousefi
Pubblicazione: (2024-06-01)

Background Activity of Reverse Transcriptases
di: Angelica V. Timofeeva, et al.
Pubblicazione: (2001-01-01)

A reverse transcriptase ribozyme
di: Biswajit Samanta, et al.
Pubblicazione: (2017-09-01)

Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
di: Romines, K, et al.
Pubblicazione: (2006)

Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
di: Romines, K, et al.
Pubblicazione: (2006)

Approved HIV reverse transcriptase inhibitors in the past decade
di: Guangdi Li, et al.
Pubblicazione: (2022-04-01)

Reverse transcriptase activity in psoriatic lesions: effects of reverse transcriptase inhibitors on keratinocyte proliferation and differentiation
di: Bonté Frédéric, et al.
Pubblicazione: (2009-09-01)

HTLV-1 reverse transcriptase homology model provides structural basis for sensitivity to existing nucleoside/nucleotide reverse transcriptase inhibitors
di: Nicolas Tardiota, et al.
Pubblicazione: (2024-01-01)

Crystals of HIV-1 reverse transcriptase diffracting to 2.2 A resolution.
di: Stammers, D, et al.
Pubblicazione: (1994)

Asymmetric conformational maturation of HIV-1 reverse transcriptase
di: Xunhai Zheng, et al.
Pubblicazione: (2015-06-01)

Phenylethylthiazolylthiourea (PETT) non-nucleoside inhibitors of HIV-1 and HIV-2 reverse transcriptases. Structural and biochemical analyses.
di: Ren, J, et al.
Pubblicazione: (2000)

Continuous and discontinuous changes in the unit cell of HIV-1 reverse transcriptase crystals on dehydration.
di: Esnouf, R, et al.
Pubblicazione: (1998)

Telomerase reverse transcriptase and neurodegenerative diseases
di: Xin Yu, et al.
Pubblicazione: (2023-03-01)

Biochemical mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to stavudine.
di: Lennerstrand, J, et al.
Pubblicazione: (2001)

The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: lessons for inhibitor design.
di: Ren, J, et al.
Pubblicazione: (1995)

Targeting the Structural Maturation Pathway of HIV-1 Reverse Transcriptase
di: Thomas W. Kirby, et al.
Pubblicazione: (2023-11-01)

Designing Novel Hydrazinecarbothioamides as Potential HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
di: Hong Yin, et al.
Pubblicazione: (2017-10-01)

HuR interacts with human immunodeficiency virus type 1 reverse transcriptase, and modulates reverse transcription in infected cells
di: Ennifar Eric, et al.
Pubblicazione: (2008-06-01)

Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2.
di: Milton, J, et al.
Pubblicazione: (1998)

Association between the CYP2B6 polymorphisms and nonnucleoside reverse transcriptase inhibitors drug-induced liver injury: a systematic review and meta-analysis
di: Noppadol Chanhom, et al.
Pubblicazione: (2024-11-01)

Reverse transcriptase inhibitors from curcuma phaeocaulis/
di: Hou, Yu-Chi, et al.