Leukotriene B4receptor antagonists as therapeutics for inflammatory disease: preclinical and clinical developments
| Autor: | Alexandra Hicks, Ann F. Hoffman, Robert Alan Goodnow, Seth P. Monkarsh |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Leukotriene B4
Drug Evaluation Preclinical Receptors Leukotriene B4 Disease Pharmacology chemistry.chemical_compound Phospholipase A2 Animals Humans Medicine Pharmacology (medical) Receptor Inflammation Clinical Trials as Topic biology business.industry Leukotriene A4 Leukotriene B4 receptor Drugs Investigational General Medicine Inflammatory mediator Cytosol chemistry biology.protein lipids (amino acids peptides and proteins) business Signal Transduction |
| Zdroj: | Expert Opinion on Investigational Drugs. 16:1909-1920 |
| ISSN: | 1744-7658 1354-3784 |
| Popis: | Leukotriene B(4) (LTB(4)) is a lipid inflammatory mediator derived from membrane phospholipids by the sequential actions of cytosolic phospholipase A2 (PLA2), 5-lipoxygenase (5-LO) and leukotriene A(4) (LTA(4)) hydrolase. Several inflammatory diseases, including asthma, chronic obstructive pulmonary disease, arthritis and inflammatory bowel disease, have been associated with elevated levels of LTB(4). As a result, pharmacological strategies to modulate the synthesis of LTB(4) (inhibition of PLA2, 5-LO or LTA(4) hydrolase) or the effects of LTB(4) itself (antagonism of LTB(4) receptors) are being developed by several companies. Two G-protein-coupled receptors mediate the effects of LTB(4), namely BLT1 and BLT2. The pharmacology, expression and function of these two receptors were last reviewed by Tager and Luster in 2004. Since then, there has been an increased understanding of the function of these receptors, in particular for the lesser understood of the two receptors, BLT2. Furthermore, since last reviewed in 1996, there have been several clinical developments in the use of BLT receptor antagonists for inflammatory diseases. This review summarizes the latest preclinical and clinical developments in BLT antagonism for inflammatory diseases and discusses potential future developments. |
| Databáze: | OpenAIRE |
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