Racemic X-ray structure of L-type calcium channel antagonist Calciseptine prepared by total chemical synthesis  

作　　者：Chen-Chen Chen Shuai Gao Hua-Song Ai Qian Qu Chang-Lin Tian Yi-Ming Li 

机构地区：[1]High Magnetic Field Laboratory, Chinese Academy of Sciences, Hefei 230031, China [2]School of Life Sciences, University of Science and Technology of China, Hefei 230026, China [3]School of Biological and Medical Engineering, Hefei University of Technology, Hefei 230009, China [4]Department of Chemistry, Tsinghua University, Beijing 100084, China

出　　处：《Science China Chemistry》2018年第6期702-707,共6页中国科学（化学英文版）

基　　金：supported by the National Natural Science Foundation of China (21572043, 21473176);the Ministry of Science and Technology (2016YFA0400900, 2015CB910103);the Fundamental Research Funds for the Central Universities (PA2017GDQT0021)

摘　　要：Snake toxin Calciseptine as a natural antagonist of L-type calcium channel has potential drug values, but its structural information remains unknown. Here, we report the total chemical synthesis of Calciseptine by using hydrazide based native chemical ligation. The crystal structure of Calciseptine was determined by racemic protein crystallography technique. Compared to the structure of its homologous family protein, we found that Calciseptine is adopting a typical three-finger structure.Snake toxin Calciseptine as a natural antagonist of L-type calcium channel has potential drug values, but its structural information remains unknown. Here, we report the total chemical synthesis of Calciseptine by using hydrazide based native chemical ligation. The crystal structure of Calciseptine was determined by racemic protein crystallography technique. Compared to the structure of its homologous family protein, we found that Calciseptine is adopting a typical three-finger structure.

关 键 词：protein chemical synthesis calciseptine hydrazide based native chemical ligation racemic protein crystallography 

分 类 号：TQ460.1[化学工程—制药化工]