Formyl peptide receptor chimeras define domains involved in ligand binding.

A novel nonpeptide ligand for formyl peptide receptor-like 1.

Formyl peptide receptor-like 1 (FPRL1) is a G protein-coupled receptor that binds natural and synthetic peptides as well as lipoxin A(4) and mediates important biological functions. To facilitate its pharmacological characterization, we screened a compound library and identified a substituted quinazolinone (Quin-C1, 4-butoxy-N-[2-(4-methoxy-phenyl)-4-oxo-1,4-dihydro-2H-quinazolin-3-yl]-benzamid...

Ligand Binding Receptor through Inhibition of Cognate Antagonizes Human Formyl Peptide The Immunosuppressant Cyclosporin A

Domains of the human neutrophil N-formyl peptide receptor involved in G protein coupling. Mapping with receptor-derived peptides.

Chemotactic signaling by the human neutrophil N-formyl peptide receptor requires its association with heterotrimeric G protein. Synthetic peptides and a fusion protein derived from the intracellular regions of the receptor were used to identify sites which interact with G protein. A peptide derived from the second intracellular loop (C12R), and peptides (F15R and S22L) and a fusion protein deri...

Structural and functional characterization of the human formyl peptide receptor ligand-binding region.

The formyl peptide (N-formyl-1-methionyl-1-leucyl-1-phenylalanine [FMLP]) receptor is involved in the activation of neutrophils and their subsequent response to chemotactic N-formylated peptides. Recently, we found that the first extracellular loop closest to the N-terminal end of the FMLP receptor exhibited the strongest ligand binding compared with that shown by other extracellular regions. B...

Analysis of ligand binding specificity of receptor chimeras.

Finally, these results were obtained from one animal: because cognitive problems could be solved in different ways by different subjects, it is important that techniques for reading out brain operations be sensitive enough to be applied to single subjects. Indeed, the findings of our study indicate that the population vector is a sensitive tool by which an insight can be gained into the brain p...