硅烷化
部分
化学
生物分子
硫醇
试剂
硅
组合化学
乙醚
硅醚
基质(水族馆)
有机化学
催化作用
生物化学
海洋学
地质学
作者
Susanto Teng,Zhenguo Zhang,Bohan Li,Lanyang Li,Michael Siew Chye. Tan,Zhenhua Jia,Teck Peng Loh
标识
DOI:10.1002/anie.202311906
摘要
Site-specific modification of thiol-containing biomolecules has been recognized as a versatile and powerful strategy for probing our biological systems and discovering novel therapeutics. The addition of lipophilic silicon moiety opens up new avenues for multi-disciplinary research with broad applications in both the medicinal and material sciences. However, adhering to the strict biocompatibility requirements, and achieving the introduction of labile silicon handle and high chemo-selectivity have been formidable. In this paper, we report silicon-based conjugating reagents including β-trialkylsilyl and silyl ether-tethered alkynones that selectively react with thiols under physiological conditions. The pH-neutral, metal-free and additive-free reaction yields stable products with broad substrate compatibility and full retention of silicon handles in most cases. Besides simple aliphatic and aromatic thiols, this approach is applicable in the labeling of thiols present in proteins, sugars and payloads, thereby expanding the toolbox of thiol conjugation.
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