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Synthetic Reprogramming of Kinases Expands Cellular Activities of Proteins
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-05-31 , DOI: 10.1002/anie.202202770
Veronika M Shoba 1, 2 , Dhanushka N P Munkanatta Godage 1, 2 , Santosh K Chaudhary 1, 2 , Arghya Deb 1, 2 , Sachini U Siriwardena 1, 2 , Amit Choudhary 1, 2, 3
Affiliation  

A high-yielding synthetic route to bifunctional molecules that reprogram activities of protein kinase C and engineered Abelson kinase to induce phosphorylation on neo-substrates is reported. These phosphorylations have promising inhibitory effects on the activity of Bruton's tyrosine kinase (BTK) and BCR-ABL-dependent cancer cells.

中文翻译:

激酶的合成重编程扩大了蛋白质的细胞活性

报道了一种双功能分子的高产合成路线,该双功能分子重新编程蛋白激酶 C 的活性并改造 Abelson 激酶以诱导新底物上的磷酸化。这些磷酸化对布鲁顿酪氨酸激酶 (BTK) 和 BCR-ABL 依赖性癌细胞的活性具有良好的抑制作用。
更新日期:2022-05-31
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