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. Author manuscript; available in PMC: 2011 Sep 19.
Published in final edited form as: Clin Cancer Res. 2010 Apr 27;16(13):3322–3328. doi: 10.1158/1078-0432.CCR-09-1955

Table 1.

Current direct and indirect AMPK activators

Activator Effect on AMPK Mechanism
Metformin indirect Increase AMP/ATP by inhibition of complex 1 of mitochondrial respiratory chain
TZDs* indirect Increase PPARγ-mediated release of adiponectin, which consequently activates AMPK
Deguelin indirect Not fully clarified. Decrease of ATP
Epigallocatechin-3-gallate indirect Activation of the AMPK activator CaMKK**
Barberin indirect Increase AMP/ATP by inhibition of mitochondrial function
α-Lipoic acid indirect n.d.
Resveratrol indirect Not fully clarified. Possible activation of SIRT1*** and consequent deacetylation of the AMPK activator LKB1
AICAR **** direct AMP mimetic
A-769662 direct Allosteric binding of β1 AMPK subunit
PT1 direct Allosteric binding of α1 AMPK subunit

n.d.= not determined yet,

*

TZDs= thazolidinediones,

**

CAMKK= Calmodulin-dependent protein kinase kinase,

***

SIRT1= sirtuin 1,

****

AICAR= 5-Aminoimidazole-4-carboxamide-1-b-riboside.