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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 한국미생물생명공학회 Journal of Microbiology and Biotechnology Journal of Microbiology and Biotechnology 제28권 제8호
- 발행연도
- 2018.1
- 수록면
- 1,401 - 1,411 (11page)
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The serine-threonine kinase AKT plays a pivotal role in tumor progression and is frequently overactivated in cancer cells; this protein is therefore a critical therapeutic target for cancer intervention. We aimed to identify small molecule inhibitors of the pleckstrin homology (PH) domain of AKT to disrupt binding of phosphatidylinositol-3,4,5-trisphosphate (PIP3), thereby downregulating AKT activity. Liposome pulldown assays coupled with fluorescence spectrometry were used to screen flavonoids for inhibition of the AKT PH-PIP3 interaction. Western blotting was used to determine the effects of the inhibitors on AKT activation in cancer cells, and in silico docking was used for structural analysis and optimization of inhibitor structure. Several flavonoids showing up to 50% inhibition of the AKT PH-PIP3 interaction decreased the level of AKT activation at the cellular level. In addition, the modified flavonoid showed increased inhibitory effects and the approach would be applied to develop anticancer drug candidates. In this study, we provide a rationale for targeting the lipidbinding domain of AKT, rather than the catalytic kinase domain, in anticancer drug development.
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참고문헌 (34)
참고문헌 신청
Stahelin RV / 2009 / Lipid binding domains: more than simple lipid effectors / J. Lipid Res. 50:S299~S304
Hurley JH / 2001 / Subcellular targeting by membrane lipids / Curr. Opin. Cell Biol. 13:146~152
Park M-J / 2016 / SH2 domains serve as lipid-binding modules for pTyrsignaling proteins / Mol. Cell 62:7~20
Vivanco I / 2002 / The phosphatidylinositol 3-kinase-AKT pathway in human cancer / Nat. Rev. Cancer 2:489~501
Maehama T / 1999 / PTEN: a tumour suppressor that functions as a phospholipid phosphatase / Trends Cell Biol. 9:125~128
Hurley JH / 2001 / Subcellular targeting by membrane lipids / Curr. Opin. Cell Biol. 13:146~152
Park M-J / 2016 / SH2 domains serve as lipid-binding modules for pTyrsignaling proteins / Mol. Cell 62:7~20
Vivanco I / 2002 / The phosphatidylinositol 3-kinase-AKT pathway in human cancer / Nat. Rev. Cancer 2:489~501
Maehama T / 1999 / PTEN: a tumour suppressor that functions as a phospholipid phosphatase / Trends Cell Biol. 9:125~128
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