Abstract
HIV-1 integrase is a multidomain enzyme which is required for the integration of viral DNA into the host genome. It is one of three enzymes of HIV, the others being the Reverse Transcriptase and the Protease. It is an attractive target for therapeutic drug design. The enzyme consists of three domains. The N-terminal domain has a His2Cys2 motif which chelates zinc, the core domain has the catalytic DDE motif which is required for its enzymatic activity, and the C-terminal domain has an SH3-like fold which binds DNA nonspecifically. We review the structures of various integrase fragments, the core domain with inhibitors bound, and propose a model for DNA binding.
Keywords: hiv-1 integrase, reverse transcriptase, protease, drug design
Current Topics in Medicinal Chemistry
Title: Structure and Function of HIV-1 Integrase
Volume: 4 Issue: 9
Author(s): Thang K. Chiu and David R. Davies
Affiliation:
Keywords: hiv-1 integrase, reverse transcriptase, protease, drug design
Abstract: HIV-1 integrase is a multidomain enzyme which is required for the integration of viral DNA into the host genome. It is one of three enzymes of HIV, the others being the Reverse Transcriptase and the Protease. It is an attractive target for therapeutic drug design. The enzyme consists of three domains. The N-terminal domain has a His2Cys2 motif which chelates zinc, the core domain has the catalytic DDE motif which is required for its enzymatic activity, and the C-terminal domain has an SH3-like fold which binds DNA nonspecifically. We review the structures of various integrase fragments, the core domain with inhibitors bound, and propose a model for DNA binding.
Export Options
About this article
Cite this article as:
Chiu K. Thang and Davies R. David, Structure and Function of HIV-1 Integrase, Current Topics in Medicinal Chemistry 2004; 4 (9) . https://dx.doi.org/10.2174/1568026043388547
DOI https://dx.doi.org/10.2174/1568026043388547 |
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
-
Role of Sequence Variations in <i>AhR</i> Gene Towards Modulating Smoking Induced Lung Cancer Susceptibility in North Indian Population: A Multiple Interaction Analysis
Current Genomics Thalidomide as an Immunotherapeutic Agent: The Effects on Neutrophil- Mediated Inflammation
Current Pharmaceutical Design Targeting Heat Shock Proteins 70/90 and Proteasome for Cancer Therapy
Current Medicinal Chemistry Calorie Restriction and Dietary Restriction Mimetics: A Strategy for Improving Healthy Aging and Longevity
Current Pharmaceutical Design Intracellular Signaling Pathways Modulated by Phenolic Compounds: Application for New Anti-Inflammatory Drugs Discovery
Current Medicinal Chemistry Editorial (Thematic Issue: Chemoresistance in Gynecologic Cancers)
Current Cancer Therapy Reviews B-Cell Based Gene Therapy for Inducing Tolerance
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Role of Emerging Genomics and Proteomics Technologies in Cancer Drug Target Discovery
Current Cancer Drug Targets Recent Progress in the Field of β-(1,3)-Glucans and New Applications
Mini-Reviews in Medicinal Chemistry Subject Index To Volume 9
Combinatorial Chemistry & High Throughput Screening Efficacy of Pegylated Lyposomal Anthracyclines and of Intra-Arterial Carboplatin and Doxorubicin Combined with Local Hyperthermia in a Case of Malignant Endovascular Papillary Angioendothelioma
Current Drug Delivery Subject Index to Volume 4
Current Drug Targets Mucosal T Cell Proliferation and Apoptosis in Inflammatory Bowel Disease
Current Drug Targets Cell Surface Nucleolin as a Target for Anti-Cancer Therapies
Recent Patents on Anti-Cancer Drug Discovery Disease-Modifying Therapies in Frontotemporal Lobar Degeneration
Current Medicinal Chemistry Immunotoxins Constructed with Ribosome-Inactivating Proteins and their Enhancers: A Lethal Cocktail with Tumor Specific Efficacy
Current Pharmaceutical Design Genistein Down-Regulates miR-223 Expression in Pancreatic Cancer Cells
Current Drug Targets FDG-PET/CT Radiomics Models for The Early Prediction of Locoregional Recurrence in Head and Neck Cancer
Current Medical Imaging Molecular Dynamics and Structural Studies of the Ets Domain-DNA Complexes
Current Bioinformatics Mast Cells as Targets of Pimecrolimus
Current Pharmaceutical Design