Abstract
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by the viral-coded reverse transcriptase (RT), which has two associated functions: the RNA- and DNA-dependent DNA polymerase (RDDP and DDDP) function and the ribonuclease H (RNase H) function. The RNase H function catalyzes the selective hydrolysis of the RNA strand of the RNA:DNA heteroduplex replication intermediate. The RT associated activities are both essential for HIV-1 replication and validated targets for drug development, but only the polymerase function has been widely investigated as drug target. In fact, either nucleoside or non-nucleoside RT inhibitors currently used in therapy act on the polymerase associated activity. In this review, we describe the compounds, reported up to today, which inhibit the HIV-1 RNase H function, their chemical structures, the structure-activity relationships and the mechanism of action.
Keywords: HIV-1, reverse transcriptase, ribonuclease H, RNase H, RNase H inhibitor, natural compounds, diketo acids, hydrazones
Current Medicinal Chemistry
Title: HIV-1 RT-Associated RNase H Function Inhibitors: Recent Advances in Drug Development
Volume: 17 Issue: 26
Author(s): E. Tramontano and R. Di Santo
Affiliation:
Keywords: HIV-1, reverse transcriptase, ribonuclease H, RNase H, RNase H inhibitor, natural compounds, diketo acids, hydrazones
Abstract: The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by the viral-coded reverse transcriptase (RT), which has two associated functions: the RNA- and DNA-dependent DNA polymerase (RDDP and DDDP) function and the ribonuclease H (RNase H) function. The RNase H function catalyzes the selective hydrolysis of the RNA strand of the RNA:DNA heteroduplex replication intermediate. The RT associated activities are both essential for HIV-1 replication and validated targets for drug development, but only the polymerase function has been widely investigated as drug target. In fact, either nucleoside or non-nucleoside RT inhibitors currently used in therapy act on the polymerase associated activity. In this review, we describe the compounds, reported up to today, which inhibit the HIV-1 RNase H function, their chemical structures, the structure-activity relationships and the mechanism of action.
Export Options
About this article
Cite this article as:
Tramontano E. and Di Santo R., HIV-1 RT-Associated RNase H Function Inhibitors: Recent Advances in Drug Development, Current Medicinal Chemistry 2010; 17 (26) . https://dx.doi.org/10.2174/092986710792065045
DOI https://dx.doi.org/10.2174/092986710792065045 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
A Review on Screening Models for Potential Therapeutic Candidates and Targets Against SARS-CoV-2
Current Drug Targets Computational Evaluation and In Vitro Validation of New Epidermal Growth Factor Receptor Inhibitors
Current Topics in Medicinal Chemistry Pyrazolopyrimidine Derivatives as Antineoplastic Agents: with a Special Focus on Thyroid Cancer
Mini-Reviews in Medicinal Chemistry Synthesis and Anti-HIV Evaluation of Novel 1,2,4-triazole Derivatives as Potential Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors
Letters in Drug Design & Discovery Clinical Pattern and Causality Assessment of Drug-induced Cutaneous Reactions in a Tertiary Care Hospital in India: A Prospective Study
Current Drug Safety Innovative In Silico Approaches to Address Avian Flu Using Grid Technology
Infectious Disorders - Drug Targets Target Validation: Linking Target and Chemical Properties to Desired Product Profile
Current Topics in Medicinal Chemistry Oxidative Stress and Antioxidant Potential of One Hundred Medicinal Plants
Current Topics in Medicinal Chemistry Synthesis and <i>In Vitro</i> anti-HCV and Antitumor Evaluation of Schisandronic Acid Derivatives
Medicinal Chemistry Targeting Inhibition of COX-2: A Review of Patents, 2002 - 2006
Recent Patents on Inflammation & Allergy Drug Discovery The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis
Mini-Reviews in Medicinal Chemistry Fragmental Methods in the Analysis of Biological Activities of Diverse Compound Sets
Mini-Reviews in Medicinal Chemistry Broadening Our View of Protective Antibody Responses Against HIV
Current HIV Research Aspirin Intolerance: Experimental Models for Bed-to-Bench
Current Drug Targets The Role of Nanoparticles as Nanocarriers for the Controlled Release of some Potential Existing Antiviral Drugs for SARS-CoV-2 Management: A Review
Coronaviruses Synthesis and Antitumour Activity of the Primin (2-methoxy-6-n-pentyl-1,4-benzoquinone) and Analogues
Medicinal Chemistry Cerebral Malaria - A Neurovascular Pathology with Many Riddles Still to be Solved
Current Neurovascular Research Codon Usage Biases in Alzheimers Disease and Other Neurodegenerative Diseases
Protein & Peptide Letters The Chemical Structure and Bioactivity of Cycloartane-type Compounds
Current Organic Chemistry Exploring Pharmacological Significance of Chalcone Scaffold: A Review
Current Medicinal Chemistry