Abstract
Integrase (IN) is the newest validated target against AIDS and retroviral infections. The remarkable activity of raltegravir (Isentress®) led to its rapid approval by the FDA in 2007 as the first IN inhibitor. Several other IN strand transfer inhibitors (STIs) are in development with the primary goal to overcome resistance due to the rapid occurrence of IN mutations in raltegravir-treated patients. Thus, many scientists and drug companies are actively pursuing clinically useful IN inhibitors. The objective of this review is to provide an update on the IN inhibitors reported in the last two years, including second generation STI, recently developed hydroxylated aromatics, natural products, peptide, antibody and oligonucleotide inhibitors. Additionally, the targeting of IN cofactors such as LEDGF and Vpr will be discussed as novel strategies for the treatment of AIDS.
Keywords: HIV-1 IN, diketo acids, HIV inhibitors, AIDS, IN inhibitors, peptides, oligonucleotides
Current Topics in Medicinal Chemistry
Title: HIV-1 IN Inhibitors: 2010 Update and Perspectives
Volume: 9 Issue: 11
Author(s): Christophe Marchand, Kasthuraiah Maddali, Mathieu Metifiot and Yves Pommier
Affiliation:
Keywords: HIV-1 IN, diketo acids, HIV inhibitors, AIDS, IN inhibitors, peptides, oligonucleotides
Abstract: Integrase (IN) is the newest validated target against AIDS and retroviral infections. The remarkable activity of raltegravir (Isentress®) led to its rapid approval by the FDA in 2007 as the first IN inhibitor. Several other IN strand transfer inhibitors (STIs) are in development with the primary goal to overcome resistance due to the rapid occurrence of IN mutations in raltegravir-treated patients. Thus, many scientists and drug companies are actively pursuing clinically useful IN inhibitors. The objective of this review is to provide an update on the IN inhibitors reported in the last two years, including second generation STI, recently developed hydroxylated aromatics, natural products, peptide, antibody and oligonucleotide inhibitors. Additionally, the targeting of IN cofactors such as LEDGF and Vpr will be discussed as novel strategies for the treatment of AIDS.
Export Options
About this article
Cite this article as:
Marchand Christophe, Maddali Kasthuraiah, Metifiot Mathieu and Pommier Yves, HIV-1 IN Inhibitors: 2010 Update and Perspectives, Current Topics in Medicinal Chemistry 2009; 9 (11) . https://dx.doi.org/10.2174/156802609789630910
DOI https://dx.doi.org/10.2174/156802609789630910 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Nanoemulsions for Skin Targeting: Present Status and Future Prospects
Drug Delivery Letters Plants vs. Cancer: A Review on Natural Phytochemicals in Preventing and Treating Cancers and Their Druggability
Anti-Cancer Agents in Medicinal Chemistry Evolution and Pathogenesis of Oncoviruses Associated with Head and Neck Cancer: History and Current Concepts
Recent Patents on Biomarkers Skin Cancers in Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry Novel Molecular-Targeted Therapeutics for the Treatment of Cancer
Anti-Cancer Agents in Medicinal Chemistry Infection, Stem Cells and Cancer Signals
Current Pharmaceutical Biotechnology Multi-Target Inhibitors for Proteins Associated with Alzheimer: In Silico Discovery using Fragment-Based Descriptors
Current Alzheimer Research New Perspectives in the Treatment of Melanoma: Anti-Angiogenic and Anti-Lymphangiogenic Strategies
Recent Patents on Anti-Cancer Drug Discovery The Use of Anthracyclines for Therapy of CNS Tumors
Anti-Cancer Agents in Medicinal Chemistry Editorial [Hot Topic:New Research Tolls for Antique Pediatric Tumors:The Dilemma of Transposing Drug-Resistance (Guest Editor: E.T. Valera)]
Current Pharmaceutical Biotechnology Targeting the Fibroblast Growth Factor Receptors for the Treatment of Cancer
Anti-Cancer Agents in Medicinal Chemistry The Beneficial Role of Vitamin D in Human Immunodeficiency Virus Infection
Current HIV Research Subject Index To Volume 9
Combinatorial Chemistry & High Throughput Screening BRAF Inhibitor Therapy for Melanoma, Thyroid and Colorectal Cancers: Development of Resistance and Future Prospects
Current Cancer Drug Targets Anti-Neoplastic Activity of 1,3-Diaza-2-Functionalized-Adamantan-6-One Compounds Against Melanoma Cells
Medicinal Chemistry Molecular and Cellular Activities of Vitamin E Analogues
Mini-Reviews in Medicinal Chemistry Effect of HAART on Salivary Composition and Oxidative Profile in HIVInfected Patients
Current HIV Research Accessing the Blood-Brain Barrier to Treat Brain Disorders
Current Nanomedicine Drug-Related Cardiotoxicity for the Treatment of Haematological Malignancies in Elderly
Current Pharmaceutical Design Antineoplastic Potential of Medicinal Plants
Recent Patents on Biotechnology