Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.in vitro: Azoramide is a dual-function endoplasmic reticulum (ER) modulator. Azoramide improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress in multiple systems. Azoramide regulates ER folding and secretion capacity without inducing ER stress. Azoramide might have the protective effects of enhancing chaperone expression and reducing protein synthesis without inducing cytotoxicity and apoptosis.in vivo: Azoramide exhibits potent antidiabetic efficacy in two independent mouse models of obesity by improving insulin sensitivity and pancreatic β cell function. Azoramide improves glucose homeostasis in mice with genetic obesity. Azoramide improves glucose homeostasis in mice with diet-induced obesity.
References:
[1]. Fu S, et al. Sci Transl Med. 2015 Jun 17;7(292):292ra98. doi: 10.1126/scitranslmed.aaa9134. Phenotypic assays identify azoramide as a small-molecule modulator of the unfolded protein response withantidiabetic activity.