Journal
BMB REPORTS
Volume 43, Issue 4, Pages 245-249Publisher
KOREAN SOCIETY BIOCHEMISTRY & MOLECULAR BIOLOGY
DOI: 10.5483/BMBRep.2010.43.4.245
Keywords
Glutamate dehydrogenase; Hyperinsulinism; Inhibitor; KHG26377
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Funding
- National Research Foundation of Korea [2009-0073270]
- Asan Institute for Life Sciences [2009-010]
- National Research Foundation of Korea [2009-0073270] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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GDH has been known to be related with hyperinsulinism-hyperammonemia 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 V-max of GDH was decreased by 59% whereas K-m 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. [BMB reports 2010; 43(4): 245-249]
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