Synthesis of glutamine transporter inhibitors regulating amino acids concentrations in neurotransmission system

调节神经传递系统氨基酸浓度的谷氨酰胺转运蛋白抑制剂的合成

• 批准号: 19510228
• 负责人: SHIMAMOTO Keiko
• 金额: $ 2.83万
• 依托单位: Suntory Institute for Bioorganic Research
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2007
• 资助国家: 日本
• 起止时间: 2007 至 2009
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-19510228/
• 关键词: グルタミン; トランスポーター; 阻害剤; グリア細胞; 立体配座固定; グルタミン酸; 中性アミノ酸; シスチン; ヘテロエクスチェンジ

Extracellular concentrations of amino acids and sugars are regulated by transporters. In order to elucidate physiological roles in neurotransmission system and substrate recognition mechanisms of these transporters, we synthesized selective inhibitors for neutral amino acid transporter (ASCT2) and glutamate-cyctine exchanger (xCT).

细胞外氨基酸和糖的浓度由转运体调节。为了阐明这些转运体在神经传递系统中的生理作用和底物识别机制，我们合成了中性氨基酸转运体（ASCT2）和谷氨酸-环素交换体（xCT）的选择性抑制剂。

项目成果

Glutamate transporter GLAST/EAAT1 directs cell surface expression of FXYD2/gamma subunit of Na, K-ATPase in human fetal astrocytes

谷氨酸转运蛋白 GLAST/EAAT1 指导人胎儿星形胶质细胞中 FXYD2/Na、K-ATPase γ 亚基的细胞表面表达

• 发表时间: 2007
• 期刊: Neurochem. Int. 50
• 作者: M. Gegelashvili;A. Rodriguez-Kern;L. Sung;K. Shimamoto;G. Gegelashvili
• 通讯作者: G. Gegelashvili

Regioselective Domino Metathesis of Unsymmetrical 7-Oxanorbornenes with Electron-Rich Vinyl Acetate toward Biologically Active Glutamate Analogues.

• DOI: 10.1002/ejoc.200900580
• 发表时间: 2009-11-01
• 期刊: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
• 影响因子: 2.8
• 作者: Oikawa, Masato;Ikoma, Minoru;Sasaki, Makoto;Gill, Martin B.;Swanson, Geoffrey T.;Shimamoto, Keiko;Sakai, Ryuichi
• 通讯作者: Sakai, Ryuichi

Low-affinity excitatory amino acid uptake in hipocampal astrocytes : A possible role of Na+/dicarboxylate cotransporters

海马星形胶质细胞中低亲和力兴奋性氨基酸摄取：Na /二羧酸盐协同转运蛋白的可能作用

• 发表时间: 2008
• 期刊: Glia 56
• 作者: M. Sasaki;K. Tsubone;K. Aoki;N. Akiyama;M. Shoji;M. Oikawa;R. Sakai;K. Shimamoto;A. T. Holten
• 通讯作者: A. T. Holten

Glutamate transporter blockers for elucidation of the function of excitatory neurotransmission systems

• DOI: 10.1002/tcr.20145
• 发表时间: 2008-01-01
• 期刊: CHEMICAL RECORD
• 影响因子: 6.6
• 作者: Shimamoto, Keiko

Improved synthesis and in vitro/in vivo activities of natural product-inspired, artificial glutamate analogs.

• DOI: 10.1016/j.bmc.2010.04.044
• 发表时间: 2010-06-01
• 期刊: BIOORGANIC & MEDICINAL CHEMISTRY
• 影响因子: 3.5
• 作者: Oikawa, Masato;Ikoma, Minoru;Sasaki, Makoto;Gill, Martin B.;Swanson, Geoffrey T.;Shimamoto, Keiko;Sakai, Ryuichi
• 通讯作者: Sakai, Ryuichi