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Ligand bias in receptor tyrosine kinase signaling
- Source :
- The Journal of Biological Chemistry
- Publication Year :
- 2020
- Publisher :
- Elsevier BV, 2020.
-
Abstract
- Ligand bias is the ability of ligands to differentially activate certain receptor signaling responses compared with others. It reflects differences in the responses of a receptor to specific ligands and has implications for the development of highly specific therapeutics. Whereas ligand bias has been studied primarily for G protein–coupled receptors (GPCRs), there are also reports of ligand bias for receptor tyrosine kinases (RTKs). However, the understanding of RTK ligand bias is lagging behind the knowledge of GPCR ligand bias. In this review, we highlight how protocols that were developed to study GPCR signaling can be used to identify and quantify RTK ligand bias. We also introduce an operational model that can provide insights into the biophysical basis of RTK activation and ligand bias. Finally, we discuss possible mechanisms underpinning RTK ligand bias. Thus, this review serves as a primer for researchers interested in investigating ligand bias in RTK signaling.
- Subjects :
- 0301 basic medicine
Cell signaling
bias coefficient
receptor
Cell Communication
Computational biology
Ligands
bias plot
Biochemistry
Receptor tyrosine kinase (RTK)
Receptor tyrosine kinase
GPCR Signaling
thermodynamics
03 medical and health sciences
Protein structure
protein conformation
Animals
Humans
cell signaling
Receptor
Molecular Biology
Rtk signaling
G protein-coupled receptor
dimerization
ligand functional selectivity
phosphotyrosine signaling
030102 biochemistry & molecular biology
biology
Ligand
Chemistry
JBC Reviews
fungi
mathematical modeling
Receptor Protein-Tyrosine Kinases
Cell Biology
ligand bias
dimer stability
Enzyme Activation
030104 developmental biology
receptor tyrosine kinase
biology.protein
signaling
Signal Transduction
Subjects
Details
- ISSN :
- 00219258
- Volume :
- 295
- Database :
- OpenAIRE
- Journal :
- Journal of Biological Chemistry
- Accession number :
- edsair.doi.dedup.....4195c46d39c3a31136ecd41694574401