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PET probe detecting non-small cell lung cancer susceptible to epidermal growth factor receptor tyrosine kinase inhibitor therapy.
Makino, Akira; Miyazaki, Anna; Tomoike, Ayaka; Kimura, Hiroyuki; Arimitsu, Kenji; Hirata, Masahiko; Ohmomo, Yoshiro; Nishii, Ryuichi; Okazawa, Hidehiko; Kiyono, Yasushi; Ono, Masahiro; Saji, Hideo.
Afiliación
  • Makino A; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Adachi-cho, Sakyo-ku, Kyoto 6068501, Japan; Biomedical Imaging Research Center (BIRC), University of Fukui, 23-3 Matsuoka-shimoaizuki, Eiheiji-cho, Yoshida-gun, Fukui 9101193, Japan. Electronic address: amakino@u-fukui.ac.jp
  • Miyazaki A; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Adachi-cho, Sakyo-ku, Kyoto 6068501, Japan.
  • Tomoike A; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Adachi-cho, Sakyo-ku, Kyoto 6068501, Japan.
  • Kimura H; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Adachi-cho, Sakyo-ku, Kyoto 6068501, Japan; Department of Analytical and Bioinorganic Chemistry, Kyoto Pharmaceutical University, Kyoto 6078414, Japan.
  • Arimitsu K; Department of Analytical and Bioinorganic Chemistry, Kyoto Pharmaceutical University, Kyoto 6078414, Japan.
  • Hirata M; Graduate School of Pharmaceutical Sciences, Osaka University of Pharmaceutical Sciences, Osaka 5691041, Japan.
  • Ohmomo Y; Graduate School of Pharmaceutical Sciences, Osaka University of Pharmaceutical Sciences, Osaka 5691041, Japan.
  • Nishii R; National Institute of Radiological Sciences, Chiba 2638555, Japan.
  • Okazawa H; Biomedical Imaging Research Center (BIRC), University of Fukui, 23-3 Matsuoka-shimoaizuki, Eiheiji-cho, Yoshida-gun, Fukui 9101193, Japan.
  • Kiyono Y; Biomedical Imaging Research Center (BIRC), University of Fukui, 23-3 Matsuoka-shimoaizuki, Eiheiji-cho, Yoshida-gun, Fukui 9101193, Japan.
  • Ono M; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Adachi-cho, Sakyo-ku, Kyoto 6068501, Japan.
  • Saji H; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Adachi-cho, Sakyo-ku, Kyoto 6068501, Japan. Electronic address: hsaji@pharm.kyoto-u.ac.jp.
Bioorg Med Chem ; 26(8): 1609-1613, 2018 05 01.
Article en En | MEDLINE | ID: mdl-29478801
Tyrosine kinase inhibitors for epidermal growth factor receptor (EGFR-TKIs) are used as molecular targeted therapy for non-small cell lung cancer (NSCLC) patients. The therapy is applied to the patients having EGFR-primary L858R mutation, but drug tolerance caused by EGFR-secondary mutation is occurred within one and half years. For the non-invasive detection of the EGFR-TKIs treatment positive patients by positron emission tomograpy (PET) imagaing, fluorine-18 labeled thienopyrimidine derivative, [18F]FTP2 was newly synthesized. EGFR inhibition assay, cell uptake study, and blocking study indicated [18F]FTP2 binds with high and selective affinity for EGFR with L858R mutation, and not with L858R/T790M dual mutations. On animal PET study using tumor bearing mice, H3255 cells expressing L858R mutated EGFR was more clearly visualized than H1975 cells expressing L858R/T790M dual mutated EGFR. [18F]FTP2 has potential for detecting NSCLC which is susceptible to EGFR-TKI treatment.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Carcinoma de Pulmón de Células no Pequeñas / Radiofármacos / Inhibidores de Proteínas Quinasas / Tomografía de Emisión de Positrones / Receptores ErbB / Neoplasias Pulmonares Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Carcinoma de Pulmón de Células no Pequeñas / Radiofármacos / Inhibidores de Proteínas Quinasas / Tomografía de Emisión de Positrones / Receptores ErbB / Neoplasias Pulmonares Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article Pais de publicación: Reino Unido