Novel leukotriene biosynthesis inhibitors (2012-2016) as anti-inflammatory agents.

作者: Oliver Werz , Jana Gerstmeier , Ulrike Garscha

DOI: 10.1080/13543776.2017.1276568

关键词: Lipid signalingLeukotriene-A4 hydrolaseBiologyBiosynthesisLeukotrieneInflammationReceptor5-lipoxygenase-activating proteinBiochemistryArachidonate 5-lipoxygenase

摘要: ABSTRACTIntroduction: Leukotrienes (LTs) are lipid mediators produced from arachidonic acid with a broad variety of bioactivities in allergy and inflammation. The biosynthesis LTs mainly involves 5-lipoxygenase (5-LO) its 5-lipoxygenase-activating protein (FLAP), LTA4 hydrolase LTC4 synthase that all may represent potential targets for LT inhibitors.Areas covered: We introduce the biosynthetic pathway cellular regulation, diverse biological actions their receptors, we briefly describe pharmacological strategies suppression formation as well classes current inhibitors. main focus is placed on comprehensive discussion recently reported inhibitors 5-LO, FLAP, synthase, based literature search (PubMed Thomson Innovation Patents Searches), covering 2012–2016.Expert opinion: Although many new series 5-LO have been presented without patenting, essentially by aca...

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