AMP-activated protein kinase modulators: a patent review (2006 - 2010)

AMPK is a key player in the regulation of energy balance at both the cellular and whole-body levels, placing it at the center stage in studies of metabolic disorders. Recently, AMPK has also been identified as a potential target for either therapy or prevention of some types of cancer. Thus, identification of AMPK modulators for possible use as novel therapeutic drugs, both for treatment of metabolic disorders and cancer, will have a high commercial potential.

This review covers the structures and activities of AMPK modulators described in the patent literature since 2006. The patents reviewed include those for direct and/or indirect activators of AMPK, and novel pharmaceutical compounds with potential for use in the prevention and/or treatment of metabolic disorders, and cancer targeting AMPK.

Targeting of AMPK appears to be an attractive strategy in the treatment of metabolic disorders. However, some detrimental effects of AMPK have also been reported, including a possible tumor-promoting effect in some settings and a heart disease-causing effect. Moreover, activation of AMPK in the hypothalamus may cause undesired consequences, such as an increase in feeding and body weight gain. These effects, therefore, must be carefully assessed for the development of therapeutic drugs targeting AMPK.