Abstract
In the past eight years, numerous series of small molecule CXCR2 and CXCR1 antagonists have been disclosed. These compounds have proved to be effective inhibitors of ELR+ chemokine-induced chemotaxis of neutrophils and other immune cells in vitro and have also been efficacious in several animal models of inflammatory disease. Although some of these compounds have been reported to be in clinical development, no data on clinical studies in patients with inflammatory disease has been revealed to date. This review details the medicinal chemistry and pharmacology of the aforementioned antagonist series.
Keywords: CXCR2, CXCR1, IL-8, GRO', neutrophil (PMN), chemotaxis, small molecule antagonist
Current Topics in Medicinal Chemistry
Title: Small Molecule Antagonists of the CXCR2 and CXCR1 Chemokine Receptors as Therapeutic Agents for the Treatment of Inflammatory Diseases
Volume: 6 Issue: 13
Author(s): Jakob Busch-Petersen
Affiliation:
Keywords: CXCR2, CXCR1, IL-8, GRO', neutrophil (PMN), chemotaxis, small molecule antagonist
Abstract: In the past eight years, numerous series of small molecule CXCR2 and CXCR1 antagonists have been disclosed. These compounds have proved to be effective inhibitors of ELR+ chemokine-induced chemotaxis of neutrophils and other immune cells in vitro and have also been efficacious in several animal models of inflammatory disease. Although some of these compounds have been reported to be in clinical development, no data on clinical studies in patients with inflammatory disease has been revealed to date. This review details the medicinal chemistry and pharmacology of the aforementioned antagonist series.
Export Options
About this article
Cite this article as:
Busch-Petersen Jakob, Small Molecule Antagonists of the CXCR2 and CXCR1 Chemokine Receptors as Therapeutic Agents for the Treatment of Inflammatory Diseases, Current Topics in Medicinal Chemistry 2006; 6 (13) . https://dx.doi.org/10.2174/15680266106061345
DOI https://dx.doi.org/10.2174/15680266106061345 |
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
![](/images/wayfinder.jpg)
- 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
-
The Role of Toll-Like Receptors in Chronic Fatigue Syndrome/Myalgic Encephalomyelitis: A New Promising Therapeutic Approach?
CNS & Neurological Disorders - Drug Targets Mechanisms of Control of Neuron Survival by the Endocannabinoid System
Current Pharmaceutical Design Pleiotropic Effects of Nicotinic Acid: Beyond High Density Lipoprotein Cholesterol Elevation
Current Vascular Pharmacology Brain Injury Associated with Widely Abused Amphetamines: Neuroinflammation, Neurogenesis and Blood-Brain Barrier
Current Drug Abuse Reviews The Role of Oxidative Stress in Huntington’s Disease: Are Antioxidants Good Therapeutic Candidates?
Current Drug Targets Role of Thrombin Activatable Fibrinolysis Inhibitor in Endocrine and Cardiovascular Disorders
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Protease Inhibitors in the Clinic
Medicinal Chemistry Minocycline and Doxycycline: More Than Antibiotics
Current Molecular Pharmacology BK Channel Modulators: A Comprehensive Overview
Current Medicinal Chemistry Fish Oil Prevents Oxidative Stress and Exerts Sustained Antiamnesic Effect After Global Cerebral Ischemia
CNS & Neurological Disorders - Drug Targets The Importance of Humanized Yeast to Better Understand the Role of Bcl-2 Family in Apoptosis: Finding of Novel Therapeutic Opportunities
Current Pharmaceutical Design Flavonoid Enriched Fraction of Campylandra aurantiaca Attenuates Carbon Tetrachloride Induced Oxidative DNA Damage in Mouse Peritoneal Macrophages in Animal Model
Current Drug Discovery Technologies Natural Phenolic Compounds as Cardiovascular Therapeutics: Potential Role of their Antiinflammatory Effects
Current Vascular Pharmacology The Neurovascular Protection Afforded by Delayed Local Hypothermia after Transient Middle Cerebral Artery Occlusion
Current Neurovascular Research Multivalent & Multifunctional Ligands to β-Amyloid
Current Pharmaceutical Design Structure and Function of Myelinated Nerve Fibers in the Rabbit Eye Following Ischemia/Reperfusion Injury
Current Neurovascular Research Insight to the Pathophysiology of Stable Angina Pectoris
Current Pharmaceutical Design Meet Our Editorial Board Member
Current Chemical Biology Vascular Toxicity of Chemotherapeutic Agents
Current Vascular Pharmacology The Design and Development of Deferiprone (L1) and Other Iron Chelators for Clinical Use: Targeting Methods and Application Prospects
Current Medicinal Chemistry