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Using small molecule GSK3beta inhibitors to treat inflammation #MMPMID20858169
Klamer G; Song E; Ko KH; O'Brien TA; Dolnikov A
Curr Med Chem 2010[]; 17 (26): 2873-81 PMID20858169show ga
Glycogen Synthase Kinase 3 beta (GSK3beta) is a serine-threonine kinase originally identified for its role in the conversion of glucose to glycogen. Pharmacological inhibition can be achieved by drug binding to ATP or magnesium binding sites on the enzyme. Pharmaceutical companies have developed several small molecule GSK3beta inhibitors for diabetes research. Additionally, GSK3beta inhibitors are being clinically tested as therapeutics for neurological diseases, however, the mechanisms of involvement are unclear. Several studies have shown that the therapeutic effect of GSK3beta inhibition is associated with the inhibition of inflammation. Similarly, the mechanisms underlying the anti-inflammatory function of GSK3beta inhibition are not well understood. GSK3beta inhibition attenuates activation of the pro-inflammatory transcription factor NFkappaB, and activates the immuno-modulatory transcription factor beta-catenin. GSK3beta inhibition has also been shown to induce secretion of the anti-inflammatory cytokine IL-10. In addition, pharmacological inhibition of GSK3beta suppressed alloreactive T-cell responses. The combined anti-proliferative and anti-inflammatory properties of small molecule inhibitors of GSK3beta make them an attractive treatment modality towards the control of inflammation.
Curr+Med+Chem 2010 ; 17 (26): 2873-81
