Abstract
Since the beginning of the HIV epidemic almost 70 million people have been infected with HIV. It is estimated that 42 million people are currently living with HIV/AIDS. The spread of HIV continues throughout the world and current estimates indicate that in 2002, 5 million people were newly infected with HIV and 3 million people died. Current treatments employ a combination of therapeutic agents that target the viral reverse transcriptase and protease enzymes and viral entry. However the clinical benefit of these agents is often limited due to issues of regimen compliance, significant side effects, and the emergence of viral strains that are drug resistant. The introduction of novel agents that interfere with alternate stages in the viral life cycle represent potential solutions to these problems. The integration of the HIV genome into the cellular chromosome, a process catalyzed by the viral enzyme integrase, has been shown to be essential for viral replication. Since HIV integrase has no direct cellular counterpart it presents itself as an attractive target for therapeutic intervention. This review summarizes recent and promising developments both in the HIV integrase field and the global quest for therapeutically useful inhibitors of HIV integrase.
Keywords: hiv-1 Integrase, aids, chemotherapeutics, cellular chromosome, hiv genome
Current Topics in Medicinal Chemistry
Title: HIV-1 Integrase: A Target for New AIDS Chemotherapeutics
Volume: 4 Issue: 9
Author(s): Neville J. Anthony
Affiliation:
Keywords: hiv-1 Integrase, aids, chemotherapeutics, cellular chromosome, hiv genome
Abstract: Since the beginning of the HIV epidemic almost 70 million people have been infected with HIV. It is estimated that 42 million people are currently living with HIV/AIDS. The spread of HIV continues throughout the world and current estimates indicate that in 2002, 5 million people were newly infected with HIV and 3 million people died. Current treatments employ a combination of therapeutic agents that target the viral reverse transcriptase and protease enzymes and viral entry. However the clinical benefit of these agents is often limited due to issues of regimen compliance, significant side effects, and the emergence of viral strains that are drug resistant. The introduction of novel agents that interfere with alternate stages in the viral life cycle represent potential solutions to these problems. The integration of the HIV genome into the cellular chromosome, a process catalyzed by the viral enzyme integrase, has been shown to be essential for viral replication. Since HIV integrase has no direct cellular counterpart it presents itself as an attractive target for therapeutic intervention. This review summarizes recent and promising developments both in the HIV integrase field and the global quest for therapeutically useful inhibitors of HIV integrase.
Export Options
About this article
Cite this article as:
Anthony J. Neville, HIV-1 Integrase: A Target for New AIDS Chemotherapeutics, Current Topics in Medicinal Chemistry 2004; 4 (9) . https://dx.doi.org/10.2174/1568026043388448
DOI https://dx.doi.org/10.2174/1568026043388448 |
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
-
Porcine Epidemic Diarrhea: Causative Agent, Epidemiology, Clinical
Characteristics, and Treatment Strategy Targeting Main Protease
Protein & Peptide Letters Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity
Medicinal Chemistry Pyrrolo[1,2-a]azepines Coupled with Benzothiazole and Fluorinated Aryl Thiourea Scaffolds as Promising Antioxidant and Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Quality of Service in Wireless Sensor Networks: Imperatives and Challenges
International Journal of Sensors, Wireless Communications and Control Discovery of Potent SARS-CoV-2 Inhibitors from Approved Antiviral Drugs via Docking and Virtual Screening
Combinatorial Chemistry & High Throughput Screening Microtubule-Stabilizing Natural Products as Promising Cancer Therapeutics
Current Medicinal Chemistry Potential Implications of Angiotensin-converting Enzyme 2 Blockades on Neuroinflammation in SARS-CoV-2 Infection
Current Drug Targets Novel VEGF-independent Strategies Targeting Tumor Vasculature: Clinical Aspects
Current Pharmaceutical Design Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides
Letters in Drug Design & Discovery Design, Synthesis, <i>In Silico</i> and <i>In Vitro</i> Evaluation of Novel Pyrimidine Derivatives as EGFR Inhibitors
Anti-Cancer Agents in Medicinal Chemistry The Recent Medicinal Chemistry Development of Jak2 Tyrosine Kinase Small Molecule Inhibitors
Current Medicinal Chemistry Dual Inhibitors of β-Amyloid Aggregation and Acetylcholinesterase as Multi-Target Anti-Alzheimer Drug Candidates
Current Topics in Medicinal Chemistry Binding Modes of 2-Phenylamino-6-oxopurines to Herpes Simplex Virus Thymidine Kinases
Letters in Drug Design & Discovery Probing Multidrug Resistance P-glycoprotein Transporter Activity with SPECT Radiopharmaceuticals
Current Topics in Medicinal Chemistry Drug-Metabolizing Enzymes Mechanisms and Functions
Current Drug Metabolism Chalcone and Curcumin Derivatives: A Way Ahead for Malarial Treatment
Mini-Reviews in Medicinal Chemistry Natural Alpha-Glucosidase Inhibitors: Therapeutic Implication and Structure- Activity Relation Ship
Letters in Drug Design & Discovery HDL Elevators and Mimetics - Emerging Therapies for Atherosclerosis
Cardiovascular & Hematological Agents in Medicinal Chemistry 1,3,4-Oxadiazole Derivatives as Potential Biological Agents
Mini-Reviews in Medicinal Chemistry Hydroxychloroquine (HCQ) and its Synthetic Precursors: A Review
Mini-Reviews in Organic Chemistry