The structural basis of Akt PH domain interaction with calmodulin
2021年5月18日 · Akt is a principal component in the Ras/PI3K/Akt/mTOR pathway, translocating to the plasma membrane by calmodulin that releases autoinhibition. At the membrane, PIP 3 …
Structure of autoinhibited Akt1 reveals mechanism of PIP - PNAS
2021年8月12日 · We have now determined the crystal structure of Akt1, revealing an autoinhibitory interface between the PH and kinase domains that is often mutated in cancer …
The Akt activation inhibitor TCN-P inhibits Akt ... - Nature
2010年5月21日 · In this study, using biochemical and cell biological studies, surface plasmon resonance (SPR) and nuclear magnetic resonance (NMR), we show that TCN-P, but not TCN, …
The structural determinants of PH domain-mediated regulation of Akt ...
2020年8月3日 · We determine that Akt allosteric inhibitor MK2206 drives distinct PH domain structural changes compared to baseline autoinhibited Akt. These results highlight how the …
Protein kinase B - Wikipedia
Protein kinase B (PKB), also known as Akt, is the collective name of a set of three serine/threonine-specific protein kinases that play key roles in multiple cellular processes such …
Role of a Novel PH-Kinase Domain Interface in PKB/Akt …
2009年1月20日 · The secondary structure of the kinase domain is represented as a white ribbon. The PH domain residue Trp 80 is shown in red. The position of AKT inhibitor VIII (blue) is …
Akt1 (henceforth Akt) comprises three conserved domains: an N-terminal pleckstrin homology domain (PHD), a conserved catalytic kinase domain, and a flexible C-terminal regulatory …
Interaction of Akt-PH domain and AGG. A schematic ribbon …
Abrus agglutinin (AGG), a type II ribosome-inactivating protein has been found to induce mitochondrial apoptosis. In the present study, we documented that AGG-mediated Akt …
Inspection of the known crystal structure of the Akt PH domain suggested three basic surfaces on the PH domain that could potentially interact with C-ter- minal phosphorylation sites, …
AKT crystal structure and AKT-specific inhibitors | Oncogene
2005年11月14日 · We highlight structural features of AKT kinase in its inactive and active states as well as current efforts to design structure-based small molecule inhibitors of AKT.