Reference - Detail
| RRC ID | 31880 |
|---|---|
| Author | Fukuda N, Honda S. |
| Title | Rapid evaluation of tyrosine kinase activity of membrane-integrated human epidermal growth factor receptor using the yeast Gγ recruitment system. |
| Journal | ACS Synth Biol |
| Abstract |
Epidermal growth factor receptor (EGFR) is a member of the receptor tyrosine kinase family and plays key roles in the regulation of fundamental cellular processes, including cell proliferation, migration, differentiation, and survival. Deregulation of EGFR tyrosine kinase activity is involved in the development and progression of human cancers. In the present study, we attempted to develop a method to evaluate the tyrosine kinase activity of human EGFR using the yeast Gγ recruitment system. Autophosphorylation of tyrosine residues on the cytoplasmic tail of EGFR induces recruitment of Grb2-fused Gγ subunits to the inner leaflet of the plasma membrane in yeast cells, which leads to G-protein signal transduction and activation of downstream signaling events, including mating and diploid cell growth. We demonstrate that our system is applicable for the evaluation of tyrosine kinase inhibitors, which are regarded as promising drug candidates to prevent the growth of tumor cells. This approach provides a rapid and easy-to-use tool to select EGFR-targeting tyrosine kinase inhibitors that are able to permeate eukaryotic membranes and function in intracellular environments. |
| Volume | 4(4) |
| Pages | 421-9 |
| Published | 2015-4-17 |
| DOI | 10.1021/sb500083t |
| PMID | 25006755 |
| MeSH | ErbB Receptors / genetics ErbB Receptors / metabolism* GRB2 Adaptor Protein / genetics GRB2 Adaptor Protein / metabolism* GTP-Binding Protein gamma Subunits / genetics GTP-Binding Protein gamma Subunits / metabolism* Humans Recombinant Fusion Proteins / genetics Recombinant Fusion Proteins / metabolism* Saccharomyces cerevisiae / genetics* Saccharomyces cerevisiae / metabolism* |
| IF | 4.411 |
| Times Cited | 4 |
| WOS Category | BIOCHEMICAL RESEARCH METHODS |
| 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 | 4 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| DNA material | pco12 EGFR (RDB01276) |