List of works - Celine Valant

3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists

scientific article

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

scientific article

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

scientific article published on 06 September 2016

Activation and allosteric modulation of a muscarinic acetylcholine receptor

scientific article

Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration

scientific article published on 01 October 2009

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.

scientific article

Allosteric modulation of endogenous metabolites as an avenue for drug discovery.

scientific article published on 10 May 2012

Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes.

scientific article

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

scientific article published on 24 April 2018

Crystal structure of the M5 muscarinic acetylcholine receptor

scientific article published on 26 November 2019

Endogenous allosteric modulators of G protein-coupled receptors

scientific article

Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists

scientific article published on 4 August 2015

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

scientific article

Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.

scientific article published on June 2009

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.

scientific article

Positive allosteric mechanisms of adenosine A<sub>1</sub> receptor-mediated analgesia

scientific article published on 08 September 2021

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.

scientific article

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects

scientific article published on 11 October 2011

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

scientific article

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

scientific article

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

scientific article published on 11 March 2014

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

scientific article published on 13 October 2013

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists ⬇️

scientific article published on February 9, 2012

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.

scientific article published on 17 February 2012

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004.

scientific article published on 17 April 2015

Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.

scientific article published on 5 June 2014

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

scientific article published on 17 June 2013

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors ⬇️

journal article from 'British Journal of Pharmacology' published in 2021

The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor.

scientific article published on 4 May 2011

List of works by Celine Valant

3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.

Allosteric modulation of endogenous metabolites as an avenue for drug discovery.

Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes.

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

Crystal structure of the M5 muscarinic acetylcholine receptor

Endogenous allosteric modulators of G protein-coupled receptors

Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.

Positive allosteric mechanisms of adenosine A<sub>1</sub> receptor-mediated analgesia

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists ⬇️

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004.

Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors ⬇️

The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor.