Nature Communications (Feb 2018)
A secondary RET mutation in the activation loop conferring resistance to vandetanib
- Takashi Nakaoku,
- Takashi Kohno,
- Mitsugu Araki,
- Seiji Niho,
- Rakhee Chauhan,
- Phillip P. Knowles,
- Katsuya Tsuchihara,
- Shingo Matsumoto,
- Yoko Shimada,
- Sachiyo Mimaki,
- Genichiro Ishii,
- Hitoshi Ichikawa,
- Satoru Nagatoishi,
- Kouhei Tsumoto,
- Yasushi Okuno,
- Kiyotaka Yoh,
- Neil Q. McDonald,
- Koichi Goto
Affiliations
- Takashi Nakaoku
- Division of Genome Biology, National Cancer Center Research Institute
- Takashi Kohno
- Division of Genome Biology, National Cancer Center Research Institute
- Mitsugu Araki
- Advanced Institute for Computational Science, RIKEN
- Seiji Niho
- Department of Thoracic Oncology, National Cancer Center Hospital East
- Rakhee Chauhan
- Signaling and Structural Biology Laboratory, The Francis Crick Institute
- Phillip P. Knowles
- Signaling and Structural Biology Laboratory, The Francis Crick Institute
- Katsuya Tsuchihara
- Division of Translational Genomics, Exploratory Oncology Research and Clinical Trial Center, National Cancer Center
- Shingo Matsumoto
- Division of Translational Genomics, Exploratory Oncology Research and Clinical Trial Center, National Cancer Center
- Yoko Shimada
- Division of Genome Biology, National Cancer Center Research Institute
- Sachiyo Mimaki
- Division of Translational Genomics, Exploratory Oncology Research and Clinical Trial Center, National Cancer Center
- Genichiro Ishii
- Division of Pathology, Exploratory Oncology Research and Clinical Trial Center, National Cancer Center
- Hitoshi Ichikawa
- Division of Translational Genomics, Exploratory Oncology Research and Clinical Trial Center, National Cancer Center
- Satoru Nagatoishi
- Medical Proteomics Laboratory, Institute of Medical Science, The University of Tokyo
- Kouhei Tsumoto
- Medical Proteomics Laboratory, Institute of Medical Science, The University of Tokyo
- Yasushi Okuno
- Department of Clinical System Onco-Informatics, Graduate School of Medicine, Kyoto University
- Kiyotaka Yoh
- Department of Thoracic Oncology, National Cancer Center Hospital East
- Neil Q. McDonald
- Signaling and Structural Biology Laboratory, The Francis Crick Institute
- Koichi Goto
- Department of Thoracic Oncology, National Cancer Center Hospital East
- DOI
- https://doi.org/10.1038/s41467-018-02994-7
- Journal volume & issue
-
Vol. 9,
no. 1
pp. 1 – 9
Abstract
Mechanisms of acquired resistance to RET tyrosine kinase inhibitors in lung cancers are largely unknown. Here, the authors report in a lung adenocarcinoma patient harboring a CCDC6-RET mutation in the RET kinase (S904F) that results in resistance to the kinase inhibitor vandetanib by increasing the ATP affinity and autophosphorylation activity of RET kinase.
