Description
The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components.
1 The calcium-
independent phospholipases (iPLA
2) are a PLA
2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-
Bromoenol lactone ((R)-
BEL) is an irreversible, chiral, mechanism-
based inhibitor of calcium-
independent phospholipase γ (iPLA
2γ). Unlike (S)-
BEL, (R)-
BEL does not inhibit iPLA
2β except at high doses of 20-
30 μM.
2 (R)-
BEL inhibits human recombinant iPLA
2γ with an IC
50 of approximately 0.6 μM.
References
1. Balsinde, J., Balboa, M.A., Insel, P.A., et al.
Regulation and inhibition of phospholipase A2 Annu. Rev. Pharmacol. Toxicol. 39,175-189(1999).
2. Jenkins, C.M., Han, X., Mancuso, D.J., et al.
Identification of calcium-independent phospholipase A2 (iPLA2)β, and not iPLA2γ, as the mediator of arginine vasopressin-induced arachidonic acid release in A-10 smooth muscle cells J. Biol. Chem. 277(36),32807-32814(2002).
