Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.

We have used a structure-based approach to design a novel series of non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Detailed analysis of a wide range of crystal structures of HIV-1 RT-NNRTI complexes together with data on drug resistance mutations has identified factors important for tight binding o...

Full description

Bibliographic Details
Main Authors:	Hopkins, A, Ren, J, Milton, J, Hazen, R, Chan, J, Stuart, D, Stammers, D
Format:	Journal article
Language:	English
Published:	2004

Similar Items

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
by: Freeman, G, et al.
Published: (2004)

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

Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIV reverse transcriptase.
by: Ren, J, et al.
Published: (2008)

Crystallographic analysis of the binding modes of thiazoloisoindolinone non-nucleoside inhibitors to HIV-1 reverse transcriptase and comparison with modeling studies.
by: Ren, J, et al.
Published: (1999)

2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
by: Chan, J, et al.
Published: (2001)

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

Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
by: Ren, J, et al.
Published: (2008)

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

Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors.
by: Hopkins, A, et al.
Published: (1996)

Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation non-nucleoside inhibitors.
by: Ren, J, et al.
Published: (2001)

Structure of HIV-2 reverse transcriptase at 2.35-A resolution and the mechanism of resistance to non-nucleoside inhibitors.
by: Ren, J, et al.
Published: (2002)

HEPT: From an investigation of lithiation of nucleosides towards a rational design of non-nucleoside reverse transcriptase inhibitors of HIV-1
by: Tanaka, H, et al.
Published: (1999)

Binding of the second generation non-nucleoside inhibitor S-1153 to HIV-1 reverse transcriptase involves extensive main chain hydrogen bonding.
by: Ren, J, et al.
Published: (2000)

Crystal structures of HIV-1 reverse transcriptases mutated at codons 100, 106 and 108 and mechanisms of resistance to non-nucleoside inhibitors.
by: Ren, J, et al.
Published: (2004)

HIV reverse transcriptase structures: designing new inhibitors and understanding mechanisms of drug resistance.
by: Ren, J, et al.
Published: (2005)

Structural basis for the resilience of efavirenz (DMP-266) to drug resistance mutations in HIV-1 reverse transcriptase.
by: Ren, J, et al.
Published: (2000)

Structural insights into mechanisms of non-nucleoside drug resistance for HIV-1 reverse transcriptases mutated at codons 101 or 138.
by: Ren, J, et al.
Published: (2006)

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

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

Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
by: Valeria Famiglini, et al.
Published: (2016-02-01)

The Lysine 65 Residue in HIV-1 Reverse Transcriptase Function and in Nucleoside Analog Drug Resistance
by: Scott J. Garforth, et al.
Published: (2014-10-01)

Lipidic strategy for improving bioavailability of nucleoside HIV reverse transcriptase inhibitor
by: N. S. Shastina, et al.
Published: (2011-04-01)

Global Conformational Dynamics of HIV-1 Reverse Transcriptase Bound to Non-Nucleoside Inhibitors
by: Peter V. Coveney, et al.
Published: (2012-07-01)

Biophysical Insights into the Inhibitory Mechanism of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
by: Nicolas Sluis-Cremer, et al.
Published: (2013-11-01)

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.
by: Esnouf, R, et al.
Published: (1997)

Novel Thiazolidin-4-ones as Potential Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase
by: Anthi Petrou, et al.
Published: (2019-10-01)

Modeling of cytotoxicity on some non- nucleoside reverse transcriptase inhibitors of HIV-1: role of physicochemical parameters
by: B.K. Tiwari, et al.
Published: (2006-02-01)

3'-Azido-3'-deoxythymidine drug resistance mutations in HIV-1 reverse transcriptase can induce long range conformational changes.
by: Ren, J, et al.
Published: (1998)

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

Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV
by: Daniel M. Himmel, et al.
Published: (2020-06-01)

APOBEC3 selects V179I in HIV-1 reverse transcriptase to provide selective advantage for non-nucleoside reverse transcriptase inhibitor-resistant mutants
by: Richa Dwivedi, et al.
Published: (2022-07-01)

Identification of Boronate-Containing Diarylpyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
by: Da Feng, et al.
Published: (2022-11-01)

Allosteric inhibitors against HIV-1 reverse transcriptase: design and synthesis of MKC-442 analogues having an omega-functionalized acyclic structure.
by: Tanaka, H, et al.
Published: (1998)

Dolutegravir Plus Two Nucleoside Reverse Transcriptase Inhibitors versus Efavirenz Plus Two Nucleoside Reverse Transcriptase Inhibitors As Initial Antiretroviral Therapy for People with HIV: A Systematic Review.
by: George W Rutherford, et al.
Published: (2016-01-01)

Drivers of HIV-1 drug resistance to non-nucleoside reverse-transcriptase inhibitors (NNRTIs) in nine southern African countries: a modelling study
by: Julien Riou, et al.
Published: (2021-10-01)

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

Cloning, expression, purification, and crystallisation of HIV-2 reverse transcriptase.
by: Bird, L, et al.
Published: (2003)

Efficacy and safety of novel russian non-nucleoside reverse transcriptase inhibitor elsulfavirine in combination with 2 nucleoside/nucleotide reverse transcriptase inhibitors in first-line HIV treatment – 96-week study
by: A. V. Kravchenko, et al.
Published: (2018-07-01)

Nucleoside analogue reverse transcriptase inhibitors differentially inhibit human LINE-1 retrotransposition.
by: R Brad Jones, et al.
Published: (2008-01-01)

Mechanisms of nucleoside analogue resistance associated with the selection of HIV-1 reverse transcriptase thumb subdomain polymorphisms
by: Betancor, G, et al.
Published: (2010)