ABSTRACT

Diabetes is the most common metabolic disease in humans. The hallmark of diabetes is an elevated blood glucose concentration, but this abnormality is just one of many biochemical and physiological alterations that occur in the disease. An increasing amount of data point to a role for transient receptor potential (TRP) channels in pancreatic beta-cells, and the regulation of insulin secretion. TRP channels have been described both in primary beta-cells and insulin-secreting cell lines. TRP vanilloid (TRPV2), TRPV4, TRP canonical (TRPC1), TRPC4, TRPC6, TRP melastatin (TRPM2), TRPM3, TRPM4, and TRPM5 are identified in insulinoma cell lines such as MIN6 or INS-1. TRP channels are interesting targets for the development of insulin secretagogues. Emerging evidence indicates that TRP channels regulate insulin release and ß-cell function, specifically through their ability to increase intracellular Ca2+ levels and membrane depolarization. Several TRP channels show interesting potential to be used as a target for insulinotropic drugs.