Haloenol lactone (HELSS) is a potent and irreversible inhibitor that selectively targets and forms a covalent bond with myocardial group VI iPLA2 (calcium-independent phospholipase A2). Group VI iPLA2 (Calcium-independent phospholipase A2) is a mediator of arachidonic acid release from aortic smooth cells induced by vasopressin. Inhibition of arachidonic acid release was found to be saturable and specific due to HELSS's 1,000-fold selectivity for inhibition of calcium-independent versus calcium-dependent PLA2. HELSS has also been observed to inhibit cellular cytosolic magnesium-dependent PAP (phosphatidic acid phosphohydrolase) activity in intact P388D1 macrophages. It is noted that this compound is also a GST (glutathione S-transferases) inhibitor that could help prevent GST-mediated drug resistance. HELSS (Haloenol lactone suicide substrate, BEL, Bromoenol lactone) is an inhibitor of Chymotrypsin.
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See how others have used HELSS (Haloenol lactone suicide substrate, BEL, Bromoenol lactone). Click on the entry to view the PubMed entry .
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