Yang, Seung-Ju Hahn, Hoh-Gyu Choi, Soo Young Cho, Sung-Woo 2024-01-20T19:31:54Z 2024-01-20T19:31:54Z 2021-09-02 2010-04-30 1976-6696 https://pubs.kist.re.kr/handle/201004/131530 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] English KOREAN SOCIETY BIOCHEMISTRY & MOLECULAR BIOLOGY INSULIN-SECRETION HYPERINSULINISM/HYPERAMMONEMIA SYNDROME REGULATORY MUTATIONS BINDING HYPERAMMONEMIA PROFILES SIRT4 Inhibitory effects of KHG26377 on glutamate dehydrogenase activity in cultured islets Article 10.5483/BMBRep.2010.43.4.245 1 BMB REPORTS, v.43, no.4, pp.245 - 249 BMB REPORTS 43 4 245 249 scie scopus kci ART001439147 000277292400003 2-s2.0-77953509705 Biochemistry & Molecular Biology Biochemistry & Molecular Biology Article INSULIN-SECRETION HYPERINSULINISM/HYPERAMMONEMIA SYNDROME REGULATORY MUTATIONS BINDING HYPERAMMONEMIA PROFILES SIRT4 Glutamate dehydrogenase Hyperinsulinism Inhibitor KHG26377