Substitution at the 8-position of 3"-deoxy-cyclic ADP-carbocyclic-ribose, a highly potent Ca2+-mobilizing agent, provides partial agonists
Substitution at the 8-position of 3"-deoxy-cyclic ADP-carbocyclic-ribose, a highly potent Ca2+-mobilizing agent, provides partial agonists
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DOI：
10.1016/j.bmc.2007.02.001
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发表时间：
2007-04-15
影响因子：
3.5
通讯作者：
Shuto, Satoshi
中科院分区：
文献类型：
--
作者：
Kudoh, Takashi;Murayama, Takashi;Shuto, Satoshi
我们之前表明，3”-脱氧-环adp -碳环核糖（3”-脱氧- cadpcr， 4）是环adp -核糖（cADPR, 1）的稳定和高效类似物，cADPR是Ca2+动员的第二信使。根据这些结果，我们设计并合成了其他在8位有取代基的cADPcR的3 ‘’修饰类似物，并发现这种8位修饰使它们成为部分激动剂。在这些化合物中，8-NH2-3”-脱氧- cadpcr（10）被鉴定为有效的部分激动剂，EC50值为17 nM。(c) 2007年Elsevier Ltd.出版
We previously showed that 3 ''-deoxy-cyclic ADP-carbocyclic-ribose (3 ''-deoxy-cADPcR, 4) is a stable and highly potent analogue of cyclic ADP-ribose (cADPR, 1), a Ca2+-mobilizing second messenger. From these results, we designed and synthesized other 3 ''-modified analogues of cADPcR having a substituent at the 8-position and found that this modification at the 8-position made them partial agonists. Among these compounds, 8-NH2-3 ''-deoxy-cADPcR (10) was identified as a potent partial agonist with an EC50 value of 17 nM. (c) 2007 Published by Elsevier Ltd.