Abstract
This review will focus on the discovery and clinical development of small molecule antagonists of CCR5 for the treatment of HIV-1/AIDS, as well as for the potential treatment of inflammatory diseases. In particular, we will focus on the specific medicinal chemistry problems that were faced during the discovery of the molecules. We will also describe limited data from clinical development phases focusing on specific issues that arose during the clinical trials. Finally, we will touch on the mechanism of action of CCR5 antagonists.
Keywords: CCR5, HIV-1/AIDS, inflammatory diseases, medicinal chemistry, clinical trials, antagonists
Current Topics in Medicinal Chemistry
Title: Small Molecule Antagonists of the Chemokine Receptor CCR5
Volume: 10 Issue: 13
Author(s): Remy C. Lemoine and Jutta Wanner
Affiliation:
Keywords: CCR5, HIV-1/AIDS, inflammatory diseases, medicinal chemistry, clinical trials, antagonists
Abstract: This review will focus on the discovery and clinical development of small molecule antagonists of CCR5 for the treatment of HIV-1/AIDS, as well as for the potential treatment of inflammatory diseases. In particular, we will focus on the specific medicinal chemistry problems that were faced during the discovery of the molecules. We will also describe limited data from clinical development phases focusing on specific issues that arose during the clinical trials. Finally, we will touch on the mechanism of action of CCR5 antagonists.
Export Options
About this article
Cite this article as:
C. Lemoine Remy and Wanner Jutta, Small Molecule Antagonists of the Chemokine Receptor CCR5, Current Topics in Medicinal Chemistry 2010; 10 (13) . https://dx.doi.org/10.2174/156802610791561219
DOI https://dx.doi.org/10.2174/156802610791561219 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
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
- 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
-
Prospectives of Antihypertensive Nano-ceuticals as Alternative Therapeutics
Current Drug Targets An Update on Natural Occurrence and Biological Activity of Chromones
Current Medicinal Chemistry Bronchiolitis Obliterans Following Lung Transplantation and Stem Cell Transplantation in Pediatric Patients
Current Pediatric Reviews The ACE2-Ang-(1-7)-Mas Axis and Cardioprotection
Current Cardiology Reviews PPARγ: Potential Therapeutic Target for Ailments Beyond Diabetes and its Natural Agonism
Current Drug Targets Enzymatic Processing of <i>Omega</i> 3 Long Chain Polyunsaturated Fatty Acid Oils
Current Nutrition & Food Science The CX3C-Chemokine Fractalkine in Kidney Diseases
Mini-Reviews in Medicinal Chemistry Anti Tumor Necrosis Factor Alpha (TNFα) Therapy in Ankylosing Spondylitis - Asian Perspective
Current Rheumatology Reviews The Role of P2X Receptors in Bone Biology
Current Medicinal Chemistry What is the Role for Glycoprotein IIB/IIIA Inhibitor Use in the Catheterization Laboratory in the Current Era?
Current Vascular Pharmacology Effect of Diets with Different Lipid’s Sources On Serum and Brain Fatty Acids Profile: Experimental Model
Endocrine, Metabolic & Immune Disorders - Drug Targets Patented Small Molecules Used for Reprogramming
Recent Patents on Regenerative Medicine Parathyroid Hormone and Heart Failure: Novel Biomarker Strategy
Endocrine, Metabolic & Immune Disorders - Drug Targets Rhinovirus-Associated Wheeze During Infancy and Asthma Development
Current Respiratory Medicine Reviews Synthesis, Physico-Chemical Properties and DFT Calculations of New 2-(4- Arylpiperazine-1-yl)-1-(3-ethylbenzofuran-2-yl)ethanols As Potential Antihypertensive Agents
Current Organic Chemistry Pathophysiology of Erectile Dysfunction
Current Drug Targets Anti-Cancer, Pharmacokinetic and Biodistribution Studies of Cremophor EL Free Alternative Paclitaxel Formulation
Current Drug Safety Beta-Blockers use for Hypertension in the Elderly
Cardiovascular & Hematological Agents in Medicinal Chemistry Genetic Variations in Telomere Maintenance, with Implications on Tissue Renewal Capacity and Chronic Disease Pathologies
Current Pharmacogenomics and Personalized Medicine Aβ Monomers, Oligomers and Fibrils: Structural Features
Current Bioactive Compounds