当前位置: X-MOL 学术Drug. Discov. Today › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Releasing the technical 'shackles' on GPCR drug discovery: opportunities enabled by detergent-free polymer lipid particle (PoLiPa) purification.
Drug Discovery Today ( IF 6.5 ) Pub Date : 2020-08-21 , DOI: 10.1016/j.drudis.2020.08.006
J Daniel Hothersall 1 , Andrew Y Jones 1 , Tim R Dafforn 2 , Trevor Perrior 1 , Kathryn L Chapman 1
Affiliation  

G-protein-coupled receptor (GPCR) drug research is presently hindered by the technical challenges associated with generating purified receptors. Consequently, the application of critical modern discovery technologies has been limited, and the vast untapped opportunity for new GPCR-directed medicines is not being realised. A simple but transformative solution is to purify receptors without removing them from their native phospholipid environment by using polymer lipid particle (PoLiPa) technology, with reagents such as styrene-maleic acid co-polymer (SMA). Compared with contemporary detergent-based and stabilising mutagenesis methods, the PoLiPa approach is simple and generic and, therefore, offers huge advantages, with the potential to revolutionise GPCR research by facilitating the availability of the purified receptors that are required for structural biology, biophysical, and panning technologies.



中文翻译:


释放 GPCR 药物发现的技术“束缚”:无去垢剂聚合物脂质颗粒 (PoLiPa) 纯化带来的机遇。



G 蛋白偶联受体 (GPCR) 药物研究目前受到与生成纯化受体相关的技术挑战的阻碍。因此,关键的现代发现技术的应用受到限制,并且 GPCR 导向的新药物尚未实现巨大的未开发机会。一种简单但变革性的解决方案是使用聚合物脂质颗粒 (PoLiPa) 技术以及苯乙烯-马来酸共聚物 (SMA) 等试剂来纯化受体,而不将其从其天然磷脂环境中移除。与当代基于去污剂的稳定诱变方法相比,PoLiPa 方法简单且通用,因此具有巨大的优势,有可能通过促进结构生物学、生物物理、和平移技术。

更新日期:2020-08-21
down
wechat
bug