Fluorescence resonance energy transfer to probe human M1 muscarinic receptor structure and drug binding properties.
AuthorsIlien B, Franchet C, Bernard P, Morisset S, Weill CO, Bourguignon JJ, Hibert M, Galzi JL
JournalJ Neurochem
PubMed ID12694403
'Human M1 muscarinic receptor chimeras were designed (i) to allow detection of their interaction with the fluorescent antagonist pirenzepine labelled with Bodipy [558/568], through fluorescence resonance energy transfer, (ii) to investigate the structure of the N-terminal extracellular moiety of the receptor and (iii) to set up a fluorescence-based assay to ... More
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.
AuthorsTahtaoui C, Parrot I, Klotz P, Guillier F, Galzi JL, Hibert M, Ilien B
JournalJ Med Chem
PubMed ID15294002
Following a recent description of fluorescence resonance energy transfer between enhanced green fluorescent protein (EGFP)-fused human muscarinic M1 receptors and Bodipy-labeled pirenzepine, we synthesized seven fluorescent derivatives of this antagonist in order to further characterize ligand-receptor interactions. These compounds carry Bodipy [558/568], Rhodamine Red-X [560/580], or Fluorolink Cy3 [550/570] fluorophores ... More