The probe design strategy of post-FDG tumor diagnostic agents based on the functional biomolecule expression analysis of human cultured cells

2011 Fiscal Year Final Research Report

• Project/Area Number: 21659286
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Single-year Grants
• Research Field: Radiation science
• Research Institution: Kanazawa University
• Principal Investigator: KAWAI Keiichi 金沢大学, 保健学系, 教授 (30204663)
• Co-Investigator(Renkei-kenkyūsha): TAMAI Ikumi 金沢大学, 薬学系, 教授 (20155237) ; FUJIBAYASHI Yasuhisa 独立行政法人放射線医学総合研究所, 分子イメージング研究センター, センター長 (50165411)
• Project Period (FY): 2009 – 2011
• Keywords: ヒト培養細胞 / 機能性分子発現解析 / ポストFDG / 腫瘍診断薬 / PET製剤 / 腫瘍集積性 / アミノ酸トランスポータ / 設計戦略

Research Abstract

While searching this research for the functional biomolecule used by the database for the gene expression level of the human cultured cells for evaluation of imaging probes, and it has high-expressed to the tumor cell beforehand, the amino acid derivatives are especially taken up also in a post-FDG candidate probe, and the accumulation mechanism of the labeled amino acids which shows high affinity to the amino acid transporters to which high revelation is specifically accepted by a tumor was examined in detail, and the validity of the design strategy was evaluated from correlation with amino acid transporter gene expression and tumor accumulation of the probes.

