Small-molecule discovery in the pancreatic beta cell

The pancreatic beta cell is the only cell type in the body responsible for insulin secretion, and thus plays a unique role in the control of glucose homeostasis. The loss of beta-cell mass and function plays an important role in both type 1 and type 2 diabetes. Thus, using chemical biology to identify small molecules targeting the beta cell could be an important component to developing future therapeutics for diabetes. This strategy provides an attractive path toward increasing beta-cell numbers in vivo. A regenerative strategy involves enhancing proliferation, differentiation, or neogenesis. On the other hand, protecting beta cells from cell death, or improving maturity and function, could preserve beta-cell mass. Here, we discuss the current state of chemical matter available to study beta-cell regeneration, and how they were discovered.