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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2010.1
- 수록면
- 245 - 249 (5page)
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초록· 키워드
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GDH has been known to be related with hyperinsulinismhyperammonemia syndrome. We have screened new drugs with a view to developing effective drugs modulating GDH activity. In the present work, we investigated the effects of a new drug, KHG26377 on glutamate formation and GDH activity in cultured rat islets. When KHG26377 was added to the culture medium for 24 h prior to kinetic analysis, the Vmax of GDH was decreased by 59% whereas Km is not significantly changed. The concentration of glutamate decreased by 50%and perfusion of islets with KHG26377 reduced insulin release by up to 55%. Our results show that KHG26377 regulates insulin release by inhibiting GDH activity in primary cultured islets and support the previous studies for the connection between GDH activity and insulin release. Further studies are required to determine in vivo effects and pharmacokinetics of the drug.
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참고문헌 (27)
참고문헌 신청
Choi, M. M. / 2008 / Small-interfering-RNA-mediated silencing of human glutamate dehydrogenase induces apoptosis in neuroblastoma cells / Biotechnol. Appl. Biochem. 51:107~110
Heinrikson, R. L. / 1984 / Amino acid analysis by reverse-phase high-performance liquid chromatography: precolumn derivatization with phenylisothiocyanate / Anal. Biochem. 136:65~74
Herbert, V. / 1965 / Coated charcoal immunoassay of insulin / J. Clin. Endocrinol. Metab. 25:1375~1384
Lee, E. Y. / 2001 / Identification of GTP binding site of human glutamate dehydrogenase using cassette mutagenesis and photoaffinity labeling / J. Biol. Chem. 276:47930~47936
Yoon, H. Y. / 2002 / Importance of glutamate-279 for the coenzyme binding of human glutamate dehydrogenase / J. Biol. Chem. 277:41448~41454
Heinrikson, R. L. / 1984 / Amino acid analysis by reverse-phase high-performance liquid chromatography: precolumn derivatization with phenylisothiocyanate / Anal. Biochem. 136:65~74
Herbert, V. / 1965 / Coated charcoal immunoassay of insulin / J. Clin. Endocrinol. Metab. 25:1375~1384
Lee, E. Y. / 2001 / Identification of GTP binding site of human glutamate dehydrogenase using cassette mutagenesis and photoaffinity labeling / J. Biol. Chem. 276:47930~47936
Yoon, H. Y. / 2002 / Importance of glutamate-279 for the coenzyme binding of human glutamate dehydrogenase / J. Biol. Chem. 277:41448~41454
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