Recent advances in synthetic and medicinal chemistry of phosphotyrosine and phosphonate-based phosphotyrosine analogues,RSC Medicinal Chemistry

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Recent advances in synthetic and medicinal chemistry of phosphotyrosine and phosphonate-based phosphotyrosine analogues
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-10-15 , DOI: 10.1039/d0md00272k
Nikolai Makukhin ₁ , Alessio Ciulli ₁

Affiliation

Phosphotyrosine-containing compounds attract significant attention due to their potential to modulate signalling pathways by binding to phospho-writers, erasers and readers such as SH2 and PTB domain containing proteins. Phosphotyrosine derivatives provide useful chemical tools to study protein phosphorylation/dephosphorylation, and as such represent attractive starting points for the development of binding ligands and chemical probes to study biology, and for inhibitor and degrader drug design. To overcome enzymatic lability of the phosphate group, physiologically stable phosphonate-based phosphotyrosine analogues find utility in a wide range of applications. This review covers advances over the last decade in the design of phosphotyrosine and its phosphonate-based derivatives, highlights the improved and expanded synthetic toolbox, and illustrates applications in medicinal chemistry.

中文翻译：

磷酸酪氨酸和基于膦酸酯的磷酸酪氨酸类似物的合成和药物化学的最新进展

含磷酸酪氨酸的化合物因其通过与磷酸化写入器、擦除器和读取器（例如含有 SH2 和 PTB 结构域的蛋白质）结合而调节信号传导途径的潜力而引起了广泛关注。磷酸酪氨酸衍生物为研究蛋白质磷酸化/去磷酸化提供了有用的化学工具，因此代表了开发结合配体和化学探针以研究生物学以及抑制剂和降解剂药物设计的有吸引力的起点。为了克服磷酸基团的酶不稳定性，生理稳定的基于膦酸酯的磷酸酪氨酸类似物在广泛的应用中得到了应用。这篇综述涵盖了过去十年中磷酸酪氨酸及其基于膦酸酯的衍生物的设计进展，重点介绍了改进和扩展的合成工具箱，并说明了在药物化学中的应用。

更新日期：2020-10-15

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