GlcNAc-硒唑啉抑制 OGA。
OGA inhibition by GlcNAc-selenazoline.
机构信息
Department of Science Education-Chemistry Major, Daegu University, Gyeongbuk 712-714, Republic of Korea.
出版信息
Bioorg Med Chem. 2010 Oct 1;18(19):7058-64. doi: 10.1016/j.bmc.2010.08.010. Epub 2010 Aug 11.
Abstract
The title compound, which differs from the powerful O-GlcNAcase (OGA) inhibitor GlcNAc-thiazoline only at the chalcogen atom (Se for S), is a much weaker inhibitor in a direct OGA assay. In human cells, however, the selenazoline shows comparable ability to induce hyper-O-GlcNAc-ylation, and the two show similar reduction of insulin-stimulated translocation of glucose transporter 4 in differentiated 3T3 adipocytes.
摘要
标题化合物与强效 O-GlcNAcase（OGA）抑制剂 GlcNAc-噻唑啉仅在硫属原子（Se 代替 S）上有所不同，在直接 OGA 测定中，它是一种弱得多的抑制剂。然而，在人类细胞中，硒唑啉显示出相当的诱导高 O-GlcNAc 化的能力，并且两者在分化的 3T3 脂肪细胞中显示出相似的减少胰岛素刺激的葡萄糖转运蛋白 4 的易位。
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