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
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
-
Pharmacological Strategies to Contend Against Myocardial Reperfusion Damage: Diverse Chemicals for Multiple Targets
Current Medicinal Chemistry Editorial: Recent Advances of Cell and Gene Therapy in Kidney Diseases
Current Gene Therapy Alternative Approach for Mitigation of Doxorubicin-Induced Cardiotoxicity using Herbal Agents
Current Clinical Pharmacology MiR-29 Targets PUMA to Suppress Oxygen and Glucose Deprivation/Reperfusion (OGD/R)-induced Cell Death in Hippocampal Neurons
Current Neurovascular Research Melatonin Alleviates Pyroptosis of Retinal Neurons Following Acute Intraocular Hypertension
CNS & Neurological Disorders - Drug Targets Signal Transduction Pathways and Transcription Factors as Therapeutic Targets in Inflammatory Disease: Towards Innovative Antirheumatic Therapy
Current Pharmaceutical Design Cellular Therapy of Lysosomal Storage Disorders: Current Status and Future Prospects
Current Pediatric Reviews Cardiac (myo)fibroblast: Novel Strategies for its Targeting Following Myocardial Infarction
Current Pharmaceutical Design New Proposals for Treatment Sporadic Alzheimers Disease
Central Nervous System Agents in Medicinal Chemistry Complex Inheritance for Susceptibility to Sudden Cardiac Death
Current Pharmaceutical Design Role of Cannabinoids and Endocannabinoids in Cerebral Ischemia
Current Pharmaceutical Design Roles of Arterial Baroreceptor Reflex During Bezold-Jarisch Reflex
Current Cardiology Reviews Current Understanding of HSP90 as a Novel Therapeutic Target: An Emerging Approach for the Treatment of Cancer
Current Pharmaceutical Design Editorial (No-reflow After Primary Coronary Interventions: How to Prevent and How to Treat it?)
Current Vascular Pharmacology Clinical Applicability of Conditioning Techniques in Ischemia-Reperfusion Injury: A Review of the Literature
Current Cardiology Reviews Early Pathogenesis of Atherosclerosis: The Childhood Obesity
Current Pharmaceutical Design Neuroprotection by NMDA Receptor Antagonists in a Variety of Neuropathologies
Current Drug Targets Advances in Inhibitors of FXa
Current Drug Targets Novel Imaging Techniques in Acute Kidney Injury
Current Drug Targets Inhibitors of Nitrogen Oxide Species Production in Animal Models of Inflammation and Future Directions for Therapy in Inflammatory Disorders
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents