Current state-of-the-art in preclinical and clinical development of novel non-nucleoside HIV-1 reverse transcriptase inhibitors
- 21 June 2006
- journal article
- Published by Informa Healthcare in Expert Opinion on Therapeutic Patents
- Vol. 16 (7) , 939-962
- https://doi.org/10.1517/13543776.16.7.939
Abstract
In spite of the tremendous advance in our understanding of the HIV-1 life cycle and of the molecular mechanisms underlying its pathogenesis, it is still not possible to fully control the HIV-1 infection for long periods of time, not to mention eradicate it. However, as it is still unclear whether an effective vaccine could be developed in a short time, therapeutic approaches based on the combination of different potent antiviral drugs are now thought to be the best option for the control of HIV-1 infection in patients. For this reason, development of novel molecules that are safer, more potent and less sensitive to drug resistance than available drugs is mandatory. Among the currently exploited anti-HIV drugs, non-nucleoside reverse transcriptase inhibitors play a major role. This review will summarise the most recent advances and evolutionary trends for this class of anti-HIV drugsKeywords
This publication has 41 references indexed in Scilit:
- High Potency of Indolyl Aryl Sulfone Nonnucleoside Inhibitors towards Drug-Resistant Human Immunodeficiency Virus Type 1 Reverse Transcriptase Mutants Is Due to Selective Targeting of Different Mechanistic Forms of the EnzymeAntimicrobial Agents and Chemotherapy, 2005
- Novel 8-Substituted Dipyridodiazepinone Inhibitors with a Broad-Spectrum of Activity against HIV-1 Strains Resistant to Non-nucleoside Reverse Transcriptase InhibitorsJournal of Medicinal Chemistry, 2005
- Structure Based Activity Prediction of HIV-1 Reverse Transcriptase InhibitorsJournal of Medicinal Chemistry, 2005
- Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.Journal of Medicinal Chemistry, 2004
- Design of Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 2.Journal of Medicinal Chemistry, 2004
- Simple, Short Peptide Derivatives of a Sulfonylindolecarboxamide (L-737,126) Active in Vitro against HIV-1 Wild Type and Variants Carrying Non-Nucleoside Reverse Transcriptase Inhibitor Resistance MutationsJournal of Medicinal Chemistry, 2004
- A randomized, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in antiretroviral naive, HIV-1 infected subjectsAIDS, 2003
- Structural biology of HIV 1 1Edited by P. E. WrightJournal of Molecular Biology, 1999
- Resistance to nevirapine of HIV-1 reverse transcriptase mutants: loss of stabilizing interactions and thermodynamic or steric barriers are induced by different single amino acid substitutionsJournal of Molecular Biology, 1997
- Locations of Anti-AIDS Drug Binding Sites and Resistance Mutations in the Three-dimensional Structure of HIV-1 Reverse TranscriptaseJournal of Molecular Biology, 1994