[HTML][HTML] Small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) attenuates diabetes and metabolic disorders

S Kang, R Dahl, W Hsieh, A Shin, KM Zsebo… - Journal of Biological …, 2016 - ASBMB
Dysregulation of endoplasmic reticulum (ER) Ca 2+ homeostasis triggers ER stress leading
to the development of insulin resistance in obesity and diabetes. Impaired function of the
sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) has emerged as a major contributor
to ER stress. We pharmacologically activated SERCA2b in a genetic model of insulin
resistance and type 2 diabetes (ob/ob mice) with a novel allosteric activator, CDN1163,
which markedly lowered fasting blood glucose, improved glucose tolerance, and …