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Synonyms: PHT 427 | PHT427
Compound class: Synthetic organic
Comment: PHT-427 is a novel dual inhibitor of 3-phosphoinositide dependent protein kinase 1 (PDK1) and Akt (protein kinase B) . The original identification of PHT-427 (compound 14) as an Akt inhibitor is described in  where it is shown to bind to the pleckstrin homology (PH) domain of Akt, not to the catalytic ATP binding site. PDK1 activates Akt by phosphorylating Thr308 in Akt's kinase domain.
The PDK1/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumour angiogenesis and represents a promising target for oncology therapeutics [2,4].
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Du-Cuny L, Song Z, Moses S, Powis G, Mash EA, Meuillet EJ, Zhang S. (2009)
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
Bioorg. Med. Chem., 17 (19): 6983-92. [PMID:19734051]
2. Hanada M, Feng J, Hemmings BA. (2004)
Structure, regulation and function of PKB/AKT--a major therapeutic target.
Biochim. Biophys. Acta, 1697 (1-2): 3-16. [PMID:15023346]
3. Meuillet EJ, Zuohe S, Lemos R, Ihle N, Kingston J, Watkins R, Moses SA, Zhang S, Du-Cuny L, Herbst R et al.. (2010)
Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor.
Mol. Cancer Ther., 9 (3): 706-17. [PMID:20197390]
4. Shiojima I, Walsh K. (2002)
Role of Akt signaling in vascular homeostasis and angiogenesis.
Circ. Res., 90 (12): 1243-50. [PMID:12089061]