Numerous pharmacological agents are currently being used in the clinic as a means to reduce the hyperglycemia associated with Type 2 diabetes. Which of the following class of compounds exerts a portion of their effects by activating the metabolic master regulator, AMPK?

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Biguanides, such as Metformin, exert their effects in part by activating AMPK, which helps to improve insulin sensitivity and reduce hepatic glucose production. Metformin exerts part of its effects by modulating mitochondrial activities. Metformin has a mild inhibitory effect on complex I of oxidative phosphorylation, has antioxidant properties, and activates both glucose-6-phosphate dehydrogenase, G6PDH and AMPK. The importance of AMPK in the actions of metformin stems from the role of AMPK in the regulation of both lipid and carbohydrate metabolism. The activation of AMPK by metformin is likely related to the inhibitory effects of the drug on complex I of oxidative phosphorylation. This would lead to a reduction in ATP production and, therefore, an increase in the level of AMP and as a result activation of AMPK.

Numerous Pharmacological Agents Are Currently Being Used in the Clinic