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Related Concept Videos

Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

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Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
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Drugs Used in Lower Respiratory Disorders: Overview01:17

Drugs Used in Lower Respiratory Disorders: Overview

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Lower respiratory tract disorders present challenges that often require skilled and nuanced approaches for effective management. Common ailments, such as asthma and chronic obstructive pulmonary disease (COPD), have prompted the development of intricate treatment strategies involving bronchodilators and anti-inflammatory drugs, each tailored to ease breathing and revitalize the lungs.
Bronchodilators, the first step of respiration enhancement, come in various forms, each with its own mechanism...
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Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs01:25

Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs

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Asthma is a chronic respiratory condition for which new therapeutic avenues, including anti-inflammatory drugs like mast cell stabilizers and anti-IgE treatments, continue to be developed.
Mast cell stabilizers, such as cromolyn (also known as sodium cromoglycate) and nedocromil (Tilade), are effective drugs in asthma management. These stabilizers hinder histamine release by skillfully obstructing the activation of mast cells and other cellular entities. Notably, they navigate this task without...
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Antiasthma Drugs: β2-Adrenoceptor Agonists01:25

Antiasthma Drugs: β2-Adrenoceptor Agonists

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Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce...
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Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids01:25

Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids

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Inhaled corticosteroids (ICS) are anti-inflammatory drugs used primarily in treating persistent asthma and providing long-term maintenance. They target the bronchial mucosa, the lining of the airways, to control inflammation, a critical factor in asthma progression and exacerbation.
ICS work through a multifaceted mechanism of action. They suppress the inflammatory response caused by the proliferation of TH cells. They also reduce the transcription of the IL-2 gene, which is involved in the...
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Asthma I: Introduction01:28

Asthma I: Introduction

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Asthma is a chronic inflammatory disorder of the airways characterized by variable airflow obstruction and heightened bronchial responsiveness to a wide range of triggers. The underlying inflammation leads to airway swelling, mucus hypersecretion, and smooth muscle constriction, all of which narrow the airway lumen and impede airflow. Clinically, asthma presents with recurrent episodes of wheezing, shortness of breath, chest tightness, and coughing, symptoms that typically vary in intensity and...
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Related Experiment Video

Updated: May 5, 2026

Real-time Imaging of Leukotriene B4 Mediated Cell Migration and BLT1 Interactions with β-arrestin
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Real-time Imaging of Leukotriene B4 Mediated Cell Migration and BLT1 Interactions with β-arrestin

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Leukotriene biosynthesis inhibitors.

J R Cashman1

  • 1Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco, California, 94143.

Pharmaceutical Research
|November 26, 2013
PubMed
Summary

This review covers novel anti-inflammatory drugs, specifically leukotriene biosynthesis inhibitors. Researchers are developing these inhibitors by targeting the 5-lipoxygenase enzyme, a key player in inflammation.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Leukotrienes are key mediators in inflammatory processes.
  • The 5-lipoxygenase (5-LO) enzyme catalyzes a critical step in leukotriene biosynthesis.
  • Developing effective anti-inflammatory agents requires targeting specific pathways like leukotriene synthesis.

Purpose of the Study:

  • To review the design and development of leukotriene biosynthesis inhibitors.
  • To explore the potential of targeting the 5-lipoxygenase enzyme for anti-inflammatory therapy.
  • To discuss various classes of 5-lipoxygenase inhibitors.

Main Methods:

  • Enzymatic mechanism elucidation of 5-lipoxygenase.
  • Design and synthesis of competitive inhibitors (iron chelators, redox agents, alternate substrates).

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  • Evaluation of product inhibitors and mechanism-based inactivators of 5-lipoxygenase.

    • Main Results:

    • Understanding the 5-lipoxygenase mechanism enables the development of specific inhibitors.
    • Several classes of competitive inhibitors targeting 5-lipoxygenase have been identified.
    • Product inhibitors and mechanism-based inactivators show promise for potent inhibition.

    Conclusions:

    • Leukotriene biosynthesis inhibitors represent a promising strategy for anti-inflammatory drug development.
    • Targeting 5-lipoxygenase offers a specific approach to modulating inflammatory pathways.
    • Further research into various inhibitor classes could lead to novel anti-inflammatory therapies.