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Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice.
It is proposed that ANA-12 may be a valuable tool for studying BDNF/TrkB signaling and may constitute a lead compound for developing the next generation of therapeutic agents for the treatment of mood disorders. Expand
Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist
BP 897 inhibits cocaine-seeking behaviour that depends upon the presentation of drug-associated cues, without having any intrinsic, primary rewarding effects, which indicates that compounds like BP 897 could be used for reducing the drug craving and vulnerability to relapse that are elicited by drug- associated environmental stimuli. Expand
Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents.
These studies establish nafadotride as a pure, extremely potent, competitive and preferential dopamine D3 receptor antagonist in vitro. Expand
Virtual Screening-Based Discovery and Mechanistic Characterization of the Acylthiourea MRT-10 Family as Smoothened Antagonists
A pharmacophoric model for Smo inhibitors constituted by three hydrogen bond acceptor groups and three hydrophobic regions is generated and validated and aimed at identifying novel modulators of Smo and of other G-protein coupled receptors. Expand
N-(ω-(4-(2-Methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as Dopamine D2 and D3 Receptor Ligands
The dopamine D3 receptor is recognized as a potential therapeutic target for the treatment of various neurological and psychiatric disorders. Targetting high affinity and D3 versus D2Expand
MRT‐92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor
  • L. Hoch, H. Faure, +9 authors M. Ruat
  • Biology, Medicine
  • FASEB journal : official publication of the…
  • 30 January 2015
This work convincingly confirms that MRT‐92 simultaneously recognized and occupied both sites 1 and 2 of the Smoothened receptor and demonstrates the existence of a third type of Smo antagonists, those entirely filling the Smo binding cavity from the upper extracellular part to the lower cytoplasmicproximal subpocket. Expand
Time-resolved FRET binding assay to investigate hetero-oligomer binding properties: proof of concept with dopamine D1/D3 heterodimer.
A new time-resolved FRET (TR-FRET) based assay to determine ligand affinity for the D1/D3 heteromer, easy to implement on other G protein-coupled receptors, constitutes an attractive strategy to screen for heteromer ligands. Expand
Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity.
Findings suggest that original molecules prepared by ligand-based structural optimization will help delineate Smo and Hh functions and can be developed as potential anticancer agents. Expand
Identification and characterization of Hedgehog modulator properties after functional coupling of Smoothened to G15.
These studies identify novel properties of molecules displaying potential interest in the treatment of various cancers and brain diseases, and demonstrate that Smo is capable of signaling through G15. Expand