Synthesis of Biotinylated 2-methoxystypandrone and Identification of JAK2 and IKK as its Targets

doi:10.2174/1871520617666171106123226

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Synthesis of Biotinylated 2-methoxystypandrone and Identification of JAK2 and IKK as its Targets
	Kuang, Shan 1; Sima, Zhenhua 2,3; Liu, Jiawei 2; Li, Wuguo 2; Song, Qiaoling 1; Zhang, Qing1 ; Yu, Qiang1
刊名	ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
	2018
卷号	18 期号:3 页码:422-427
关键词	2-Methoxystypandrone natural compound biotin-tagged probe anticancer drug JAK2 IKK
ISSN号	1871-5206
DOI	10.2174/1871520617666171106123226
文献子类	Article
英文摘要	Background: 2-Methoxystypandrone (2-MS), isolated from the roots of Polygonum cuspidatum, is a potent dual inhibitor of the STAT3 and NF-kappa B pathways. Objective: To investigate the molecular targets and mechanisms of 2-MS. Method: A biotin-conjugated 2-MS analog, named 2-MS-Biotin, was designed and synthesized. The effects of 2-MS-Biotin on the STAT3 and NF-kappa B pathways were examined by Western blotting. The cytotoxicity of 2MS-Biotin was evaluated using real-time cell analysis system. Proteins directly bound to 2-MS-Biotin were pulled down through streptavidin agarose beads and were detected using Western blotting. Results: 2-MS-Biotin retained the inhibition activities of the parent compound 2-MS on the STAT3 and NF-kappa B pathways as well as on cancer cell growth. Also, JAK2 and IKK proteins can be effectively pulled down by 2MS-Biotin. Conclusion: Using 2-MS-Biotin as a tool, both JAK2 and IKK were identified as the targets of 2-MS.
资助项目	China National Natural Science Foundation[81373432] ; China National Natural Science Foundation[81673465] ; China Ministry of Science and Technology Key New Drug Creation and Manufacturing Program[2013ZX09102015] ; Guangzhou Science and Technology Program[2014J4100118]
WOS关键词	POLYGONUM-CUSPIDATUM ; CHEMICAL PROTEOMICS ; CELLULAR TARGETS ; SMALL MOLECULES ; REAGENTS ; ANALOGS ; CELLS ; PROBE
WOS研究方向	Oncology ; Pharmacology & Pharmacy
语种	英语
出版者	BENTHAM SCIENCE PUBL LTD
WOS记录号	WOS:000434969100011
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272312]
专题	药理学第一研究室
通讯作者	Liu, Jiawei; Yu, Qiang
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Tumor Pharmacol, Shanghai, Peoples R China; 2.Guangzhou Univ Chinese Med, Res Ctr Med Plants Resource Sci & Engn, Minist Educ, Key Lab Chinese Med Plants Resource Lingnan, Guangzhou, Guangdong, Peoples R China; 3.Shanghai East Hosp, Jian Hosp, Pharm Dept, Shanghai, Jiangxi, Peoples R China
推荐引用方式 GB/T 7714	Kuang, Shan,Sima, Zhenhua,Liu, Jiawei,et al. Synthesis of Biotinylated 2-methoxystypandrone and Identification of JAK2 and IKK as its Targets[J]. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY,2018,18(3):422-427.
APA	Kuang, Shan.,Sima, Zhenhua.,Liu, Jiawei.,Li, Wuguo.,Song, Qiaoling.,...&Yu, Qiang.(2018).Synthesis of Biotinylated 2-methoxystypandrone and Identification of JAK2 and IKK as its Targets.ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY,18(3),422-427.
MLA	Kuang, Shan,et al."Synthesis of Biotinylated 2-methoxystypandrone and Identification of JAK2 and IKK as its Targets".ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY 18.3(2018):422-427.