AKT, also known as protein kinase B (proteinkinaseB, PKB), which contains three subtypes (AKT1, AKT2 and AKT3), their molecular structure has the same characteristics.
Akt Inhibitor is designed based on the AKT structure, by combining different parts of AKT, divided into ATP competitive inhibitor, PH structure
Inhibitors, allosteric and substrate analog inhibitors.
GSK690693 is as a representative of ATP competitive inhibitor, GSK690693 can produce inhibition at lower concentrations for three subtypes of AKT. It has the action of reduced level of phosphorylation of downstream molecular action in vitro and animal experiments, and Inhibit potential of the intracellular AKT, and inhibition of tumor cell proliferation and induce tumor cell apoptosis. Early results show that, Although GSK690693 has better anti-tumor effects in vitro, in vivo, this drug has only mild anti-tumor effect. Combined PH structure inhibitor and AKT PH phosphorylation will generate the AKT effects of inhibitory and allosteric. Specificity is an important characteristic of
AKT Inhibitor, wherein the optimal substrate specificity is allosteric inhibitor and analogs inhibitors. Many studies indicate that there are four types of AKP inhibitors if no synergy with anti-tumor drugs, the results of the vivo experiment is unsatisfactory. In addition, a number of small molecule AKT inhibitor has good anti-tumor activity, but it has poor performance pharmacy, thus it is limited to have further research on the clinical.
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