Notice bibliographique
- Notice
Type(s) de contenu et mode(s) de consultation : Texte noté : électronique
Titre(s) : Human immunodeficiency virus reverse transcriptase [Texte électronique] : a bench-to-bedside success / Stuart LeGrice, Matthias Gotte, editors
Publication : New York : Springer, [2013]
Description matérielle : 1 ressource dématérialisée
Note(s) : Includes bibliographical references and index
The Reverse Transcriptase (RT) of Human Immunodeficiency Virus Type 1 (HIV-1) arguably
ranks amongst one of the most extensively studied retroviral enzymes. Heterologous
expression and purification of HIV-1 RT in the early eighties, approval of the first
nucleoside analogue RT inhibitor (NRTI) in 1987, discovery of resistance to RT inhibitors,
approval of the first non-nucleoside analogue RT inhibitor (NNRTI) in 1996 and the
various crystal structures of RT with and without bound substrate(s) and/or inhibitors
represent only a few of the important milestones that describe the a bench-to-bedside
success in the continuing effort to combat HIV-1 infection and its consequences. Nucleoside
and nonnucleoside RT inhibitors remain important components in frequently used drug
regimens to treat the infection. RT inhibitors also play important roles in recently
validated strategies to prevent transmission of the virus.^ ; The relevance of HIV-1
RT as a drug target has simultaneously triggered interest in basic research studies
aimed at providing a more detailed understanding of interactions between proteins,
nucleic acids, and small molecule ligands in general terms. In light of the ever-growing
knowledge on structure and function of HIV-1 RT, this enzyme serves as a valuable
model system in efforts to develop novel experimental tools and to explain biochemical
processes. This monograph is designed to provide an overview of important aspects
in past and current HIV-1 RT research, with focus on mechanistic aspects and translation
of knowledge into drug discovery and development. The first section includes chapters
with emphasis placed on the coordination of the RT-associated DNA polymerase and ribonuclease
H (RNase H) activities.^ ; The second covers mechanisms of action and future perspectives
associated with NRTIs and NNRTIs, while the third section includes chapters focusing
on novel strategies to target the RT enzyme. Chapters of the final part are intended
to discuss mechanisms involved in HIV variability and the development of drug resistance.
We hope that these contributions will stimulate interest, and encourage research aimed
at the development of novel RT inhibitors. The lack of bona fide RNase H inhibitors
with potent antiviral activity provides an example for challenges and opportunities
in the field
Autre(s) auteur(s) : LeGrice, Stuart. Fonction indéterminée
Götte, Matthias. Fonction indéterminée
Sujet(s) : Transcriptase inverse
Identifiants, prix et caractéristiques : ISBN 9781461472919
Identifiant de la notice : ark:/12148/cb446658868
Notice n° :
FRBNF44665886
(notice reprise d'un réservoir extérieur)
Table des matières : Development of the First AIDS Drugs: AZT and Other Dideoxynueosides /Robert Yarchoan,
Hiroaki MitsuyaPart I ; Structure and Function of HIV RT. ; Proviral DNA Synthesis
in HIV: Background /Dorota Piekna-Przybylska Ph. D., Robert A. Bambara Ph. D. ; The
RNase H Domain: Structure, Function and Mechanism /Marcin Nowotny, Małgorzata Figiel
; Conformational Dynamics of Reverse Transcription /Stuart F.J. LeGricePart II ; Mechanism
of Action of Approved RT Inhibitors. ; Nucleoside RT Inhibitors: Structural and Molecular
Biology /Gaofei Lu, Antonio J. Acosta-Hoyos, Walter A. Scott ; Nonnucleoside Reverse
Transcriptase Inhibitors (NNRTIs) /Kalyan Das Ph. D., Eddy Arnold Ph. D., Stephen
H. Hughes Ph. D.Part III ; Alternative Strategies to Interfere with the Function of
HIV RT. ; Ribonuclease H Inhibitors: Structural and Molecular Biology /Jason W. Rausch
; Targeting Small Molecules and Peptides to the p66-p51 Reverse Transcriptase Interface
/Daouda Abba Moussa, Audrey Agopian, Gilles Divita ; Targe
