Abstract
EML4-ALK is a fusion-type protein tyrosine kinase that is generated in human non-small-cell lung cancer (NSCLC) as a result of a recurrent chromosome inversion, inv (2)(p21p23). Although mouse 3T3 fibroblasts expressing human EML4-ALK form transformed foci in culture and s.c. tumors in nude mice, it has remained unclear whether this fusion protein plays an essential role in the carcinogenesis of NSCLC. To address this issue, we have now established transgenic mouse lines that express EML4-ALK specifically in lung alveolar epithelial cells. All of the transgenic mice examined developed hundreds of adenocarcinoma nodules in both lungs within a few weeks after birth, confirming the potent oncogenic activity of the fusion kinase. Although such tumors underwent progressive enlargement in control animals, oral administration of a small-molecule inhibitor of the kinase activity of ALK resulted in their rapid disappearance. Similarly, whereas i.v. injection of 3T3 cells expressing EML4-ALK induced lethal respiratory failure in recipient nude mice, administration of the ALK inhibitor effectively cleared the tumor burden and improved the survival of such animals. These data together reinforce the pivotal role of EML4-ALK in the pathogenesis of NSCLC in humans, and they provide experimental support for the treatment of this intractable cancer with ALK inhibitors.
MeSH Terms
3T3 Cells
Animals
Carcinoma, Non-Small-Cell Lung/drug therapy,enzymology,pathology
Disease Models, Animal
Humans
Lung Neoplasms/drug therapy,enzymology,pathology
Mice
Mice, Transgenic
Oncogene Proteins, Fusion/antagonists & inhibitors,genetics,metabolism
Protein Kinase Inhibitors/pharmacology,therapeutic use
Chemicals
EML4-ALK fusion protein, human
Oncogene Proteins, Fusion
Protein Kinase Inhibitors
Authors & Affiliations
12 authors, click to expand affiliations / ORCID
Soda Manabu
Divisions of Functional Genomics and Pulmonary Medicine, Jichi Medical University, Tochigi 329-0498, Japan.
Takada Shuji
Takeuchi Kengo
Choi Young Lim
Enomoto Munehiro
Ueno Toshihide
Haruta Hidenori
Hamada Toru
Yamashita Yoshihiro
Ishikawa Yuichi
Sugiyama Yukihiko
Mano Hiroyuki
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