| 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
|
| リソース情報 |
| ヒト・動物細胞 |
A431(RCB0202) |
