β-Lactones: A Novel Class of Ca²⁺-Independent Phospholipase A₂ (Group VIA iPLA₂) Inhibitors with the Ability To Inhibit β-Cell Apoptosis.

ABSTRACT: Ca²⁺-independent phospholipase A₂ (GVIA iPLA₂) has gained increasing interest recently as it has been recognized as a participant in biological processes underlying diabetes development and autoimmune-based neurological disorders. The development of potent GVIA iPLA₂ inhibitors is of great importance because only a few have been reported so far. We present a novel class of GVIA iPLA₂ inhibitors based on the β-lactone ring. This functionality in combination with a four-carbon chain carrying a phenyl group at position-3 and a linear propyl group at position-4 of the lactone ring confers excellent potency. trans-3-(4-Phenylbutyl)-4-propyloxetan-2-one (GK563) was identified as being the most potent GVIA iPLA₂ inhibitor ever repo

SUBMITTER: Dedaki C 

PROVIDER: S-EPMC6767909 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature