Abstract
It wasnt until 1990, when the existence of two different cyclooxygenases was hypothesized, based on the evidence that steroids inhibited the increase in COX activity induced by bacterial lipopolysaccharides in macrophages, without any effects on the basal production of prostaglandins or leukotrienes. The first isoform, COX-1 is responsible for the production of “housekeeping” prostaglandins critical to the maintenance of normal renal function, gastric mucosal integrity, platelet aggregation, and the autocrine response to circulating hormones. COX-2 on the other hand is an inducible enzyme, upregulated 20-fold in macrophages, monocytes, synoviocytes, chondrocytes, fibroblasts, osteoblasts and endothelial cells by various inflammatory stimuli and cytochines. Classical findings shown that the therapeutics effects of NSAIDs are largely dependent on COX-2 inhibition, whereas some undesirable side effects are bound to COX- 1 blockade, such as gastrointestinal bleeding and renal failure. Therefore, agents that selectively inhibit COX-2 over COX-1 are desirable for the treatment of inflammation. However, since September 2004 reports of increased risk of thrombotic cardiovascular events had accumulated for coxibs, the COX-2 inhibitors. Our goal is to provide an overview of the relevant biology and pharmacology of this enzyme in atherosclerosis.
Keywords: atherosclerosis, COX-2 expression, 765GG genotype, PGE2, Nonsteroidal Anti-inflammatory drugs
Current Pharmaceutical Design
Title: COX-2: Friend or Foe?
Volume: 13 Issue: 16
Author(s): Annalisa Iezzi, Claudio Ferri, Andrea Mezzetti and Francesco Cipollone
Affiliation:
Keywords: atherosclerosis, COX-2 expression, 765GG genotype, PGE2, Nonsteroidal Anti-inflammatory drugs
Abstract: It wasnt until 1990, when the existence of two different cyclooxygenases was hypothesized, based on the evidence that steroids inhibited the increase in COX activity induced by bacterial lipopolysaccharides in macrophages, without any effects on the basal production of prostaglandins or leukotrienes. The first isoform, COX-1 is responsible for the production of “housekeeping” prostaglandins critical to the maintenance of normal renal function, gastric mucosal integrity, platelet aggregation, and the autocrine response to circulating hormones. COX-2 on the other hand is an inducible enzyme, upregulated 20-fold in macrophages, monocytes, synoviocytes, chondrocytes, fibroblasts, osteoblasts and endothelial cells by various inflammatory stimuli and cytochines. Classical findings shown that the therapeutics effects of NSAIDs are largely dependent on COX-2 inhibition, whereas some undesirable side effects are bound to COX- 1 blockade, such as gastrointestinal bleeding and renal failure. Therefore, agents that selectively inhibit COX-2 over COX-1 are desirable for the treatment of inflammation. However, since September 2004 reports of increased risk of thrombotic cardiovascular events had accumulated for coxibs, the COX-2 inhibitors. Our goal is to provide an overview of the relevant biology and pharmacology of this enzyme in atherosclerosis.
Export Options
About this article
Cite this article as:
Iezzi Annalisa, Ferri Claudio, Mezzetti Andrea and Cipollone Francesco, COX-2: Friend or Foe?, Current Pharmaceutical Design 2007; 13 (16) . https://dx.doi.org/10.2174/138161207780831293
DOI https://dx.doi.org/10.2174/138161207780831293 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Use of Mesenchymal Stem Cells in Crohn's Disease and Perianal Fistulas:
A Narrative Review
Current Stem Cell Research & Therapy Targeting Small Arteries of Hypertensive Status with Novel ATP-Sensitive Potassium Channel Openers&#
Current Vascular Pharmacology Pulmonary Disease in Beta-Thalassemia
Current Respiratory Medicine Reviews The Efficacy and Safety of Cilnidipine on Mild to Moderate Essential Hypertension: A Systematic Review and Meta-analysis of Randomized Controlled Trials in Chinese Patients
Cardiovascular & Hematological Disorders-Drug Targets Spectrum of Radiopharmaceuticals in Nuclear Oncology
Current Cancer Drug Targets Apoptosis and Oxidative Stress-Related Diseases: The p66Shc Connection
Current Molecular Medicine Cardiovascular Complications of HIV Infection and Treatment
Cardiovascular & Hematological Agents in Medicinal Chemistry Reprogrammed Metabolism of Cancer Cells as a Potential Therapeutic Target
Current Pharmaceutical Design SGLT-2 Inhibition: Novel Therapeutics for Reno-and Cardioprotection in Diabetes Mellitus
Current Diabetes Reviews An NMR Metabolomic Study in the Old Order Amish to Study Increased Dietary Salt Associated with Elevation of Organic Osmolytes Detected in Urine
Current Metabolomics Editorial (Thematic Issue: Endocrine Disorders and Cognitive Function in the Elderly)
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery microRNAs as Anti-Cancer Therapy
Current Pharmaceutical Design Remote Control of Pulmonary Blood Flow
Current Cardiology Reviews Yoga can Alter the Autonomic Neural Activity: A Critical Analysis
Current Traditional Medicine Fragmented ECG as a Risk Marker in Cardiovascular Diseases
Current Cardiology Reviews Effect of Chronic Melatonin Administration on Several Physiological Parameters from Old Wistar Rats and Samp8 Mice
Current Aging Science Clinical Pharmacotherapy for Obesity: Current Drugs and Those in Advanced Development
Current Drug Targets Guide of Hypertensive Crisis Pharmacotherapy
Cardiovascular & Hematological Disorders-Drug Targets Editorial [Hot Topic: Cardiac Cell Therapy: anno 2011 (Executive Guest Editor: Sophie Van Linthout)
Current Pharmaceutical Design Drug Metabolism and Pharmacokinetics of Dammarane Triterpenoids
Current Drug Metabolism