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A new cellular model of response to estrogens: a bioluminescent test to characterize (anti) estrogen molecules.
TLDR
A cellular model in which estrogenic action can be detected by bioluminescence is developed, based on MCF-7 cells stably transfected with a receptor gene which allows expression of the firefly luciferase enzyme under control of the estrogen regulatory element of the Xenopus vitellogenin A2 gene. Expand
Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations.
TLDR
It is shown that it is possible to modulate food intake without altering growth hormone secretion, using ghrelin receptor ligands based on the trisubstituted 1,2,4-triazole structure. Expand
Prolonged treatment of breast cancer cells with antiestrogens increases the activating protein-1-mediated response: involvement of the estrogen receptor.
TLDR
A latent activation of AP-1 pathway could appear in the course of breast cancer antiestrogen treatment, in conditions where natural PKC activators are abnormally produced with unexpected consequences on the results of a long term antiestrogens treatment. Expand
MVLN Cells: A bioluminescent MCF-7-derived cell line to study the modulation of estrogenic activity
TLDR
It is concluded that this chimeric response faithfully reflects estrogenic action in the cell and can be used to develop different aspects of the endocrine research. Expand
Regulation of ERK1/2 activity by ghrelin‐activated growth hormone secretagogue receptor 1A involves a PLC/PKCɛ pathway
TLDR
In Chinese hamster ovary (CHO) cells, ghrelin induced, via the human GHSR‐1a, a transient and dose‐dependent activation of ERK1/2 leading to activation of the transcriptional factor Elk1 and the involvement of novel PKC isoforms, but not conventional or atypical PKCs. Expand
Activation of the ghrelin receptor is described by a privileged collective motion: a model for constitutive and agonist-induced activation of a sub-class A G-protein coupled receptor (GPCR).
TLDR
The model offered a powerful approach to study the conformational diversity and the activation mechanism of GPCRs and suggested stabilization of the Trp276 residue and of the whole receptor in the active state, preventing the motion observed along mode 16 computed for the unbound receptor. Expand
Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex
TLDR
These data provide direct evidence of a mechanism for ghrelin receptor-mediated Gq signaling in which transition of the receptor from an inactive to an active conformation is accompanied by a rearrangement of a preassembled receptor:G protein complex, ultimately leading to G protein activation and signaling. Expand
Regulation of ERK1/2 activity by ghrelin-activated growth hormone secretagogue receptor 1A involves a PLC/PKCvarepsilon pathway.
TLDR
In Chinese hamster ovary (CHO) cells, ghrelin induced, via the human GHSR-1a, a transient and dose-dependent activation of ERK1/2 leading to activation of the transcriptional factor Elk1 and the involvement of novel PKC isoforms (epsilon, delta), but not conventional or atypical PKCs. Expand
RU 38486: a potent antiglucocorticoid in vitro and in vivo.
TLDR
The antiglucocorticoid activity of RU 38486, was studied both in vitro and in vivo, and is the first pure antagonist of dexamethasone-induced hepatic TAT. Expand
GHSR-D2R heteromerization modulates dopamine signaling through an effect on G protein conformation
TLDR
It is demonstrated that receptor heteromerization directly impacts on dopamine-mediated Gi protein activation by modulating the conformation of its α-subunit, shedding light on the way a GPCR oligomer can affect G protein activation to modulate signaling. Expand
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