FLAP (Arachidonate 5-lipoxygenase-activating protein) is a protein that in humans is encoded by the ALOX5AP gene. FLAP is necessary for the activation of 5-lipoxygenase and therefore for the production of leukotrienes. It is an integral protein within the nuclear membrane. FLAP is necessary in synthesis of leukotriene, which are lipid mediators of inflammation that is involved in respiratory and cardiovascular diseases. FLAP functions as a membrane anchor for 5-lipooxygenase and as an amine acid-bind protein. Gene polymorphisms in FLAP are suspected of playing a role in Alzheimer's disease. Leukotrienes, which need the FLAP protein to be made, have an established pathological role in allergic and respiratory diseases. Animal and human genetic evidence suggests they may also have an important role in atherosclerosis, myocardial infarction, and stroke. The structure of FLAP provides a tool for the development of novel therapies for respiratory and cardiovascular diseases and for the design of focused experiments to probe the cell biology of FLAP and its role in leukotriene biosynthesis.
||MK886 is a potent 5-lipoxygenase activating protein inhibitor (FLAP) also a non-competitive inhibitor of PPAR alpha. a potent inhibitor of leukotriene (LT) biosynthesis in intact human polymorphonuclear leukocytes with IC 50 of 2.5 nM. Block the synthessis of leukotrien intact activate leukocyte.
||ABT-080 is a potent FLAP inhibitor that inhibits ionophore-stimulated LTB(4) formation with with IC50 of 20 nM.
||A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay.
||A potent, selective FLAP inhibitor with binding IC50 of 2.6 nM.