Akt (Protein Kinase B) Inhibitors: Small Molecules and Peptides

Akt (Protein kinase B, PKB) is a serine/threonine kinase that plays a key in regulating cell survival, angiogenesis and tumor formation. Akt is a downstream mediator of the PI 3-K pathway, which results in the recruitment of Akt to the plasma membrane via the PH (pleckstrin homology domain) of Akt.

Akt is fully activated by phosphorylation at two key sites: Ser³⁰⁸ (phosphorylated by PDK1) and Thr⁴⁷⁸ (phosphorylated by mTOR and DNA-PK). Akt can then phosphorylated a wide range of substrates including transcription factors (e.g. FOXO1), kinases (GSK-3, Raf-1, ASK, Chk1) and other proteins with important signaling roles (e.g. Bad, MDM2).

There are three isoforms of Akt: Akt 1, 2 and 3 (also known as PKBα, β and γ).