Structural insights into the high selectivity of the anti-diabetic drug mitiglinide
Frontiers in pharmacology(2022)
摘要
Mitiglinide is a highly selective fast-acting anti-diabetic drug that inhibits pancreatic KATP channels to induce insulin secretion. However, how mitiglinide binds KATP channels remains unknown. Here, we show the cryo-EM structure of the SUR1 subunit in complex with mitiglinide. The structure reveals that mitiglinide binds inside the common insulin secretagogue-binding site in the transmembrane domain of SUR1, locking SUR1 in a NBD-separated inward-facing conformation. The detailed structural analysis uncovers the molecular basis of the high selectivity of mitiglinide.
### Competing Interest Statement
The authors have declared no competing interest.
更多查看译文
关键词
K-ATP,SUR1,mitiglinide,insulin secretagogues,ABC transporter,diabetes
AI 理解论文
溯源树
样例
![](https://originalfileserver.aminer.cn/sys/aminer/pubs/mrt_preview.jpeg)
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要