Inhibitory effects of KHG26377 on glutamate dehydrogenase activity in cultured islets.

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 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.

• Publication year

  2010

• Venue

  BMB Reports

• Publication date

  2010-04-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.5483/BMBREP.2010.43.4.245PMID 20423608
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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