Abstract
The human immunodeficiency virus (HIV) causes acquired immumodeficiency syndrome (AIDS), one of the worst global pandemic. The virus infects human CD4 T cells and macrophages, and causes CD4 depletion. HIV enters target cells through the binding of the viral envelope glycoprotein to CD4 and the chemokine coreceptor, CXCR4 or CCR5. In particular, the CCR5-utilizing viruses predominate in the blood during the disease course. CCR5 is expressed on the surface of various immune cells including macrophages, monocytes, microglia, dendric cells, and active memory CD4 T cells. In the human population, the CCR5 genomic mutation, CCR5Δ32, is associated with relative resistance to HIV. These findings paved the way for the discovery and development of CCR5 inhibitors to block HIV transmission and replication. Maraviroc, discovered as a CCR5 antagonist, is the only CCR5 inhibitor that has been approved by both US FDA and the European Medicines Agency (EMA) for treating HIV/AIDS patients. In this review, we summarize the medicinal chemistry and clinical studies of Maraviroc.
Keywords: Antiretroviral therapy, clinical study, HIV-1, HIV-2, medicinal chemistry, microbicide, SAR.
Current Topics in Medicinal Chemistry
Title:Chemokine Receptor CCR5 Antagonist Maraviroc: Medicinal Chemistry and Clinical Applications
Volume: 14 Issue: 13
Author(s): Guoyan G. Xu, Jia Guo and Yuntao Wu
Affiliation:
Keywords: Antiretroviral therapy, clinical study, HIV-1, HIV-2, medicinal chemistry, microbicide, SAR.
Abstract: The human immunodeficiency virus (HIV) causes acquired immumodeficiency syndrome (AIDS), one of the worst global pandemic. The virus infects human CD4 T cells and macrophages, and causes CD4 depletion. HIV enters target cells through the binding of the viral envelope glycoprotein to CD4 and the chemokine coreceptor, CXCR4 or CCR5. In particular, the CCR5-utilizing viruses predominate in the blood during the disease course. CCR5 is expressed on the surface of various immune cells including macrophages, monocytes, microglia, dendric cells, and active memory CD4 T cells. In the human population, the CCR5 genomic mutation, CCR5Δ32, is associated with relative resistance to HIV. These findings paved the way for the discovery and development of CCR5 inhibitors to block HIV transmission and replication. Maraviroc, discovered as a CCR5 antagonist, is the only CCR5 inhibitor that has been approved by both US FDA and the European Medicines Agency (EMA) for treating HIV/AIDS patients. In this review, we summarize the medicinal chemistry and clinical studies of Maraviroc.
Export Options
About this article
Cite this article as:
Xu G. Guoyan, Guo Jia and Wu Yuntao, Chemokine Receptor CCR5 Antagonist Maraviroc: Medicinal Chemistry and Clinical Applications, Current Topics in Medicinal Chemistry 2014; 14 (13) . https://dx.doi.org/10.2174/1568026614666140827143745
DOI https://dx.doi.org/10.2174/1568026614666140827143745 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
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
- 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
-
Allopurinol Hypersensitivity Reactions: Desensitization Strategies and New Therapeutic Alternative Molecules
Inflammation & Allergy - Drug Targets (Discontinued) The Role of Biologically Active Ingredients from Chinese Herbal Medicines in the Regulation of Autophagy in Treating Cardiovascular Diseases and Other Chronic Diseases
Current Pharmaceutical Design Texture Spectrum Coupled with Entropy and Homogeneity Image Features for Myocardium Muscle Characterization
Current Bioinformatics Pathogenesis and Clinical Features of Obesity and Insulin Resistance
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) It’s Time for An Epigenomics Roadmap of Heart Failure
Current Genomics Value of Carnitine Therapy in Kidney Dialysis Patients and Effects on Cardiac Function from Human and Animal Studies
Current Drug Targets NAD+, Sirtuins, and Cardiovascular Disease
Current Pharmaceutical Design Cardiac Autonomic Nervous System in Heart Failure: Imaging Technique and Clinical Implications
Current Cardiology Reviews Targeting Cardiac Mast Cells: Pharmacological Modulation of the Local Renin-Angiotensin System
Current Pharmaceutical Design Inflammatory Mechanisms in Atherosclerosis: The Impact of Matrix Metalloproteinases
Current Topics in Medicinal Chemistry Metformin and Anti-Cancer Therapeutics: Hopes for a More Enhanced Armamentarium Against Human Neoplasias?
Current Medicinal Chemistry Occurrence and Clinical Impact of Microembolic Signals (MES) in Patients with Chronic Cardiac Diseases and Atheroaortic Plaques - A Systematic Review
Current Vascular Pharmacology Angiogenesis as a therapeutic target in breast cancer
Mini-Reviews in Medicinal Chemistry Matrix Metallopropteinases in Heart Failure
Current Topics in Medicinal Chemistry Fluoride Interactions: From Molecules to Disease
Current Signal Transduction Therapy Induction and Escalation Therapies in Multiple Sclerosis
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Postoperative Atrial Fibrillation - What Do We Really Know?
Current Vascular Pharmacology Aldosterone, From (Patho)Physiology to Treatment in Cardiovascular and Renal Damage
Current Vascular Pharmacology Non-Alcoholic Steatohepatitis: What Can We Learn from Animal Models?
Current Medicinal Chemistry Editorial: Perioperative Pharmacological Management: From Prescription Medications to Dietary Supplements
Current Clinical Pharmacology