Biological evaluation and docking studies of recently identified ... | 寵物協尋網
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由DASabbah著作·2012·被引用36次—PMID:22212721·PMCID:PMC4472446·DOI:10.1016/j.bmcl.2011.12.044 ...
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The alpha isoform of the phosphatidylinositol-3-kinases (PI3Kα) 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 PI3Kα-selective compounds. The pharmacophore searching identified three structurally novel inhibitors of PI3Kα and its H1047R mutant. Our biological studies show that two of our hit molecules suppressed the formation of pAKT, a downstream effector of PI3Kα, 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.
2145 Dearborn Ave Missoula | 寵物協尋網
2145 Dearborn Ave, Missoula | 寵物協尋網
2145 Dearborn Ave, Missoula | 寵物協尋網
22212721 | 寵物協尋網
22212721 | 寵物協尋網
22212721 | 寵物協尋網
5942 E Calle Silvosa, Tucson | 寵物協尋網
Biological evaluation and docking studies of recently identified ... | 寵物協尋網
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