CAY10590

Phospholipase A₂ (PLA₂) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis.¹ Three primary types of PLA₂ exist: secretory (sPLA₂), calcium-dependent cytosolic (cPLA₂), and calcium-independent cytosolic (iPLA₂).² Of these three enzymes, cPLA₂ is the rate-limiting stimulus for release of arachidonic acid whereas sPLA₂ amplifies the action of cPLA₂ and regulates phagocytosis and foam cell formation.³ CAY10590, a simple amide based on (R)-γ-norleucine, is a potent and selective inhibitor of sPLA₂. It exhibits 95% inhibition (X_I(50) = 0.003) of sPLA₂ at 0.091 mole fraction without affecting the activities of cPLA₂ or iPLA₂.⁴

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1. Dennis, E.A. Phospholipases. The Enzymes XVI, (1983).

2. Dennis, E.A. Diversity of group types, regulation, and function of phospholipase A₂. The Journal of Biological Chemisty 269(18), 13057-13060 (1994).

3. Balestrieri, B., and Arm, J.P. Group V sPLA₂: Classical and novel functions. Biochim. Biophys. Acta 1761(11), 1280-1288 (2006).

4. Antonopoulou, G., Barbayianni, E., Magrioti, V., et al. Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A₂ enzymes. Bioorg. Med. Chem. 16(24), 10257-10269 (2008).