Design, Synthesis, and Identification of 4α-azidoethyl-Cyclic ADP-Carbocyclic-Ribose as a Highly Potent Analogue of Cyclic ADP-Ribose a Ca2+-mobilizing Second Messenger
Design, Synthesis, and Identification of 4α-azidoethyl-Cyclic ADP-Carbocyclic-Ribose as a Highly Potent Analogue of Cyclic ADP-Ribose a Ca2+-mobilizing Second Messenger
复制标题
4α-叠氮乙基-环状 ADP-碳环-核糖的设计、合成和鉴定，作为环状 ADP-核糖（Ca2+ 动员第二信使）的高效类似物
DOI：
10.1021/acs.jmedchem.6b00437
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发表时间：
2016
期刊：
影响因子：
7.3
通讯作者：
S.
中科院分区：
文献类型：
--
作者：
Sato;T.; Watanabe;M.; Tsuzuki;T.; Takano;S.; Murayama;T.; Sakurai;T.; Kameda;T.; Arisawa;M.; Fukuda;H.; Shuto;S.
环二磷酸腺苷-碳环核糖（cADPcR,2）是环二磷酸腺苷-核糖（cADPR,1）的稳定等效物，是Ca2+动员的第二信使。基于cadpr相关化合物的结构-活性关系和cADPcR的三维结构建模，我们设计并合成了cyclic-ADP-4″α-叠氮乙基碳环核糖（N3-cADPcR,3），证明其具有很强的Ca2+动员活性（EC50= 24 nM）。N3-cADPcR将成为制备有效研究cadpr介导的信号通路的生物工具的有用前体。
Cyclic adenosine diphosphate-carbocyclic-ribose (cADPcR,2) is a stable equivalent of cyclic adenosine diphosphate-ribose (cADPR,1), a Ca2+-mobilizing second messenger. On the basis of the structure–activity relationship of cADPR-related compounds and three-dimensional structural modeling of cADPcR, we designed and synthesized cyclic-ADP-4″α-azidoethyl carbocyclic-ribose (N3-cADPcR,3) to demonstrate that it has a highly potent Ca2+-mobilizing activity (EC50= 24 nM). N3-cADPcR will be a useful precursor for the preparation of biological tools effective to investigate cADPR-mediated signaling pathways.