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一种通过 mRNA 展示体外选择订书肽抑制剂的新策略。

A new strategy for the in vitro selection of stapled peptide inhibitors by mRNA display.

机构信息

Department of Chemistry, Virginia Commonwealth University, 1001 West Main Street, P. O. Box 842006, Richmond, VA 23284, USA.

School of Mathematics & Natural Sciences, Chemistry & Biochemistry, 118 College Drive #5043, Hattiesburg, MS 39406, USA.

出版信息

Chem Commun (Camb). 2019 Aug 7;55(61):8959-8962. doi: 10.1039/c8cc10192b. Epub 2019 Jul 10.

Abstract

Hydrocarbon stapled peptides are promising therapeutics for inhibition of intracellular protein-protein interactions. Here we develop a new high-throughput strategy for hydrocarbon stapled peptide discovery based on mRNA display of peptides containing α-methyl cysteine and cyclized with m-dibromoxylene. We focus on development of a peptide binder to the HPV16 E2 protein.

摘要

碳氢化合物订书肽是抑制细胞内蛋白质-蛋白质相互作用的有前途的治疗方法。在这里,我们开发了一种基于含有α-甲基半胱氨酸的肽的 mRNA 展示和与 m-二溴对二甲苯环化的新型高通量碳氢化合物订书肽发现策略。我们专注于开发针对 HPV16 E2 蛋白的肽结合物。

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