AKT inhibitors block AKT membrane recruitment

Stable Identifier
R-HSA-2400010
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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AKT inhibitors bind AKT and prevent its association with the membrane, thereby blocking AKT activation (Kondapaka et al. 2003, Yap et al. 2011, Berndt et al. 2010). AKT inhibitors annotated here target all AKT isoforms (AKT1, AKT2 and AKT3). None of the annotated inhibitors are AKT E17K mutant specific and none of them have been approved for clinical use. For a recent review, please refer to Liu et al. 2009.

Literature References
PubMed ID Title Journal Year
14617782 Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation

Kondapaka, SB, Singh, SS, Dasmahapatra, GP, Sausville, EA, Roy, KK

Mol. Cancer Ther. 2003
19644473 Targeting the phosphoinositide 3-kinase pathway in cancer

Liu, P, Cheng, H, Roberts, TM, Zhao, JJ

Nat Rev Drug Discov 2009
22025163 First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors

Yap, TA, Yan, L, Patnaik, A, Fearen, I, Olmos, D, Papadopoulos, K, Baird, RD, Delgado, L, Taylor, A, Lupinacci, L, Riisnaes, R, Pope, LL, Heaton, SP, Thomas, G, Garrett, MD, Sullivan, DM, de Bono, JS, Tolcher, AW

J. Clin. Oncol. 2011
20489726 The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane

Berndt, N, Yang, H, Trinczek, B, Betzi, S, Zhang, Z, Wu, B, Lawrence, NJ, Pellecchia, M, Schönbrunn, E, Cheng, JQ, Sebti, SM

Cell Death Differ. 2010
Participants
Participant Of
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created