“点击循环 ADP-核糖”：一种中性第二信使模拟物。
'Click cyclic ADP-ribose': a neutral second messenger mimic.
机构信息
Wolfson Laboratory of Medicinal Chemistry, Dept. of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, UK.
出版信息
Chem Commun (Camb). 2014 Mar 7;50(19):2458-61. doi: 10.1039/c3cc49249d. Epub 2014 Jan 23.
Analogues of the potent Ca(2+) releasing second messenger cyclic ADP-ribose (cADPR) with a 1,2,3-triazole pyrophosphate bioisostere were synthesised by click-mediated macrocyclisation. The ability to activate Ca(2+) release was surprisingly retained, and hydrolysis of cADPR by CD38 could also be inhibited, illustrating the potential of this approach to design drug-like signalling pathway modulators.
通过点击介导的大环化反应，合成了具有 1,2,3-三唑焦磷酸生物等排体的强效 Ca(2+)释放第二信使环 ADP-核糖（cADPR）类似物。令人惊讶的是，它们激活 Ca(2+)释放的能力得以保留，同时 CD38 对 cADPR 的水解也可以被抑制，这说明了这种方法在设计类似药物的信号通路调节剂方面的潜力。
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