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2012 ; 22
(2
): 876-80
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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
PMID22212721
show ga
The alpha isoform of the phosphatidylinositol-3-kinases (PI3K?) is often mutated,
amplified and overexpressed 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.