RF-amide neuropeptides and their receptors in Mammals: Pharmacological properties, drug development and main physiological functions

R Quillet, S Ayachi, F Bihel, K Elhabazi, B Ilien… - Pharmacology & …, 2016 - Elsevier
RF-amide neuropeptides, with their typical Arg-Phe-NH 2 signature at their carboxyl C-termini,
belong to a lineage of peptides that spans almost the entire life tree. Throughout evolution…

[HTML][HTML] The neurokinin A receptor activates calcium and cAMP responses through distinct conformational states

T Palanche, B Ilien, S Zoffmann, MP Reck… - Journal of Biological …, 2001 - ASBMB
G protein-coupled receptors are thought to mediate agonist-evoked signal transduction by
interconverting between discrete conformational states endowed with different …

Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors

…, T Sorg, H Meziane, B Petit-Demoulière, B Ilien… - …, 2013 - Elsevier
Mammalian RF-amide peptides are encoded by five different genes and act through five
different G protein-coupled receptors. RF-amide-related peptides-1 and -3, neuropeptides AF …

Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor

…, F Guillier, JL Galzi, M Hibert, B Ilien - Journal of medicinal …, 2004 - ACS Publications
Following a recent description of fluorescence resonance energy transfer between enhanced
green fluorescent protein (EGFP)-fused human muscarinic M1 receptors and Bodipy-…

Assessment of morphine-induced hyperalgesia and analgesic tolerance in mice using thermal and mechanical nociceptive modalities

K Elhabazi, S Ayachi, B Ilien, F Simonin - JoVE (Journal of Visualized …, 2014 - jove.com
Opioid-induced hyperalgesia and tolerance severely impact the clinical efficacy of opiates
as pain relievers in animals and humans. The molecular mechanisms underlying both …

Time-Resolved FRET Binding Assay to Investigate Hetero-Oligomer Binding Properties: Proof of Concept with Dopamine D1/D3 Heterodimer

…, E Dupuis, C Thomas, A Mann, B Ilien… - ACS Chemical …, 2015 - ACS Publications
G protein-coupled receptors (GPCRs) have been described to form hetero-oligomers. The
importance of these complexes in physiology and pathology is considered crucial, and …

[HTML][HTML] Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process

B Ilien, N Glasser, JP Clamme, P Didier… - Journal of biological …, 2009 - ASBMB
Ligand binding to G protein-coupled receptors is a complex process that involves
sequential receptor conformational changes, ligand translocation, and possibly ligand-induced …

Fluorescence resonance energy transfer to probe human M1 muscarinic receptor structure and drug binding properties

B Ilien, C Franchet, P Bernard, S Morisset… - Journal of …, 2003 - Wiley Online Library
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 …

A rapid and versatile method to label receptor ligands using “click” chemistry: Validation with the muscarinic M1 antagonist pirenzepine

D Bonnet, B Ilien, JL Galzi, S Riché… - Bioconjugate …, 2006 - ACS Publications
Tagged biologically active molecules represent powerful pharmacological tools to study and
characterize ligand−receptor interactions. However, the labeling of such molecules is not …

Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors

…, E Kellenberger, M Hibert, JL Galzi, B Ilien - Journal of medicinal …, 2012 - ACS Publications
Two fluorescent derivatives of the M1 muscarinic selective agonist AC-42 were synthesized
by coupling the lissamine rhodamine B fluorophore (in ortho and para positions) to AC42-…