The two faces of protein palmitoylation in islet β-cell function: potential implications in the pathophysiology of islet metabolic dysregulation and diabetes.

The two faces of protein palmitoylation in islet β-cell function: potential implications in the pathophysiology of islet metabolic dysregulation and diabetes. Recent Pat Endocr Metab Immune Drug Discov. 2013 Sep;7(3):203-12 Authors: Mohammed AM, Chen F, Kowluru A Abstract Several cellular proteins undergo post-translational lipidation, including prenylation, palmitoylation and myristoylation, which are felt to promote intracellular targeting, membrane association and interaction with effector partner proteins. Recent findings implicate definitive roles of isoprenylation in islet β-cell function including glucose-stimulated insulin secretion [GSIS]. Published evidence also suggests novel regulatory roles for protein palmitoylation not only in GSIS but also in the metabolic dysfunction induced by proinflammatory cytokines and lipotoxic conditions. Herein, we overviewed the existing evidence on the regulatory roles of protein palmitoylation in the metabolic [dys]regulation of the islet β-cell and highlighted the developments in this area, specifically on potential identity of palmitoylated proteins, and on the utility of two structurally distinct inhibitors of palmitoylation [e.g., cerulenin and 2-bromopalmitate] in halting the metabolic dysfunction of the islet β-cell known to occur following exposure to proinflammatory cytokines and lipotoxic conditions. Potential avenues for future research, including the immediate need for disco...
Source: Recent Patents on Endocrine, Metabolic and Immune Drug Discovery - Category: Endocrinology Tags: Recent Pat Endocr Metab Immune Drug Discov Source Type: research