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Protein kinase B (PKB; PKBA; AKT; AKT1)

In vitro studies suggest identifying the type of AKT1 mutations in patients with cancer could help guide treatment decisions. In a mouse lymphoid cell line, expression of Akt1 with mutations in the pleckstrin homology (PH)-kinase domain (KD) led to constitutive Akt1 activation, whereas expression of wild-type Akt1 did not. In vitro, allosteric AKT1 inhibitors showed lower efficacy for AKT1 with PH-KD mutations than for wild-type AKT1 or AKT1 with other activating mutations. In the same assay, ATP-site inhibitors were effective at blocking AKT1 with PH-KD mutations. Next steps could include determining how various mutations in AKT1 affect tumor responsiveness to various AKT1 inhibitors.
At least 11 companies have AKT1 inhibitors in clinical and preclinical development to treat cancer.

SciBX 5(47); doi:10.1038/scibx.2012.1232
Published online Dec. 6, 2012

Patent and licensing status undisclosed

Parikh, C. et al. Proc. Natl. Acad. Sci. USA; published online Nov. 7, 2012;
Contact: Somasekar Seshagiri, Genentech Inc.,
South San Francisco, Calif.