Synthesis of A11Cys-B11Cys Disulfide Surrogates of H2 Relaxin through an Intermolecular Native Chemical Ligation-Assisted Diaminodiacid Strategy.
Synthesis of A11Cys-B11Cys Disulfide Surrogates of H2 Relaxin through an Intermolecular Native Chemical Ligation-Assisted Diaminodiacid Strategy.
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DOI：
10.1021/acs.orglett.3c02381
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发表时间：
2023-08
期刊：
影响因子：
5.2
通讯作者：
Rui Zhao;P. Shi;Xiao Wei;Zhemin Xia;Chaowei Shi;Jing Shi
中科院分区：
文献类型：
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作者：
Rui Zhao;P. Shi;Xiao Wei;Zhemin Xia;Chaowei Shi;Jing Shi
我们报告了一种分子间天然化学连接辅助的二氨基二酸策略，用于H2松弛素的A11 Cys-B11 Cys二硫键替代物的灵活构建。通过合成四种新的H2松弛素类似物证明了这种策略的实用性，其中发现H2- 2a-B28 Ile与天然H2松弛素相比表现出改善的效力、选择性和稳定性。
We report an intermolecular native chemical ligation-assisted diaminodiacid strategy for the flexible construction of A11Cys-B11Cys disulfide surrogates of H2 relaxin. The practicality of this strategy was evidenced by the synthesis of four new H2 relaxin analogs, among which H2-2a-B28Ile is found to exhibit improved potency, selectivity, and stability compared with native H2 relaxin.