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The Leukotriene C4 (LTC4) generation pathway is a multi-step biochemical process primarily occurring in human leukocytes, including eosinophils, mast cells, and macrophages [PMID: 18304342]. It involves the conversion of arachidonic acid into the potent pro-inflammatory mediator LTC4 through the sequential action of 5-lipoxygenase (5-LOX), 5-lipoxygenase-activating protein (FLAP), and leukotriene C4 synthase (LTC4S) [UniProt P09917, P20292, P30351]. LTC4 is the precursor to other cysteinyl leukotrienes (LTD4 and LTE4), which play a central role in the pathophysiology of asthma and allergic rhinitis by inducing bronchoconstriction, mucus hypersecretion, and increased vascular permeability [StatPearls PMID: 30725821]. Pharmacological targeting of this pathway typically involves inhibitors of 5-LOX or FLAP to prevent the formation of these mediators [PubChem CID 60490]. While clinically effective for respiratory conditions, drugs targeting this pathway, such as zileuton, require monitoring for adverse effects like liver enzyme elevations and neuropsychiatric symptoms [FDA Label Zileuton].
Inhibition of the enzymatic conversion of arachidonic acid to leukotriene C4 through the targeting of 5-lipoxygenase (5-LOX), 5-lipoxygenase-activating protein (FLAP), or leukotriene C4 synthase (LTC4S) [PMID: 21170012].
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