Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling

被引:17
作者
Olsen, Reid H. J. [1 ]
English, Justin G. [2 ]
机构
[1] Exscientia PLC, GPCR Pharmacol, Oxford Sci Pk,Schrodinger Bldg, Oxford OX4 4GE, England
[2] Univ Utah, Sch Med, Dept Biochem, Salt Lake City, UT 84132 USA
关键词
BERKY; biosensor; BRET; FRET; functional selectivity; G protein coupled receptors; G proteins; GEMTA; GPCR; signalling bias; SPASM; transducerome; TRUPATH; MEDIATED ACTIVATION; CELLS; ALPHA; ASSAY; SPECIFICITY; SUBUNITS; G(S);
D O I
10.1111/bph.15962
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Enzymatic and cellular signalling biosensors are used to decipher the activities of complex biological systems. Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in the human body, are plentiful and vary in utility, form and function. Their applications have continually expanded our understanding of this important protein class. Here, we briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric signalling complexes.
引用
收藏
页码:1433 / 1443
页数:11
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