Journal article

Enhanced activation of cellular AMPK by dual-small molecule treatment: AICAR and A769662

Serge Ducommun, Rebecca J Ford, Laurent Bultot, Maria Deak, Luc Bertrand, Bruce E Kemp, Gregory R Steinberg, Kei Sakamoto

AJP Endocrinology and Metabolism | AMER PHYSIOLOGICAL SOC | Published : 2014


AMP-activated protein kinase (AMPK) is a key cellular energy sensor and regulator of metabolic homeostasis. Activation of AMPK provides beneficial outcomes in fighting against metabolic disorders such as insulin resistance and type 2 diabetes. Currently, there is no allosteric AMPK activator available for the treatment of metabolic diseases, and limited compounds are available to robustly stimulate cellular/tissue AMPK in a specific manner. Here we investigated whether simultaneous administration of two different pharmacological AMPK activators, which bind and act on different sites, would result in an additive or synergistic effect on AMPK and its downstream signaling and physiological even..

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Funding Acknowledgements

These studies were supported by grants and fellowships from the Australian Research Council (B. E. Kemp), the Australian National Health and Medical Research Council (B. E. Kemp and G. R. Steinberg), the Canadian Diabetes Association (G. R. Steinberg), and the Canadian Institutes of Health Research (CIHR) (G. R. Steinberg) and supported in part by the Victorian Government's OIS Program (B. E. Kemp) and the Canadian Foundation for Innovation (G. R. Steinberg). G. R. Steinberg is a Canada Research Chair in Metabolism and Obesity. L. Bertrand is Research Associate of the Fonds National de la Recherche Scientifique (FNRS), Belgium.