Abstract
Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority. The ribonuclease H (RNase H) activity of the HIV-1 reverse transcriptase catalyzes the selective hydrolysis of the RNA strand of RNA:DNA heteroduplex replication intermediates, and represents an attractive unexploited target for drug development. This review reports on recent progress in the characterization of HIV-1 RNase H inhibitors from 2013 to 2016, describing their chemical structures, structureactivity relationship and binding modes. Focus is given to emerging medicinal chemistry principles and insights into the discovery and development of RNase H inhibitors.
Keywords: AIDS, HIV-1, RNase H inhibitors, dual inhibitors, drug design, SAR, antiviral, metalloenzyme.
Current Medicinal Chemistry
Title:Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges
Volume: 25 Issue: 14
Author(s): Xueshun Wang, Ping Gao, Luis Menendez-Arias, Xinyong Liu*Peng Zhan*
Affiliation:
- Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong,China
- Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong,China
Keywords: AIDS, HIV-1, RNase H inhibitors, dual inhibitors, drug design, SAR, antiviral, metalloenzyme.
Abstract: Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority. The ribonuclease H (RNase H) activity of the HIV-1 reverse transcriptase catalyzes the selective hydrolysis of the RNA strand of RNA:DNA heteroduplex replication intermediates, and represents an attractive unexploited target for drug development. This review reports on recent progress in the characterization of HIV-1 RNase H inhibitors from 2013 to 2016, describing their chemical structures, structureactivity relationship and binding modes. Focus is given to emerging medicinal chemistry principles and insights into the discovery and development of RNase H inhibitors.
Export Options
About this article
Cite this article as:
Wang Xueshun, Gao Ping, Menendez-Arias Luis, Liu Xinyong*, Zhan Peng*, Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges, Current Medicinal Chemistry 2018; 25 (14) . https://dx.doi.org/10.2174/0929867324666170113110839
DOI https://dx.doi.org/10.2174/0929867324666170113110839 |
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
-
Synthesis and Biological Evaluation of Potent Antifungal Agents
Current Topics in Medicinal Chemistry Recent Patents Relating To HCV Molecules Like Putative Targets For Therapeutic Intervention
Recent Patents on DNA & Gene Sequences Innovative Ingredients Fortified Nutrients Enriched Biscuits and Cookies: Quality and Sensory Analyses
Current Nutrition & Food Science Novel Benzo[d]imidazole-based Heterocycles as Broad Spectrum Anti-viral Agents: Design, Synthesis and Exploration of Molecular Basis of Action
Mini-Reviews in Medicinal Chemistry The Prediction of Carcinogenicity from Molecular Structure
Current Computer-Aided Drug Design Metal Complexes, their Cellular Targets and Potential for Cancer Therapy
Current Pharmaceutical Design The Histopathology of Spondyloarthropathy
Current Molecular Medicine Ventilation During Pediatric CPR
Current Pediatric Reviews The Role of Apoptosis in Influenza Virus Pathogenesis and the Mechanisms Involved in Anti-Influenza Therapies
Current Chemical Biology Using A Sociological Model to Analyze Access to Pediatric HIV/AIDS Care in Rural Sub-Saharan Africas
Current HIV Research Tumor Homing Peptides as Molecular Probes for Cancer Therapeutics, Diagnostics and Theranostics
Current Medicinal Chemistry A Novel Treatment Strategy for Sepsis and Septic Shock Based on the Interactions between Prostanoids, Nitric Oxide, and 20-Hydroxyeicosatetraenoic Acid
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Anti-Inflammatory and Anti-Allergy Drugs in Rhinosinusitis
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Role of Moving Average Analysis for Development of Multi-Target (Q)SAR Models
Mini-Reviews in Medicinal Chemistry The Effect of Synthetic Curcumin Analogues on Obesity, Diabetes and Cardiovascular Disease: A Literature Review
Current Medicinal Chemistry COVID-19: An Insight on the Third Respiratory Global Emergency of the Century
Coronaviruses subject Index To Volume 1
Current Drug Targets - CNS & Neurological Disorders Evidence-Based Review of Physiologic Effects of Kangaroo Care
Current Women`s Health Reviews Organic Antifungal Drugs and Targets of Their Action
Current Topics in Medicinal Chemistry Anti-Inflammatory and Antioxidant Properties of a New Arylidene-Thiazolidinedione in Macrophages
Current Medicinal Chemistry