Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden; Department of Organic and Physical Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Warsaw, Poland; Department of Medical Biochemistry and Microbiology, Uppsala University, Uppsala, Sweden.
Department of Physiology and Pharmacology, Molecular Pharmacology of GPCRs, Karolinska Institute, Stockholm, Sweden.
SLAS Discov. 2024 Sep;29(6):100174. doi: 10.1016/j.slasd.2024.100174. Epub 2024 Jul 29.
Bioluminescence- and fluorescence-based resonance energy transfer assays have gained considerable attention in pharmacological research as high-throughput scalable tools applicable to drug discovery. To this end, G protein-coupled receptors represent the biggest target class for marketed drugs, and among them, orphan G protein-coupled receptors have the biggest untapped therapeutic potential. In this review, the cases where biophysical methods, BRET and FRET, were employed for deorphanization and ligand discovery studies on orphan G protein-coupled receptors are listed and discussed.
基于生物发光和荧光的共振能量转移测定法在药理学研究中得到了相当大的关注，因为它们是适用于药物发现的高通量可扩展工具。为此，G 蛋白偶联受体是上市药物的最大靶标类别，其中，孤儿 G 蛋白偶联受体具有最大的未开发治疗潜力。在这篇综述中，列出并讨论了在孤儿 G 蛋白偶联受体的去孤儿化和配体发现研究中使用生物物理方法 BRET 和 FRET 的情况。
