Abstract
Current therapeutic strategies to inhibit the replication of human immunodeficiency virus type 1 (HIV-1) use a combination of drugs targeted at the viral reverse transcriptase, protease and integrase enzymes. The clinical advantages of this combination therapy are considerable, although the emergence of drug-resistant viral strains still presents a challenge. Import of the HIV-1 viral pre-integration complex (PIC) into the nucleus is a vital step in the process of viral replication in non-dividing cells (such as terminally differentiated macrophages). The interaction between the HIV-1 accessory protein, Vpr, and the cellular protein, importin-α, is critical for nuclear import of the PIC. Targeting the protein-protein interactions involved in the regulation of HIV-1 replication might be one way to combat the continued emergence of drug-resistant HIV-1 mutants. In this review, the current status of AIDS therapy, the mechanisms involved in the nuclear import of the PIC and the discovery of a new small molecular inhibitor of HIV-1 replication are discussed.
Keywords: HIV-1 Vpr, nuclear import, pre-integration complex (PIC), importin (Imp)- α, anti-HIV-1 therapy, small molecule inhibitor
Current Chemical Biology
Title: Discovery of a Small Molecule Inhibitor of the Interaction Between HIV-1 Proteins and Cellular Cofactors: A Novel Candidate Anti-HIV-1 Drug
Volume: 4 Issue: 3
Author(s): Guangai Xue and Yoko Aida
Affiliation:
Keywords: HIV-1 Vpr, nuclear import, pre-integration complex (PIC), importin (Imp)- α, anti-HIV-1 therapy, small molecule inhibitor
Abstract: Current therapeutic strategies to inhibit the replication of human immunodeficiency virus type 1 (HIV-1) use a combination of drugs targeted at the viral reverse transcriptase, protease and integrase enzymes. The clinical advantages of this combination therapy are considerable, although the emergence of drug-resistant viral strains still presents a challenge. Import of the HIV-1 viral pre-integration complex (PIC) into the nucleus is a vital step in the process of viral replication in non-dividing cells (such as terminally differentiated macrophages). The interaction between the HIV-1 accessory protein, Vpr, and the cellular protein, importin-α, is critical for nuclear import of the PIC. Targeting the protein-protein interactions involved in the regulation of HIV-1 replication might be one way to combat the continued emergence of drug-resistant HIV-1 mutants. In this review, the current status of AIDS therapy, the mechanisms involved in the nuclear import of the PIC and the discovery of a new small molecular inhibitor of HIV-1 replication are discussed.
Export Options
About this article
Cite this article as:
Xue Guangai and Aida Yoko, Discovery of a Small Molecule Inhibitor of the Interaction Between HIV-1 Proteins and Cellular Cofactors: A Novel Candidate Anti-HIV-1 Drug, Current Chemical Biology 2010; 4 (3) . https://dx.doi.org/10.2174/2212796811004030188
DOI https://dx.doi.org/10.2174/2212796811004030188 |
Print ISSN 2212-7968 |
Publisher Name Bentham Science Publisher |
Online ISSN 1872-3136 |
- 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
-
Potential Role of PKC Inhibitors in the Treatment of Hematological Malignancies
Current Pharmaceutical Design The PTEN/PI3K/AKT Signalling Pathway in Cancer, Therapeutic Implications
Current Cancer Drug Targets Editorial: Overview on microRNAs in Cancer Development and Virus Infection
MicroRNA Lipids as a Target for Drugs Modulating Multidrug Resistance of Cancer Cells
Current Drug Targets Growth Factors and Chemokines: A Comparative Functional Approach Between Invertebrates and Vertebrates
Current Medicinal Chemistry Development of Hedgehog Pathway Inhibitors (HPI) in Treatment of Cancer
Current Chemical Biology Cardiotonic Steroids, Hypertension and Cardiovascular Disease
Current Hypertension Reviews Supramolecular Approaches for Drug Development
Current Medicinal Chemistry Glycosyltransferases, Important Tools for Drug Design
Current Topics in Medicinal Chemistry Microscopies at the Nanoscale for Nano-Scale Drug Delivery Systems
Current Drug Targets An Overview on Fibroblast Growth Factors: Structural, Functional and Therapeutic Implications
Current Proteomics The Controlled Release of Drugs and Bioactive Compounds from Mesoporous Silica Nanoparticles
Current Drug Delivery Single-Photon Emission Computed Tomography Tracers for Predicting and Monitoring Cancer Therapy
Current Pharmaceutical Biotechnology Approaches for Developing Novel Microtubule Targeting Agents (MTAs) for Therapeutic Exploitation
Current Pharmaceutical Design Radiopharmaceutical Tracking of Particles Injected into Tumors: A Model to Study Clearance Kinetics
Current Drug Delivery Protein Tyrosine Signaling and its Potential Therapeutic Implications in Carcinogenesis
Current Pharmaceutical Design Annexin A5 Imaging: An Academic Research – Clinical Trials and Theses
Current Molecular Imaging (Discontinued) Cytoprotection and Immunomodulation in Cancer Therapy
Current Medicinal Chemistry - Anti-Cancer Agents Chromosomal Abnormalities, Cancer and Mouse Models The Critical Role of Translocation-Associated Genes in Human Cancer
Current Genomics Tubulin Colchicine Binding Site Inhibitors as Vascular Disrupting Agents in Clinical Developments
Current Medicinal Chemistry