Molecular design of amylase inhibitor based on the substrate recognition property of the enzyme

基于酶底物识别特性的淀粉酶抑制剂的分子设计

• 批准号: 21603001
• 负责人: KAWABATA Jun
• 金额: $ 3.16万
• 依托单位: Hokkaido University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2009
• 资助国家: 日本
• 起止时间: 2009 至 2011
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21603001/
• 关键词: α-アミラーゼ; 酵素阻害剤; 糖尿病; 分子設計; グルコシダーゼ阻害剤; α-アミラーゼ; 酵素阻害剤; 糖尿病; 分子設計; グルコシダーゼ阻害剤

Inhibition of the pancreaticα-amylase is useful for the treatment of obesity and diabetes mellitus. However, not many small molecule inhibitors are known for this enzyme due to its characteristic substrate recognition which recognizes chained glucoses. We used this characteristic mode of substrate recognition to design new small moleculeα-amylase inhibitors and synthesized them. These synthetic inhibitors revealed a useful property of the pancreaticα-amylase for further development of the inhibitor.

胰腺α-淀粉酶的抑制作用可用于治疗肥胖症和糖尿病。然而，由于识别链链葡萄糖的特征性底物识别，因此没有多少小分子抑制剂以这种酶而闻名。我们使用这种底物识别的特征模式来设计新的小分子α-淀粉酶抑制剂并合成它们。这些合成抑制剂揭示了胰腺α-淀粉酶的有用特性，用于进一步发展抑制剂。