| RRC ID |
44528
|
| 著者 |
Okamoto K, Kodama K, Takase K, Sugi NH, Yamamoto Y, Iwata M, Tsuruoka A.
|
| タイトル |
Antitumor activities of the targeted multi-tyrosine kinase inhibitor lenvatinib (E7080) against RET gene fusion-driven tumor models.
|
| ジャーナル |
Cancer Lett
|
| Abstract |
RET gene fusions are recurrent oncogenes identified in thyroid and lung carcinomas. Lenvatinib is a multi-tyrosine kinase inhibitor currently under evaluation in several clinical trials. Here we evaluated lenvatinib in RET gene fusion-driven preclinical models. In cellular assays, lenvatinib inhibited auto-phosphorylation of KIF5B-RET, CCDC6-RET, and NcoA4-RET. Lenvatinib suppressed the growth of CCDC6-RET human thyroid and lung cancer cell lines, and as well, suppressed anchorage-independent growth and tumorigenicity of RET gene fusion-transformed NIH3T3 cells. These results demonstrate that lenvatinib can exert antitumor activity against RET gene fusion-driven tumor models by inhibiting oncogenic RET gene fusion signaling.
|
| 巻・号 |
340(1)
|
| ページ |
97-103
|
| 公開日 |
2013-10-28
|
| DOI |
10.1016/j.canlet.2013.07.007
|
| PII |
S0304-3835(13)00512-0
|
| PMID |
23856031
|
| MeSH |
Animals
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Transformation, Neoplastic / drug effects
Cell Transformation, Neoplastic / genetics
Cytoskeletal Proteins / genetics
Cytoskeletal Proteins / metabolism
Drug Screening Assays, Antitumor
Female
Humans
Mice
Mice, Inbred BALB C
Mice, Nude
NIH 3T3 Cells
Neoplasm Transplantation
Neoplasms / drug therapy*
Neoplasms / enzymology
Neoplasms / genetics
Oncogene Proteins, Fusion / antagonists & inhibitors*
Oncogene Proteins, Fusion / genetics
Oncogene Proteins, Fusion / metabolism
Phenylurea Compounds / pharmacology*
Protein Kinase Inhibitors / pharmacology
Proto-Oncogene Proteins c-ret / antagonists & inhibitors*
Proto-Oncogene Proteins c-ret / genetics
Proto-Oncogene Proteins c-ret / metabolism
Quinolines / pharmacology*
Signal Transduction
|
| IF |
7.36
|
| 引用数 |
126
|
|
WOS 分野
|
ONCOLOGY
|
| リソース情報 |
| ヒト・動物細胞 |
LC-2/ad(RCB0440) |
