@misc{oai:repo.qst.go.jp:00073078, author = {Yamaguchi, Hiroshi and Sumi, Takuya and Kang, Jiyoung and Okada, Maki and Yamashiro, Keiichi and Tateno, Masaru and 山口 博司 and 岡田 真希}, month = {Nov}, note = {[Background] In this study, imaging agents for glutamate transporter were aimed to be developed. The off-target bindings were eliminated from the existing inhibitors by employing computational docking examinations and structural informatics techniques, which thereby led to discovery of PET imaging agents to monitor the distributions specific to GLT in the brain. [Methods] An in silico binding assay was performed by using our protein-ligand docking simulations, where tamoxifen, which binds to both GLT and ERα proteins, was employed as an initial probe for the analysis. [Result] As a result of our analysis, the GLT-binding derivatives, which were hindered to bind to ERα, were obtained as derivatives of tamoxifen and tetrahydrobenzopyran. [Outlook] Radiolabeling of the designed molecules obtained by our in silico binding assay is now being considered toward utilizing them as the PET imaging agents., 第58回日本核医学会学術総会}, title = {Development of imaging agents specific to GLT excluding the off-target binding}, year = {2018} }