Research Products

• [Journal Article] Down-regulation of Calcium/calmodulin-dependent Protein Kinase Kinase 2 by Androgen Deprivation Induces Castration-resistant ProstateCancer (2012)
  • Author(s): Shima T., Mizokami A., Miyagi T., Kawai K., Izumi K., Kumaki M., Ofude M., Zhang J., Keller E. T. and Namiki M
  • Journal Title: Prostate in press Volume: (in press)
• [Journal Article] Cerebral Oxygen Metabolism of Rats using Injectable O^<15>-Oxygen with a Steady-state Method (2012)
  • Author(s): Kobayashi M., Mori T., Kiyono Y., Tiwari V., Maruyama R., Kawai K., Okazawa H
  • Journal Title: J. Cereb. Blood Flow Metab Volume: 32 Pages: 33-40
• [Journal Article] Appropriate Parameters of Ordered-Subset Expectation Maximization Algorithm on Measurement of Myocardial Blood Flow and Oxygen Consumption with C^<11>-Acetate PET (2012)
  • Author(s): Kobayashi M., Mori T., Kiyono Y., TsujikawaT., Maruyama R., Higaki Y., Shikano N., Nishii R., Kawai K., Kudo T., Okazawa H
  • Journal Title: Nucl. Med. Commun Volume: 33 Pages: 130-138
• [Journal Article] Functional Characterization of Apical Transporters Expressed in Rat Proximal Tubular Cells(PTCs) in Primary Culture (2011)
  • Author(s): Nakanishi T., Fukushi A., Sato M., Yoshifuji M., Gose T., Shirasaka Y., Ohe K., Kobayashi M., Kawai K., Tamai I
  • Journal Title: Mol. Pharm Volume: 8 Pages: 2142-2150
• [Journal Article] Putative Transport Mechanism and Intracellular Fate of Anti-18F-FACBC(Trans-1-amino-3-F^<18>-fluorocyclobutanecarboxylic Acid) in Human Prostate Cancer (2011)
  • Author(s): Okudaira H., Shikano N., Nishii R., Miyagi T., Yoshimoto M., Kobayashi M., Ohe K., Nakanishi T., Tamai I., Namiki M., Kawai K
  • Journal Title: J. Nucl. Med Volume: 52 Pages: 822-829
• [Journal Article] Differential Expression of FosB, c-Fos, and Zif268 in Forebrain Regions after Acute or Chronic L-DOPA Treatment in a RatModel of Parkinson's Disease (2011)
  • Author(s): Ebihara K., Ishida Y., Takeda R., Abe H., Matsuo H., Kawai K., Magata Y., Nishimori T
  • Journal Title: Neurosci. Lett Volume: 496 Pages: 90-94
• [Journal Article] Development of an H_2^<15> O Steady-state Method Combining a Bolus and Slow Increasing Injection with a Multiprogramming Syringe Pump (2011)
  • Author(s): Kobayashi M., Kiyono Y., Maruyama R., MoriT., Kawai K., Okazawa H
  • Journal Title: J. Cereb. Blood Flow Metab Volume: 31 Pages: 527-534
• [Journal Article] Radioiodinated 4-Iodo-L-meta-tyrosine, a System L Selective Artificial Amino Acid : Molecular Design and Transport Characterizationin in Chinese Hamster Ovary Cells(CHO-K_1 Cells) (2010)
  • Author(s): Shikano N., Kotani T., Nakajima S., OguraM., Nakazawa S., Sagara J., Kobayashi M., Nakazawa S., Baba T., Yamaguchi N., Kubota N., Iwamura Y., Kawai K
  • Journal Title: Nucl. Med. Biol Volume: 37 Pages: 903-910
• [Journal Article] Comparison of theTranscellular Transport of FDG and D-Glucose by the Kidney Epithelial Cell Line LLC-PK_1 (2010)
  • Author(s): Kobayashi M., Shikano N., Nishii R., KiyonoY., Araki H., Nishi K., Oh M., Okudaira H., Ogura M., Yoshimoto M., Okazawa H., Fujibayashi Y., Kawai K
  • Journal Title: Nucl. Med. Commun Volume: 31 Pages: 141-146
• [Journal Article] Uptake of 3-[ I^<125>] Iodo-α-methyl-L-tyrosine intoColon Cancer DLD-1 Cells : Characterization and Inhibitory Effect of Natural Amino Acids and Amino Acid-likeDrugs (2010)
  • Author(s): Shikano N., Ogura M., Okudaira H., Nakajima S., Kotani T., Kobayashi M., Nakazawa S., Baba T., Yamaguchi N., Kubota N., Iwamura Y., Kawai K
  • Journal Title: Nucl. Med. Biol Volume: 37 Pages: 197-204
• [Journal Article] Stimulation of I^<125>-3-Iodo-alpha-methyl-L-tyrosine in Chinese Hamster Ovary(CHO-K1) Cells by Tyrosine Esters (2010)
  • Author(s): Shikano N., Ogura M., Sagara J., Nakajima S., Kobayashi M., Baba T., Yamaguchi N., Iwamura Y., Kubota N., Kawai K
  • Journal Title: Nucl. Med. Biol Volume: 37 Pages: 189-196
• [Journal Article] Evaluation of Radioiodinated Vesamicol Analogs for Sigma Receptor Imaging in Tumor and Radionuclide ReceptorTherapy (2009)
  • Author(s): Ogawa K., Shiba K., Akhter N., YoshimotoM., Washiyama K., Kinuya S., Kawai K., Mori H
  • Journal Title: Cancer Sci Volume: 100 Pages: 2188-2192
• [Journal Article] Improvement of N-isopropyl-p-[ I^<123>] iodoamphetamine Cerebral Accumulation by Competitive Displacement of Serum Protein Binding with Amino-Acid Infusion (2009)
  • Author(s): Kuga N., Shikano N., Takamura N., Nishii R., Yamasaki K., Kobayashi M., Nagamachi S., Tamura S., Kawai K
  • Journal Title: J. Nucl. Me Volume: 50 Pages: 1378-1383
• [Journal Article] Intracellular Reactions Affecting 2-Amino-4-([ C^<11>] methylthio) butyricacid([ C^<11>] Methionine) Response to Carbon Ion Radiotherapy in C10 Glioma Cells (2009)
  • Author(s): Uehara T., Nakagawa M., Takai N., Koike S., Furusawa Y., Ando K., Kawai K., Akizawa H., Irie T., Arano Y
  • Journal Title: Nucl. Med. Biol Volume: 36 Pages: 985-991
