Novel nucleobase-simplified cyclic ADP-ribose analogue: A concise synthesis and Ca(2+)-mobilizing activity in
Lingjun Li1, Cornelia C Siebrands, Zhenjun Yang
1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China.
Abstract:
A purine nucleobase-simplified cyclic ADP ribose (cADPR) analogue was synthesized, in which a 1,2,3-triazole-4-amide was constructed, instead of a purine moiety, and the northern ribose was replaced by an ether strand. Compound exhibits calcium release activity in intact T-lymphocytes and indicates that it is a membrane-permeable cADPR mimic. Thus, the cADPR analogue containing 1,2,3-triazole-4-amide provides a novel template for further designing cADPR analogues and elucidating their structure-activity relationships.
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