HIV-1 Reverse Transcriptase Still Remains a New Drug Target : Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions
Joint Authors
Tramontano, Enzo
Esposito, Francesca
Corona, Angela
Source
Molecular Biology International
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-23, 23 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-06-20
Country of Publication
Egypt
No. of Pages
23
Main Subjects
Natural & Life Sciences (Multidisciplinary)
Biology
Abstract EN
During the retrotranscription process, characteristic of all retroviruses, the viral ssRNA genome is converted into integration-competent dsDNA.
This process is accomplished by the virus-coded reverse transcriptase (RT) protein, which is a primary target in the current treatments for HIV-1 infection.
In particular, in the approved therapeutic regimens two classes of drugs target RT, namely, nucleoside RT inhibitors (NRTIs) and nonnucleoside RT inhibitors (NNRTIs).
Both classes inhibit the RT-associated polymerase activity: the NRTIs compete with the natural dNTP substrate and act as chain terminators, while the NNRTIs bind to an allosteric pocket and inhibit polymerization noncompetitively.
In addition to these two classes, other RT inhibitors (RTIs) that target RT by distinct mechanisms have been identified and are currently under development.
These include translocation-defective RTIs, delayed chain terminators RTIs, lethal mutagenesis RTIs, dinucleotide tetraphosphates, nucleotide-competing RTIs, pyrophosphate analogs, RT-associated RNase H function inhibitors, and dual activities inhibitors.
This paper describes the HIV-1 RT function and molecular structure, illustrates the currently approved RTIs, and focuses on the mechanisms of action of the newer classes of RTIs.
American Psychological Association (APA)
Esposito, Francesca& Corona, Angela& Tramontano, Enzo. 2012. HIV-1 Reverse Transcriptase Still Remains a New Drug Target : Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions. Molecular Biology International،Vol. 2012, no. 2012, pp.1-23.
https://search.emarefa.net/detail/BIM-482940
Modern Language Association (MLA)
Esposito, Francesca…[et al.]. HIV-1 Reverse Transcriptase Still Remains a New Drug Target : Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions. Molecular Biology International No. 2012 (2012), pp.1-23.
https://search.emarefa.net/detail/BIM-482940
American Medical Association (AMA)
Esposito, Francesca& Corona, Angela& Tramontano, Enzo. HIV-1 Reverse Transcriptase Still Remains a New Drug Target : Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions. Molecular Biology International. 2012. Vol. 2012, no. 2012, pp.1-23.
https://search.emarefa.net/detail/BIM-482940
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-482940