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j.nucmedbio.2014.10.006.pdf | 683.79 kB | Adobe PDF | 見る/開く |
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dc.contributor.author | Temma, Takashi | en |
dc.contributor.author | Nishigori, Kantaro | en |
dc.contributor.author | Onoe, Satoru | en |
dc.contributor.author | Sampei, Sotaro | en |
dc.contributor.author | Kimura, Ikuo | en |
dc.contributor.author | Ono, Masahiro | en |
dc.contributor.author | Saji, Hideo | en |
dc.contributor.alternative | 天滿, 敬 | ja |
dc.contributor.alternative | 佐治, 英郎 | ja |
dc.date.accessioned | 2015-02-12T07:39:55Z | - |
dc.date.available | 2015-02-12T07:39:55Z | - |
dc.date.issued | 2015-02 | - |
dc.identifier.issn | 0969-8051 | - |
dc.identifier.uri | http://hdl.handle.net/2433/193665 | - |
dc.description.abstract | 【Introduction】Cancer-associated adipocytes metabolically interact with adjacent cancer cells to promote tumor proliferation and metastasis. Fatty acid binding protein 4 (FABP4) participates in this interaction, and is gathering attention as a therapeutic and diagnostic target. Positron emission tomography (PET) is a useful diagnostic method that enables noninvasive in vivo quantitative imaging of biofunctional molecules with probes labeled with positron-emitting radioisotopes. Here a novel 18F labeled probe for PET FABP4 imaging developed through dedicated drug design from a radioiodinated probe we recently reported is evaluated in vitro and in vivo.【Methods】We designed the [18F]-labeled FTAP1 and FTAP3 probe, composed of a single or triple oxyethylene linker and a triazolopyrimidine scaffold derived from an FABP4 inhibitor. FABP4 binding affinities for chemically synthesized FTAP1 and FTAP3 were measured using FABP4 and 8-anilino-1-naphthalene sulfonic acid. Cell membrane permeability was measured using a commercially available plate assay system. After radiosynthesis, [18F]FTAP1 affinity and selectivity were evaluated using immobilized FABP3, FABP4, and FABP5. Cell uptake was investigated using differentiated adipocytes expressing FABP4 with inhibitor treatment. Following biodistribution studies in C6 glioblastoma-bearing mice, ex vivo autoradiography and immunohistochemistry were performed using thin sliced tumor sections. PET/CT imaging was then performed on C6 tumor bearing mice.【[Results】FTAP1 showed high FABP4 affinity (Ki = 68 ± 8.9 nM) and adequate cell permeability. [18F]FTAP1 with ≥ 98% radiochemical purity was shown to selectively bind to FABP4 (16.3- and 9.3-fold higher than for FABP3 and FABP5, respectively). [18F]FTAP1 was taken up by FABP4 expressing cells, and this uptake could be blocked by an inhibitor, indicating very low non-specific cell binding. [18F]FTAP1 showed high tumor accumulation, which demonstrates its potential use for in vivo tumor PET imaging, and the intratumoral radioactivity distribution corresponded to the FABP4 expression profile.【Conclusion】][18F]FTAP1 is a promising PET probe to target FABP4. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier Inc. | en |
dc.rights | © 2014 Elsevier Inc. | en |
dc.rights | この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 | ja |
dc.rights | This is not the published version. Please cite only the published version. | en |
dc.subject | Fatty acid binding protein 4 | en |
dc.subject | Radiolabeled probe | en |
dc.subject | Positron emission tomography | en |
dc.subject | PET | en |
dc.subject | Nuclear imaging | en |
dc.title | Radiofluorinated probe for PET imaging of fatty acid binding protein 4 in cancer. | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA10864894 | - |
dc.identifier.jtitle | Nuclear medicine and biology | en |
dc.identifier.volume | 42 | - |
dc.identifier.issue | 2 | - |
dc.identifier.spage | 184 | - |
dc.identifier.epage | 191 | - |
dc.relation.doi | 10.1016/j.nucmedbio.2014.10.006 | - |
dc.textversion | author | - |
dc.identifier.pmid | 25457456 | - |
dcterms.accessRights | open access | - |
出現コレクション: | 学術雑誌掲載論文等 |
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