• [Presentation] Transport Mechanism of Trans-1-amino-3-F^<18>-fluorocyclobutanecarboxylic Acid(F^<18>-FACBC) in Human Prostate Cancer (2012)
  • Author(s): Okudaira H., Shikano N., Nishii R., Miyagi T., Yoshimoto M., Kobayashi M., Ohe K., Nakanishi T., Namiki M., Tamai I., Kawai K
  • Organizer: International Symposium on Past, Present and Future of Molecular Pharmacokinetics
  • Place of Presentation: University of Tokyo(Japan)
  • Year and Date: 2012-01-16
• [Presentation] 放射性医薬品の開発・体内動態制御と個別化医療 (2011)
  • Author(s): 川井恵一
  • Organizer: バイオセミナー"未来へのバイオ技術"月例会
  • Place of Presentation: バイオインダストリー協会(東京都)
  • Year and Date: 2011-12-05
• [Presentation] Usefulness of Double Tracer PET Study using[ F^<18>] FDG and Amino Acid Radiotracer,[ C^<11>] MeAIB, in the Diagnosis of Mediastinal Diseases (2011)
  • Author(s): Higashi T., Nishii R., Kagawa S., Kishibe Y., Takahashi M., Kobayashi M., Kawai K
  • Organizer: The Society of Nuclear Medicine 58th Annual Meeting
  • Place of Presentation: San Antonio Convention Center(U. S. A.)
  • Year and Date: 2011-06-04
• [Presentation] Effects of Antiangiogenic Drugs on FDG, FLT and Methionine Uptake in LS180 and HUVEC (2010)
  • Author(s): Yoshimoto M., Kinuya S., Kawai K
  • Organizer: The Society of Nuclear Medicine 57th Annual Meeting
  • Place of Presentation: Salt Palace Convention Center(U. S. A.)
  • Year and Date: 2010-06-05
• [Presentation] Accumulation and Transport Mechanism of Anti-1-Amino-3-[ F^<18>] fluorocyclobutane-1-carboxylic Acid in Representative Human Carcinomas (2010)
  • Author(s): Kobayashi M., Kagawa S., Nishii R., Takahashi F., Ohe K., Yoshimoto M., Shikano N., Higashi T., Nagamachi S., KawaiK
  • Organizer: The Society of Nuclear Medicine 57th Annual Meeting
  • Place of Presentation: Salt Palace Convention Center(U. S. A.)
  • Year and Date: 2010-05-06
• [Presentation] Assessment of Efficacy of[ C^<11>]-MeAIB PET as a Biomarker of the System A Amino Acid Transport : Comparison with[ 11C^<11>]-MET PET and[ F^<18>]-FDG PET in the Patients with Glioblastoma Multiforme (2010)
  • Author(s): Nishii R., Higashi T., Kagawa S., Kishibe Y., Takahashi M., Kobayashi M., Kawai K., Nagamachi S
  • Organizer: The Society of Nuclear Medicine 57th Annual Meeting
  • Place of Presentation: Salt Palace Convention Center(U. S. A.)
  • Year and Date: 2010-05-06
• [Presentation] 放射性医薬品の体内動態制御とターゲティングコンファーマティヴ個別化医療 (2010)
  • Author(s): 川井恵一
  • Organizer: 第66回日本放射線技術学会総会学術大会
  • Place of Presentation: パシフィコ横浜会議センター(神奈川県)
  • Year and Date: 2010-04-09
• [Presentation] Trans-stimulation of 3-I-125-Iodo-alpha-methyl-L-tyrosine Uptake into Chinese Hamster Ovary Cell by Amino Acid Esters (2009)
  • Author(s): Shikano N., Ogura M., Nakajima S., YamaguchiN., Kubota N., Iwamura Y., Kawai K
  • Organizer: 18th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: Edmonton's Shaw Conference Centre(Canada)
  • Year and Date: 2009-07-12
• [Presentation] Uptake Inhibition of 3-I-125-Iodoalpha-methyl-L-tyrosine into Colon Cancer DLD-1 Cell by Amino Acid Like Drugs (2009)
  • Author(s): Ogura M., Shikano N., Nakajima S., Yamaguchi N., Kubota N., Iwamura Y., KawaiK
  • Organizer: 18th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: Edmonton's Shaw Conference Centre(Canada)
  • Year and Date: 2009-07-12
• [Presentation] Mechanism of Renal FDG Transcellular Transport and Cellular Accumulation using LLC-PK_1 Cells (2009)
  • Author(s): Kobayashi M., Araki H., Nishi K., Shikano N., Kiyono Y., Nishii R., Fujibayashi Y., Okazawa H., Kawai K
  • Organizer: The Society of Nuclear Medicine 56th Annual Meeting
  • Place of Presentation: Metro TorontoConvention Center(U. S. A.)
  • Year and Date: 2009-06-13
• [Presentation] Mechanism of Renal FDG Transcellular Transport and Cellular Accumulation using LLC-PK_1 Cells (2009)
  • Author(s): Kobayashi M., Araki H., Nishi K., Shikano N., Kiyono Y., Nishii R., Fujibayashi Y., Okazawa H., Kawai K
  • Organizer: The Society of Nuclear Medicine 56th Annual Meeting
  • Place of Presentation: Metro Toronto Convention Center(U. S. A.)
  • Year and Date: 2009-06-13
• [Presentation] Comparison of System A and System L Amino Acid Transports in Human Pancreas with C-11 MeAIB and C-11 MET PET Study (2009)
  • Author(s): Nishii R., Kagawa S., Higashi T., Kishibe Y., Iwasaki T., Uehara T., Kobayashi M., Nagamachi S., Arano Y., Kawai K
  • Organizer: The Society of Nuclear Medicine 56th Annual Meeting
  • Place of Presentation: Metro Toronto Convention Center(U. S. A.)
  • Year and Date: 2009-06-13
• [Presentation] Estimation of Sensitivity to Gefitinib with Radioiodinated IPHY in Lung Cancer (2009)
  • Author(s): Yoshimoto M., Hirata M., Kawai K., OhmomoY
  • Organizer: The Society of Nuclear Medicine 56th Annual Meeting
  • Place of Presentation: Metro Toronto Convention Center(U. S. A.)
  • Year and Date: 2009-06-13
• [Remarks] 金沢大学研究紹介データベース
  • URL: http://kurt.kanazawa-u.ac.jp/souran_ku/info.php?teacher_id=488
• [Remarks] 金沢大学医薬保健研究域保健学系量子医療技術学講座川井研究室
  • URL: http://kawai.w3.kanazawa-u.ac.jp/index.html