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Titolo:
THE ROLE OF NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS (NNRTIS) IN THE THERAPY OF HIV-1 INFECTION
Autore:
DECLERCQ E;
Indirizzi:
CATHOLIC UNIV LOUVAIN,REGA INST MED RES,MINDERBROEDERSSTR 10 B-3000 LOUVAIN BELGIUM
Titolo Testata:
Antiviral research
fascicolo: 3, volume: 38, anno: 1998,
pagine: 153 - 179
SICI:
0166-3542(1998)38:3<153:TRONRI>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
IMMUNODEFICIENCY-VIRUS TYPE-1; HIGH-DOSE NEVIRAPINE; NONNUCLEOSIDE INHIBITORS; ANTIVIRAL ACTIVITY; ANTI-HIV-1 ACTIVITY; IN-VITRO; 1-)(2-HYDROXYETHOXY)METHYL>-6-(PHENYLTHIO)THYMINE DERIVATIVES; PYRIDINONE DERIVATIVES; SELECTIVE-INHIBITION; RESISTANCE MUTATIONS;
Keywords:
DELAVIRDINE; HIV; NEVIRAPINE; NNRTIS (NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS); REVERSE TRANSCRIPTASE; TRIPLE-DRUG COMBINATIONS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
146
Recensione:
Indirizzi per estratti:
Citazione:
E. Declercq, "THE ROLE OF NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS (NNRTIS) IN THE THERAPY OF HIV-1 INFECTION", Antiviral research, 38(3), 1998, pp. 153-179

Abstract

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have, in addition to the nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs), gained a definitive place in the treatment of HIV-I infections. Starting from the HEPT and TIBO derivatives, more than 30 structurally different classes of compounds have been identified as NNRTIs, that is compounds that are specifically inhibitory to HIV-I replication and targeted at the HIV-I reverse transcriptase (RT). Two NNRTIs (nevirapine and delavirdine) have been formally licensed for clinical use and several others are in preclinical or clinical development [thiocarboxanilide UC-781, HEPT derivative MKC-447. quinoxalineHEY 097 and DMP 266 (efavirenz)]. The NNRTIs interact with a specific'pocket' site of HIV-1 RT that is closely associated with, but distinct from, the NRTI binding site. NNRTIs are notorious for rapidly eliciting resistance due to mutations of the amino acids surrounding the NNRTI-binding site. However, the emergence of resistant HIV strains can be circumvented if the NNRTIs, alone or in combination, are used from the start at sufficiently high concentrations. In vitro, this procedure has proved to 'knock-out' virus replication and to prevent resistance from arising. In vivo, various triple-drug combinations of NNRTIs (nevirapine, delavirdine or efavirenz) with NRTIs (AZT, 3TC, ddI or d4T)and/or PIs (indinavir or nelfinavir) have been shown to afford a durable anti-HIV activity, as reflected by both a decrease in plasma HIV-1RNA levels and increased CD4 T-lymphocyte counts. (C) 1998 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 15:05:05