2013年5月
A conformationally fixed analog of the peptide mimic Grb2-SH2 domain: Synthesis and evaluation against the A431 cancer cell
Molecular BioSystems
- ,
- ,
- ,
- ,
- ,
- ,
- 巻
- 9
- 号
- 5
- 開始ページ
- 1019
- 終了ページ
- 1025
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1039/c3mb25462c
A small peptide mimic of the Grb2-SH2 domain, which was previously prepared through the template-assisted click approach and exhibited selective A431 tumor growth inhibition both in vitro and in vivo, was further elaborated on to enhance the interaction with target phosphorylated proteins. A conformationally fixed analog was efficiently synthesized by solid-supported ring-closing metathesis and Cu(i)/His-mediated self-activating Huisgen [3+2] cycloadditon as the key steps, and exhibited a 10-fold enhanced affinity to a phosphorylated peptide, a truncated peptide analog of the Grb2-SH2-interacting phosphoproteins. A stronger interaction with the target phosphorylated proteins gave this cyclic analog cytotoxic activity in A431 cells. © 2013 The Royal Society of Chemistry.
- リンク情報
- ID情報
-
- DOI : 10.1039/c3mb25462c
- ISSN : 1742-206X
- ISSN : 1742-2051
- eISSN : 1742-2051
- PubMed ID : 23403766
- SCOPUS ID : 84875833811