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Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase
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
2014-10-01
DOI10.3390/molecules191015754
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
WOS记录号WOS:000344456100023
项目编号91213302 ; 81172917 ; 31301156
资助机构National Natural Sciences Foundation of China
引用统计
被引频次:16[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/50270
专题北京大学药学院
北京大学药学院_化学生物学系
北京大学药学院_药物化学系
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
推荐引用方式
GB/T 7714
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.
APA Zhu, Wenjie.,Wang, Shengjun.,Wang, Xuan.,Li, Jianguo.,Zhang, Kehui.,...&Zhang, Lihe.(2014).Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase.MOLECULES,19(10),15754-15767.
MLA Zhu, Wenjie,et al."Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase".MOLECULES 19.10(2014):15754-15767.
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