"Splicing up" drug discovery. Cell-based expression and screening of genetically-encoded libraries of backbone-cyclized polypeptides.

"Splicing up" drug discovery. Cell-based expression and screening of genetically-encoded libraries of backbone-cyclized polypeptides.
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“剪接”药物发现。基于细胞的表达和筛选骨干环化多肽的遗传编码库。

DOI:
10.1016/j.addr.2009.07.003
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发表时间:
2009-09-30
影响因子:
16.1
通讯作者:
Camarero, Julio A.
Camarero, Julio A.
中科院分区:
医学1区
文献类型:
--
作者:
Sancheti, Harshkumar;Camarero, Julio A.

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本文综述了蛋白质剪接在主链环多肽生物合成中的应用。该通用方法允许使用重组DNA表达技术在体内和体外生物合成环状多肽。对骨架环肽的生物合成途径打开了产生基于细胞的组合文库的可能性,所述组合文库可以在活细胞内筛选其减弱或抑制细胞过程的能力,从而提供了寻找治疗剂的新途径。
The present paper reviews the use of protein splicing for the biosynthesis of backbone cyclic polypeptides. This general method allows the in vivo and in vitro biosynthesis of cyclic polypeptides using recombinant DNA expression techniques. Biosynthetic access to backbone cyclic peptides opens the possibility to generate cell-based combinatorial libraries that can be screened inside living cells for their ability to attenuate or inhibit cellular processes thus providing a new way for finding therapeutic agents.
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