| Registro completo |
| Provedor de dados: |
OAK
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| País: |
Japan
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| Título: |
Improvement in the Properties of 3-Phenyl-3-trifluoromethyldiazirine Based Photoreactive Bis-Glucose Probes for GLUT4 Following Substitution on the Phenyl Ring
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| Autores: |
Hashimoto, Makoto
Yang, Jing
Hatanaka, Yasumaru
Sadakane, Yutaka
Nakagomi, Kazuya
Holman, Geoffrey David
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| Data: |
2002-07-01
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| Ano: |
2002
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| Palavras-chave: |
Photoaffinity label
Diazirine
Glucose transporter
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| Resumo: |
日本薬学会Chemical & pharmaceutical bulletin 50(7) p.1004-1006より転載
We have developed two novel 3-phenyl-3-trifluoromethyldiazirinyl bis-glucose derivatives to investigate the properties of the adipocyte glucose transporter GLUT4. These compounds were substituted by electron-with-drawing (iodo and nitro) groups on the aromatic ring of 3-phenyl-3-tritluoromethyldiazirine photophore and were found to be more photosensitive than compounds without such substituents. The compounds were used as inhibitors of insulin-stimulated glucose transport activity in order to assess half-maximal inhibition or relative affinity values for GLUT4. The affinities were found to be 60-130 times higher than the parent compound D-glu-cose. Because of the increased photo-reactivity and high affinity these compounds will be useful in studies directed at further elucidation of GLUT4 function.
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| Idioma: |
Inglês
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| Identificador: |
http://ir.obihiro.ac.jp/dspace/handle/10322/332
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| Editor: |
Pharmaceutical Society of Japan
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| Formato: |
application/pdf
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