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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 한국미생물생명공학회 Journal of Microbiology and Biotechnology Journal of Microbiology and Biotechnology 제25권 제3호
- 발행연도
- 2015.1
- 수록면
- 418 - 422 (5page)
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In the course of screening for novel cell cycle inhibitors and apoptotic inducers, CR389, elucidated as 5-(1H-benzoimidazol-2-yl)-1H-pyridin-2-one, was generated as a new hit compound. Flow cytometric analysis and western blots of PA-1 cells treated with 40 μM CR389 revealed an appreciable cell cycle arrest at the G2/M phase through direct inhibition of the CDK1 complex. In addition, activation of p53 via phosphorylation at Ser15 and subsequent up-regulation of p21CIP1 showed that CR389 also induces p53-dependent-p21CIP1-mediated cell cycle arrest. Furthermore, apoptotic induction in 40 μM CR389-treated PA-1 cells is associated with the release of cytochrome c from mitochondria through up-regulation of the proapoptotic Bax protein, which results in the activation of procaspase-9 and -3, and the cleavage of poly(ADP-ribose) polymerase (PARP). Accordingly, CR389 seems to have multiple mechanisms of antiproliferative activity through p53-mediated pathways against human ovarian cancer cells. Therefore, we conclude that CR389 is a candidate therapeutic agent for the treatment of human ovarian cancer via the activation of p53.
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등록된 정보가 없습니다.
참고문헌 (22)
참고문헌 신청
Benchimol S. / 2001 / p53-dependent pathways of apoptosis / Cell Death Differ 8 : 1049 ~ 1051
Chan TA / 2000 / Cooperative effects of genes controlling the G(2)/M checkpoint / Genes Dev 14 : 1584 ~ 1588
Choi BY / 2010 / Cell cycle arrest and cytochrome cmediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells / Bioorg. Med. Chem. L
Choi YH / 2000 / p 53-independent induction of p21 (WAF1/CIP1), reduction of cyclin b1 and G2/M arrest by the isoflavone genistein in human prostate carcinoma cells / Jpn. J.
Gray N / 1999 / ATP-site directed inhibitors of cyclin-dependent kinases / Curr. Med. Chem 6 : 859 ~ 875
Chan TA / 2000 / Cooperative effects of genes controlling the G(2)/M checkpoint / Genes Dev 14 : 1584 ~ 1588
Choi BY / 2010 / Cell cycle arrest and cytochrome cmediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells / Bioorg. Med. Chem. L
Choi YH / 2000 / p 53-independent induction of p21 (WAF1/CIP1), reduction of cyclin b1 and G2/M arrest by the isoflavone genistein in human prostate carcinoma cells / Jpn. J.
Gray N / 1999 / ATP-site directed inhibitors of cyclin-dependent kinases / Curr. Med. Chem 6 : 859 ~ 875
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