Reference - Detail
| RRC ID | 44300 |
|---|---|
| Author | Iwata T, Tanaka K, Tahara T, Nozaki S, Onoe H, Watanabe Y, Fukase K. |
| Title | A conformationally fixed analog of the peptide mimic Grb2-SH2 domain: synthesis and evaluation against the A431 cancer cell. |
| Journal | 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. |
| Volume | 9(5) |
| Pages | 1019-25 |
| Published | 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 |
| Times Cited | 4 |
| WOS Category | BIOCHEMISTRY & MOLECULAR BIOLOGY |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | X(Twitter) |
| Total number of mentions | 1 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | A431(RCB0202) |