Abstract
Dual inhibitors are drugs able to block both the COX and the 5-LOX metabolic pathways. The interest of developing such compounds is supported by a large number of pharmacological studies. Compared to COX or LOX pathways single inhibitors, dual inhibitors present at least two major advantages. First, dual inhibitors, by acting on the two major arachidonic acid metabolic pathways, possess a wide range of antiinflammatory activity. Secondly, dual inhibitors appear to be almost exempt from gastric toxicity, which is the most troublesome side effect of COX inhibitors. The mechanism of their gastric-sparing properties is not completely understood, although it has been demonstrated that leukotrienes significantly contribute to the gastric epithelial injury. Finally, both COX and LOX derivatives (prostanoids and leukotrienes, respectively) are involved in other diseases than inflammation such as cancer proliferation where the use of dual inhibitors could be an interesting approach.
Keywords: cox inhibitors, prostanoids, leukotrienes, eicosanoids, cyclooxygenase, peroxidase, meclofenamic acid, flufenamic acid, mefenamic acid, niflumic acid
Current Medicinal Chemistry
Title: New Trends in Dual 5-LOX / COX Inhibition
Volume: 9 Issue: 9
Author(s): Xavier de Leval, Fabien Julemont, Jacques Delarge, Bernard Pirotte and Jean-Michel Dogne
Affiliation:
Keywords: cox inhibitors, prostanoids, leukotrienes, eicosanoids, cyclooxygenase, peroxidase, meclofenamic acid, flufenamic acid, mefenamic acid, niflumic acid
Abstract: Dual inhibitors are drugs able to block both the COX and the 5-LOX metabolic pathways. The interest of developing such compounds is supported by a large number of pharmacological studies. Compared to COX or LOX pathways single inhibitors, dual inhibitors present at least two major advantages. First, dual inhibitors, by acting on the two major arachidonic acid metabolic pathways, possess a wide range of antiinflammatory activity. Secondly, dual inhibitors appear to be almost exempt from gastric toxicity, which is the most troublesome side effect of COX inhibitors. The mechanism of their gastric-sparing properties is not completely understood, although it has been demonstrated that leukotrienes significantly contribute to the gastric epithelial injury. Finally, both COX and LOX derivatives (prostanoids and leukotrienes, respectively) are involved in other diseases than inflammation such as cancer proliferation where the use of dual inhibitors could be an interesting approach.
Export Options
About this article
Cite this article as:
Leval de Xavier, Julemont Fabien, Delarge Jacques, Pirotte Bernard and Dogne Jean-Michel, New Trends in Dual 5-LOX / COX Inhibition, Current Medicinal Chemistry 2002; 9 (9) . https://dx.doi.org/10.2174/0929867024606713
DOI https://dx.doi.org/10.2174/0929867024606713 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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 Pharmacologic Approach to the Prevention of Preeclampsia: From Antiplatelet, Antithrombosis and Antioxidant Therapy to Anticonvulsants
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Augmenting T Helper Cell Immunity in Cancer
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Autoimmune Diabetes Mellitus: The Importance of Autoantibodies for Disease Prediction and Diagnostic Support
Current Immunology Reviews (Discontinued) Functional Improvement of Chimeric Antigen Receptor Through Intrinsic Interleukin-15Rα Signaling
Current Gene Therapy Molecular Pathways of Endothelial Cell Activation for (Targeted) Pharmacological Intervention of Chronic Inflammatory Diseases
Current Vascular Pharmacology The Role and Potential Therapeutical Applications of Antimicrobial Proteins in Infectious and Inflammatory Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets Ischemic Colitis: Current Diagnosis and Treatment
Current Drug Targets Perspectives in Breast and Ovarian Cancer Chemotherapy by Nanomedicine Approach: Nanoformulations in Clinical Research
Current Medicinal Chemistry Neuroprotective Mechanisms as Treatment Strategy in Alzheimers disease
Current Medicinal Chemistry - Central Nervous System Agents Editorial
Current Medicinal Chemistry Triptolide Induces Cell Apoptosis by Targeting H3K4me3 and Downstream Effector Proteins in KM3 Multiple Myeloma Cells
Current Pharmaceutical Biotechnology IL-17A and Multiple Sclerosis: Signaling Pathways, Producing Cells and Target Cells in the Central Nervous System
Current Drug Targets Attenuating Muscle Wasting: Cell and Gene Therapy Approaches
Current Genomics Combat Pneumococcal Infections: Adhesins as Candidates for Protein- Based Vaccine Development
Current Drug Targets Gene Therapy of Cancer Based on Interleukin 12
Current Gene Therapy Current Therapeutic Concepts in Peripartum Cardiomyopathy
Current Pharmaceutical Design New Perspectives in the Modulation of the Eicosanoid Cascade in Inflammation
Letters in Drug Design & Discovery Response to Rituximab: Has the Original Hypothesis Been Confirmed?
Current Pharmaceutical Design Dendritic Cells and their Receptors in Antitumor Immune Response
Current Molecular Medicine Renal Endothelial Dysfunction in Acute Kidney Ischemia Reperfusion Injury
Cardiovascular & Hematological Disorders-Drug Targets