Characterisation of Novel Small Compound Activators of AMPK (#101)
AMP-activated protein kinase (AMPK) is an αβγ heterotrimer which senses changes in energy availability in the form of changing adenosine nucleotide ratios2 . As a promoter of lipid oxidation and plasma glucose lowering pathways, its activation is desirable for the treatment of metabolic disorders, most notably Type 2 diabetes1 . Exercise and caloric restriction have been identified as effective physiological methods for activating AMPK, however direct pharmacological activators remain largely uncharacterised. Understanding drug-binding sites, isoform specificity and mechanism of action of known AMPK activators is crucial in the development of more effective treatments of metabolic disorders.
- Steinberg, G. R., & Kemp, B. E. (2009). AMPK in Health and Disease. Physiol Rev, 89(3), 1025-1078
- Oakhill, J. S., Scott, J. W., & Kemp, B. E. (2012). AMPK functions as an adenylate charge-regulated protein kinase. Trends in Endocrinol & Metabolism, 23(3), 125-132