Journal
TRENDS IN BIOCHEMICAL SCIENCES
Volume 40, Issue 2, Pages 79-87Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tibs.2014.12.005
Keywords
GPCR stabilization; ligand residence time; receptor residence time
Categories
Funding
- ShanghaiTech University
- Shanghai Municipal Government
Ask authors/readers for more resources
Traditionally, G protein-coupled receptor (GPCR) activity has been characterized by ligand properties including affinity (K-i), potency (IC50/EC50), efficacy (E-max), and kinetics (K-on/K-off). These properties are related to ligand residence time, a general index of drug-target interaction in vivo. Recent GPCR structure-function breakthroughs have all required ligand stabilization of the receptor in some manner, highlighting the natural instability of these important cell surface receptors. This research has initiated a new era of discovery that highlights the importance of ligand-receptor interactions beyond the traditional mindset. We propose that receptor stability is related to receptor folding and residence in the cell membrane, affording a new dimension that should be considered when studying receptor function.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available