論文 - 詳細
| RRC ID | 44300 |
|---|---|
| 著者 | Iwata T, Tanaka K, Tahara T, Nozaki S, Onoe H, Watanabe Y, Fukase K. |
| タイトル | A conformationally fixed analog of the peptide mimic Grb2-SH2 domain: synthesis and evaluation against the A431 cancer cell. |
| ジャーナル | Mol Biosyst |
| Abstract |
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. |
| 巻・号 | 9(5) |
| ページ | 1019-25 |
| 公開日 | 2013-5-1 |
| DOI | 10.1039/c3mb25462c |
| PMID | 23403766 |
| MeSH | Animals Binding, Competitive Cell Line, Tumor Cell Survival / drug effects Chemistry Techniques, Synthetic Cyclization Dose-Response Relationship, Drug GRB2 Adaptor Protein / chemistry* GRB2 Adaptor Protein / metabolism Humans Mice Mice, Inbred BALB C Mice, Nude Models, Chemical Molecular Mimicry Molecular Structure Neoplasms / drug therapy Neoplasms / metabolism Neoplasms / pathology Peptides / chemical synthesis Peptides / chemistry* Peptides / pharmacology Peptides, Cyclic / chemistry Peptides, Cyclic / metabolism Peptides, Cyclic / pharmacology Phosphoproteins / chemistry Phosphoproteins / metabolism Protein Conformation* Xenograft Model Antitumor Assays src Homology Domains* |
| IF | 3.336 |
| 引用数 | 4 |
| WOS 分野 | BIOCHEMISTRY & MOLECULAR BIOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | X(Twitter) |
| 各媒体での言及数の合計 | 1 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | A431(RCB0202) |