化学
小分子
药物发现
DNA
组合化学
计算生物学
立体化学
生物化学
生物
作者
Shea L. Johnson,Galen Missig,Minghua Wang,Kosalvisal Ouk,Kailash C. Gupta,Hanh Nho Nguyen,May Fern Toh,Tammy Szu‐Yu Ho,David Gray,Hongjun Zhang,Yong Mi Choi-Sledeski,Claude Barberis,David J. Stone,Sokhom S. Pin,Jongwon Lim
标识
DOI:10.1016/j.bmcl.2024.129889
摘要
Studies have shown that disrupting the formation of the ligand-RET-GFRα complex could be an effective way of treating pain and itch. Compared to traditional high-throughput screens, DNA encoded libraries (DELs) have distinguished themselves as a powerful technology for hit identification in recent years. The present work demonstrates the use of DEL technology identifying compound 16 as the first GFRa2/GFRa3 small molecule inhibitor (0.1/0.2 μM respectively) selective over RET. This molecule represents an opportunity to advance the development of small-molecule inhibitors targeting the GFRα-RET interface for the treatment of pain and itch.
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