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 |
- 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
-
An Update on the Cardiovascular Effects of Quercetin, a Plant Flavonoid
Current Nutrition & Food Science Cardiovascular Effects of Glucagon-Like Peptide 1
Mini-Reviews in Medicinal Chemistry Selection of Potential Pharmacological Targets in ALS Based on Whole- Genome Expression Profiling
Current Medicinal Chemistry Endothelial Dysfunction: Methods of Assessment and Application to Hypertension
Current Pharmaceutical Design Complications Associated with Recombinant Tissue Plasminogen Activator Therapy for Acute Ischaemic Stroke
CNS & Neurological Disorders - Drug Targets Estrogenic Compounds, Estrogen Receptors and Vascular Cell Signaling in the Aging Blood Vessels
Current Medicinal Chemistry Histone Deacetylase Inhibitors and Neurodegenerative Disorders: Holding the Promise
Current Pharmaceutical Design Acute and Chronic Stress-Induced Disturbances of Microglial Plasticity, Phenotype and Function
Current Drug Targets Zinc-Permeable Ion Channels: Effects on Intracellular Zinc Dynamics and Potential Physiological/Pathophysiological Significance
Current Medicinal Chemistry The Phosphodiesterase III Inhibitor Cilostazol Ameliorates Ethanolinduced Endothelial Dysfunction
Current Neurovascular Research Halogenated Agents and Cardiovascular Surgery: Has Mortality Really Decreased?
Current Vascular Pharmacology Trimetazidine: Does it Actually Reduce QT Dispersion After First Acute Myocardial Infarction?
Current Drug Therapy P-selectin Cell Adhesion Molecule in Inflammation, Thrombosis, Cancer Growth and Metastasis
Current Medicinal Chemistry Rapid Profiling and Identification of Vitexin Metabolites in Rat Urine, Plasma and Faeces after Oral Administration Using a UHPLC-Q-Exactive Orbitrap Mass Spectrometer Coupled with Multiple Data-mining Methods
Current Drug Metabolism Urocortin: Cardiovascular Actions and Therapeutic Implications
Letters in Drug Design & Discovery Neuroprotective Role of Agmatine in Neurological Diseases
Current Neuropharmacology Bacterial L-Arabinose Isomerases: Industrial Application for D-Tagatose Production
Recent Patents on DNA & Gene Sequences Meet Our Editorial Board Member
Current Gene Therapy Cardiac ATP-Sensitive Potassium Channels: A Potential Target for an Anti-Ischaemic Pharmacological Strategy
Cardiovascular & Hematological Agents in Medicinal Chemistry Ameliorative Effect of Phosphodiesterase-5 Inhibitor in Rat Model of Vascular Dementia
Current Neurovascular Research