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Aminovinyl Cysteine Containing Peptides: A Unique Motif That Imparts Key Biological Activity
JACS Au Pub Date : 2021-09-15 , DOI: 10.1021/jacsau.1c00308
Emily S Grant-Mackie 1 , Elyse T Williams 1 , Paul W R Harris 1, 2, 3 , Margaret A Brimble 1, 2, 3
Affiliation  

Natural products that contain distinctive chemical functionality can serve as useful starting points to develop Nature’s compounds into viable therapeutics. Peptide natural products, an under-represented class of medicines, such as ribosomally synthesized and post-translationally modified peptides (RiPPs), often contain noncanonical amino acids and structural motifs that give rise to potent biological activity. However, these motifs can be difficult to obtain synthetically, thereby limiting the transition of RiPPs to the clinic. Aminovinyl cysteine containing peptides, which display potent antimicrobial or anticancer activity, possess an intricate C-terminal ring that is critical for bioactivity. To date, successful methods for the total chemical synthesis of such peptides are yet to be realized, although several advancements have been achieved. In this perspective, we review this burgeoning class of aminovinyl cysteine peptides and critically evaluate the chemical strategies to install the distinct aminovinyl cysteine motif.

中文翻译:

含氨基乙烯基半胱氨酸的肽:赋予关键生物活性的独特基序

含有独特化学功能的天然产品可以作为将 Nature 的化合物开发成可行疗法的有用起点。肽天然产物是一类代表性不足的药物,例如核糖体合成和翻译后修饰肽 (RiPP),通常含有非规范氨基酸和结构基序,可产生有效的生物活性。然而,这些基序很难综合获得,从而限制了 RiPPs 向临床的过渡。含有氨基乙烯基半胱氨酸的肽具有强大的抗微生物或抗癌活性,具有复杂的 C 端环,这对生物活性至关重要。迄今为止,尽管已经取得了一些进展,但尚未实现这些肽的全化学合成的成功方法。
更新日期:2021-10-25
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