Inhibitory effects of KHG26377 on glutamate dehydrogenase activity in cultured islets

Title
Inhibitory effects of KHG26377 on glutamate dehydrogenase activity in cultured islets
Authors
양승주한호규최수영조성우
Keywords
Glutamate dehydrogenase; Hyperinsulinism; Inhibitor; KHG26377
Issue Date
2010-04
Publisher
BMB REPORTS
Citation
VOL 43, NO 4, 245-249
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/41314
ISSN
1976-6696
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KIST Publication > Article
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