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Gene Review:

FLAP - 5-lipoxygenase-activating protein

Ovis aries

Brideau, C. et al., Wube, A.A. et al.

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High impact information on FLAP

MK-0591 has a high affinity for 5-lipoxygenase activating protein (FLAP) as evidenced by an IC50 value of 1.6 nM in a FLAP binding assay and inhibition of the photoaffinity labelling of FLAP by two different photoaffinity ligands [1].
Therefore, the leukotriene biosynthesis inhibitory effect of knipholone was evident by its ability either to inhibit the 5-lipoxygenase activating protein (FLAP) or as a competitive (non-redox) inhibitor of the enzyme [2].

References

Pharmacology of MK-0591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-yl-methoxy)- indol-2-yl]-2,2-dimethyl propanoic acid), a potent, orally active leukotriene biosynthesis inhibitor. Brideau, C., Chan, C., Charleson, S., Denis, D., Evans, J.F., Ford-Hutchinson, A.W., Fortin, R., Gillard, J.W., Guay, J., Guévremont, D. Can. J. Physiol. Pharmacol. (1992) [Pubmed]
Knipholone, a selective inhibitor of leukotriene metabolism. Wube, A.A., Bucar, F., Asres, K., Gibbons, S., Adams, M., Streit, B., Bodensieck, A., Bauer, R. Phytomedicine (2006) [Pubmed]

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