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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2015.1
- 수록면
- 913 - 920 (8page)
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초록· 키워드
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Purpose Anomalies of Akt regulation, including overexpression in lung cancer, impart resistance toconventional chemotherapy and radiation, thereby implicating this kinase as a therapeuticintervention point. A novel scaffold of Akt inhibitors was developed through virtual screeningof chemical databases available at Birla Institute of Technology and Science, Pilani, Hyderabad,based on docking studies using Maestro. A benzothienopyrimidine derivative (BIA-6)was identified as a potential lead molecule that inhibited Akt1 enzyme activity with an IC50of 256 nM.
Materials and MethodsBIA-6 was tested for in vitro Akt1 inhibition using a fluorescence resonance energy transferkit. Anti-proliferative activity was tested in NCI-H460, A549, NCI-H1975, and NCI-H2170cell lines. The effect of the compound on p-Akt (S473) was estimated.
ResultsBIA-6 allosterically caused a dose dependent reduction of growth of cell lines with a halfmaximal growth inhibition (GI50) range of 0.49 !M to 6.6 !M. Cell cycle analysis indicatedthat BIA-6 caused a G1 phase arrest at < 100 nM but led to apoptosis at higher doses. BIA-6 also exhibited synergism with standard chemotherapeutic agents.
ConclusionBIA-6 is a novel, allosteric Akt inhibitor with potent anti-cancer activity in lung cancer celllines, that effectively blocks the phosphoinositide-3 kinase/Akt pathway with a high marginselectivity towards normal cells.
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참고문헌 (25)
참고문헌 신청
Alessi DR / 1997 / Characterization of a 3-phosphoinositidedependent protein kinase which phosphorylates and activates protein kinase Balpha / Curr Biol 7 : 261 ~ 269
Azzoli CG / 2009 / American Society of Clinical Oncology Clinical Practice Guideline update on chemotherapy for stage IV non-small-cell lung cancer / J Clin Oncol 27 : 6251
Barnett SF / 2005 / Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors / Biochem J 385 (Pt 2) : 399 ~ 408
Bhaskar PT / 2007 / The two TORCs and Akt / Dev Cell 12 : 487 ~ 502
Cantley LC / 1999 / New insights into tumor suppression : PTEN suppresses tumor formation by restraining the phosphoinositide 3-kinase/AKT pathway / Proc Natl Acad Sci U S A
Azzoli CG / 2009 / American Society of Clinical Oncology Clinical Practice Guideline update on chemotherapy for stage IV non-small-cell lung cancer / J Clin Oncol 27 : 6251
Barnett SF / 2005 / Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors / Biochem J 385 (Pt 2) : 399 ~ 408
Bhaskar PT / 2007 / The two TORCs and Akt / Dev Cell 12 : 487 ~ 502
Cantley LC / 1999 / New insights into tumor suppression : PTEN suppresses tumor formation by restraining the phosphoinositide 3-kinase/AKT pathway / Proc Natl Acad Sci U S A
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