Ligand Binding and Signal Transduction

Vainikka, S., Partanen, J., Bellosta, P., Coulier, F., Birnbaum, D., Basilico, C., Jaye, M. and Alitalo, K. (1992) Fibroblast growth factor receptor-4 shows novel features in genomic structure, ligand binding and signal transduction. EMBO J. 11 4273 280. 

Schiller PW, Nguyen TM, Weltrowska G, et al. Differential stereochemical requirements of p vs. 5 opioid receptors for ligand binding and signal transduction development of a class of potent and highly 5-selective peptide antagonists. Proc Natl Acad Sci USA 1992 89 11871-11875. 

The structure, as well as the mechanism, of ligand binding and signal transduction by chemokine receptors is similar to those of other members of the G... 

Analysis of ligand binding and signal transduction properties of the receptor was made based on the assumption that GPCRs exist and function as monomers. A number ofclassCGPCRs have been shown to form dimers at the plasma membrane. 

The endothelin receptor subtypes show differences in their signal transduction, ligand binding and tissue distribution. The ETA receptor is isopeptide-selective and binds ET-1 and ET-2 with the same and ET-3 with 70-100-fold lower affinity. The ETB receptor binds all three isoforms with the same affinity. 

Whether or not transmembrane helix rotation is a crucial event that leads to receptor activation in the case of TNER superfamily, a net effect of ligand binding and receptor activation appears to be the induced closer proximity of the intracellular domains (Eig. 12A), as shovm by fluorescence energy transfer experiments (Ghan et al, 2000). In the structures of TRAF-receptor complexes, the distance between bound receptor peptides is approximately 50 A. This suggests that a distance of separation between the intracellular domains of receptor chains on the order of 50 A may be optimal for TRAP recruitment and signaling transduction. 

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