discoveryandcharacterizationofanovelinhibitorofcdc25blgh00045

doi:10.1111/j.1745-7254.2008.00841.x

	discoveryandcharacterizationofanovelinhibitorofcdc25blgh00045
	Xu FENG 1; Lina WANG 2; Yueyang ZHOU 2; Haiping YU 2; Qiang SHEN 2; Yi ZANG 2; Yubo ZHOU 2; Jingya LI 2; Haixia ZHANG 1; Jia LI 2
刊名	actapharmacologicasinica
	2008
卷号	29 期号:10 页码:1268
关键词	DUAL-SPECIFICITY PHOSPHATASE HUMAN-CELLS TRANSGENIC MICE CANCER EXPRESSION CYCLE TRANSITION PROGNOSIS MITOSIS GROWTH LGH00045 high-throughput screening cell division cycle 25B inhibitor cyclin-dependent kinase 1 cell circle
ISSN号	1671-4083
DOI	10.1111/j.1745-7254.2008.00841.x
英文摘要	Aim: Cell division cycle 25 (CDC25) phosphatases have recently been considered as potential targets for the development of new cancer therapeutic agents. We aimed to discover novel CDC25B inhibitors in the present study. Methods: A molecular level high-throughput screening (HTS) assay was set up to screen a set of 48000 pure compounds. Results: HTS, whose average Z' factor is 0.55, was finished and LGH00045, a mixed-type CDC25B inhibitor with a novel structure and relative selectivity for protein tyrosine phosphatases, was identified. Furthermore, LGH00045 impaired the proliferation of tumor cells and increased cyclin-dependent kinase 1 inhibitory tyrosine phosphorylation. In synchronized HeLa cells, LGH00045 delayed cell cycle progression at the G(2)-M transition. Conclusion: LGH00045, a novel CDC25B inhibitor identified through HTS, showed good inhibition on the proliferation of tumor cells and affected the cell cycle progression, which makes it a good hit for further structure modification.
资助项目	[Hi-Tech Research and Development Program of China]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/285465]
专题	中国科学院上海药物研究所
作者单位	1.兰州大学 2.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Xu FENG,Lina WANG,Yueyang ZHOU,et al. discoveryandcharacterizationofanovelinhibitorofcdc25blgh00045[J]. actapharmacologicasinica,2008,29(10):1268.
APA	Xu FENG.,Lina WANG.,Yueyang ZHOU.,Haiping YU.,Qiang SHEN.,...&Jia LI.(2008).discoveryandcharacterizationofanovelinhibitorofcdc25blgh00045.actapharmacologicasinica,29(10),1268.
MLA	Xu FENG,et al."discoveryandcharacterizationofanovelinhibitorofcdc25blgh00045".actapharmacologicasinica 29.10(2008):1268.