Abstract
Leukotrienes (LTs), including LTB4 and cysteinyl-LTs (CysLTs) (LTC4, LTD4, and LTE4), are potent inflammatory lipid mediators which are derived from 5 – lipoxygenase activity. CysLTs, which stimulate CysLT1 and CysLT2 receptor subtypes, are functionally involved in the pathophysiology of asthma. Selective CysLT1 receptor antagonists are effective anti-asthmatic drugs. CysLT1 receptor antagonists have been developed from leukotriene structural analogs, analogs of FPL 55712, a chromone carboxylic acid, and by random screening of corporate compound banks. This review will examine the biosynthesis, metabolism and mechanism of action of leukotrienes, their role in asthma, the therapeutic implications of the leukotriene pathway inhibition for asthma, and the medicinal chemistry strategies that have been exploited in the design of potent and selective CysLT1 receptor antagonists.
Keywords: Leukotrienes, asthma, leukotriene receptor antagonists, airway inflammation, pharmacological therapy
Mini-Reviews in Medicinal Chemistry
Title: Leukotrienes, Antileukotrienes and Asthma
Volume: 8 Issue: 7
Author(s): Paolo Montuschi
Affiliation:
Keywords: Leukotrienes, asthma, leukotriene receptor antagonists, airway inflammation, pharmacological therapy
Abstract: Leukotrienes (LTs), including LTB4 and cysteinyl-LTs (CysLTs) (LTC4, LTD4, and LTE4), are potent inflammatory lipid mediators which are derived from 5 – lipoxygenase activity. CysLTs, which stimulate CysLT1 and CysLT2 receptor subtypes, are functionally involved in the pathophysiology of asthma. Selective CysLT1 receptor antagonists are effective anti-asthmatic drugs. CysLT1 receptor antagonists have been developed from leukotriene structural analogs, analogs of FPL 55712, a chromone carboxylic acid, and by random screening of corporate compound banks. This review will examine the biosynthesis, metabolism and mechanism of action of leukotrienes, their role in asthma, the therapeutic implications of the leukotriene pathway inhibition for asthma, and the medicinal chemistry strategies that have been exploited in the design of potent and selective CysLT1 receptor antagonists.
Export Options
About this article
Cite this article as:
Montuschi Paolo, Leukotrienes, Antileukotrienes and Asthma, Mini-Reviews in Medicinal Chemistry 2008; 8 (7) . https://dx.doi.org/10.2174/138955708784567395
DOI https://dx.doi.org/10.2174/138955708784567395 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Inflammation, Hyperinflammation & Cystic Fibrosis Lung Disease – A Paradigm Shift?
Current Respiratory Medicine Reviews Novel Coronavirus SARS-CoV-2 (COVID-19) and Pregnancy: A Hypothetical View
Endocrine, Metabolic & Immune Disorders - Drug Targets Human Cognitive and Neuro-Psychiatric Bio-Markers in the Cardiac Peri-Operative Patient
Current Molecular Medicine Mechanism of Action and Potential Use of Tamoxifen in the Treatment of Acute Mania
Current Psychopharmacology Eosinophils in Cancer: Favourable or Unfavourable?
Current Medicinal Chemistry Understanding Tumor-Antigen Presentation in the New Era of Cancer Immunotherapy
Current Pharmaceutical Design The Occurrence of Bisphenol A, Phthalates, Parabens and Other Environmental Phenolic Compounds in House Dust: A Review
Current Organic Chemistry Editorial [ Hot Topic: State of the Science: Pediatric Asthma (Guest Editors: Barbara Velsor-Friedrich and Arlene Butz)]
Current Pediatric Reviews How to Keep Oxidative Stress Under Control?
Current Nutrition & Food Science Alkaloids: An Emerging Antibacterial Modality Against Methicillin Resistant Staphylococcus aureus
Current Pharmaceutical Design Airway Remodeling: Effect of Current and Future Asthma Therapies
Current Respiratory Medicine Reviews Exhaled Nitric Oxide as a Potential Biomarker of Continuous Positive Airway Pressure Therapy for Severe Obstructive Sleep Apnea Patients
Current Respiratory Medicine Reviews Antagonists of CCR4 as Immunomodulatory Agents
Current Topics in Medicinal Chemistry Sida cordifolia, a Traditional Herb in Modern Perspective – A Review
Current Traditional Medicine Avian Cytokines - An Overview
Current Pharmaceutical Design Natural Triterpenoids and their Derivatives with Pharmacological Activity Against Neurodegenerative Disorders
Mini-Reviews in Organic Chemistry Prostaglandins Pathway as a Possible Biological Link Between Cancer and Major Depression
Current Angiogenesis (Discontinued) The Medical Complications of Anorexia Nervosa and Their Treatments
Current Women`s Health Reviews Adverse Cutaneous Reactions of Systemic Antihistamines
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents An Aggressive Medical Approach for Inflammatory Bowel Disease: Clinical Challenges and Therapeutic Profiles in a Retrospective Hospitalbased Series
Current Clinical Pharmacology