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学科主题: 药学
题名:
Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase
作者: Zhu, Wenjie2; Wang, Shengjun1; Wang, Xuan1; Li, Jianguo1; Zhang, Kehui1; Zhang, Liangren1; Zhao, Yong-Juan2; Lee, Hon Cheung2; Zhang, Lihe1
关键词: synthesis ; NAD analogues ; CD38 ; inhibitors
刊名: MOLECULES
发表日期: 2014-10-01
DOI: 10.3390/molecules191015754
卷: 19, 期:10, 页:15754-15767
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Organic
研究领域[WOS]: Chemistry
关键词[WOS]: CYCLIC ADP-RIBOSE ; NICOTINAMIDE ADENINE-DINUCLEOTIDE ; STRUCTURAL BASIS ; CALCIUM-RELEASE ; INTERMEDIATE ; CYCLIZATION ; HYDROLYSIS ; SECRETION ; MECHANISM ; CATALYSIS
英文摘要:

Nicotinamide adenine dinucleotide (NAD), one of the most important coenzymes in the cells, is a substrate of the signaling enzyme CD38, by which NAD is converted to a second messenger, cyclic ADP-ribose, which releases calcium from intracellular calcium stores. Starting with 2′-deoxy-2′-fluoroarabinosyl-beta-nicotinamide adenine dinucleotide (ara-F NAD), a series of NAD analogues were synthesized and their activities to inhibit CD38 NAD glycohydrolase (NADase) were evaluated. The adenosine-modified analogues showed potent inhibitory activities, among which 2′-deoxy-2′-fluoroarabinosyl-beta-nicotinamide guanine dinucleotide (ara-F NGD) was the most effective one. The structure-activity relationship of NAD analogues was also discussed.

语种: 英语
所属项目编号: 91213302 ; 81172917 ; 31301156
项目资助者: National Natural Sciences Foundation of China
WOS记录号: WOS:000344456100023
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/50270
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Shenzhen Grad Sch, Sch Chem Biol & Biotechnol, Shenzhen 518052, Peoples R China

Recommended Citation:
Zhu, Wenjie,Wang, Shengjun,Wang, Xuan,et al. Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase[J]. MOLECULES,2014,19(10):15754-15767.
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