First-generation KATP channel inhibitors were relatively weak and poorly selective; however, extensive optimization efforts over the last several decades have led to the development of numerous different structural classes of highly potent and highly selective Kir6.2/SUR1 inhibitors (Kharade et al., 2016), many of which are Food and Drug Administration (FDA)-approved for treating type 2 diabetes. The gene discussed is ABCC8; the disease is type 2 diabetes mellitus.