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Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Bioorg+Med+Chem+Lett 2012 ; 22 (2): 876-80 Nephropedia Template TP
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Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases #MMPMID22212721
Sabbah DA; Simms NA; Brattain MG; Vennerstrom JL; Zhong H
Bioorg Med Chem Lett 2012[Jan]; 22 (2): 876-80 PMID22212721show ga
The alpha isoform of the phosphatidylinositol-3-kinases (PI3K?) is often mutated, amplified and overex-pressed in human tumors. In an effort to develop new inhibitors targeting this enzyme, we carried out a pharmacophore model study based on six PI3K?-selective compounds. The pharmacophore searching identified three structurally novel inhibitors of PI3K? and its H1047R mutant. Our biological studies show that two of our hit molecules suppressed the formation of pAKT, a downstream effector of PI3K?, and induced apoptosis in the HCT116 colon cancer cell line. QPLD-based docking showed that residues Asp933, Glu849, Val851, and Gln859 appeared to be key binding residues for active inhibitors.