Search Results - "Gerbier, Romain"
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Orphan GPR61, GPR62 and GPR135 receptors and the melatonin MT2 receptor reciprocally modulate their signaling functions
Published in Scientific reports (21-08-2017)“…Understanding the function of orphan G protein-coupled receptors (GPCRs), whose cognate ligand is unknown, is of major importance as GPCRs are privileged drug…”
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2
Apelin and Vasopressin: The Yin and Yang of Water Balance
Published in Frontiers in endocrinology (Lausanne) (22-11-2021)“…Apelin, a (neuro)vasoactive peptide, plays a prominent role in controlling body fluid homeostasis and cardiovascular functions. Experimental data performed in…”
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3
Development of original metabolically stable apelin‐17 analogs with diuretic and cardiovascular effects
Published in The FASEB journal (01-02-2017)“…ABSTRACT Apelin, a (neuro)vasoactive peptide, plays a prominent role in controlling cardiovascular functions and water balance. Because the in vivo apelin…”
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4
Melatonin MT1 and MT2 receptor ERK signaling is differentially dependent on Gi/o and Gq/11 proteins
Published in Journal of pineal research (01-05-2020)“…G protein‐coupled receptors (GPCRs) transmit extracellular signals into cells by activating G protein‐ and β‐arrestin‐dependent pathways. Extracellular…”
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5
Brain ACE2 activation following brain aminopeptidase A blockade by firibastat in salt-dependent hypertension
Published in Clinical science (1979) (26-03-2021)“…In the brain, aminopeptidase A (APA), a membrane-bound zinc metalloprotease, generates angiotensin III from angiotensin II. Brain angiotensin III exerts a…”
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6
Pharmacological evidence for transactivation within melatonin MT2 and serotonin 5‐HT2C receptor heteromers in mouse brain
Published in The FASEB journal (01-01-2021)“…Association of G protein‐coupled receptors into heterodimeric complexes has been reported for over 50 receptor pairs in vitro but functional in vivo validation…”
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7
Melatonin MT 1 and MT 2 receptor ERK signaling is differentially dependent on G i/o and G q/11 proteins
Published in Journal of pineal research (01-05-2020)“…G protein-coupled receptors (GPCRs) transmit extracellular signals into cells by activating G protein- and β-arrestin-dependent pathways. Extracellular…”
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8
LGR5 controls extracellular matrix production by stem cells in the developing intestine
Published in EMBO reports (03-07-2020)“…The Lgr5 receptor is a marker of intestinal stem cells (ISCs) that regulates Wnt/b‐catenin signaling. In this study, phenotype analysis of knockin/knockout…”
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9
LGR 5 controls extracellular matrix production by stem cells in the developing intestine
Published in EMBO reports (03-07-2020)Get full text
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10
By interacting with the C-terminal Phe of apelin, Phe$^{255}$ and Trp$^{259}$ in helix VI of the apelin receptor are critical for internalization
Published in The Journal of biological chemistry (15-10-2010)“…Apelin is the endogenous ligand of the orphan seven-transmembrane domain (TM) G protein-coupled receptor APJ. Apelin is involved in the regulation of body…”
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11
Design and validation of the first cell‐impermeant melatonin receptor agonist
Published in British journal of pharmacology (01-07-2017)“…Background and Purpose The paradigm that GPCRs are able to prolong or initiate cellular signalling through intracellular receptors recently emerged. Melatonin…”
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12
New structural insights into the apelin receptor: identification of key residues for apelin binding
Published in The FASEB journal (01-01-2015)“…Apelin is the endogenous ligand of the orphan 7‐transmembrane domain GPCRAPJ, now named the apelin receptor (ApelinR). Apelin plays a prominent role in body…”
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13
Pharmacological evidence for transactivation within melatonin MT 2 and serotonin 5-HT 2C receptor heteromers in mouse brain
Published in The FASEB journal (01-01-2021)“…Association of G protein-coupled receptors into heterodimeric complexes has been reported for over 50 receptor pairs in vitro but functional in vivo validation…”
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14
Identification and pharmacological properties of E339-3D6, the first nonpeptidic apelin receptor agonist
Published in The FASEB journal (01-05-2010)“…Apelin plays a prominent role in body fluid and cardiovascular homeostasis. To explore further upstream the role played by this peptide, nonpeptidic agonists…”
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15
O-linked melatonin dimers as bivalent ligands targeting dimeric melatonin receptors
Published in Bioorganic chemistry (01-04-2019)“…[Display omitted] •Bivalent ligands 3a-e increase BRET signals of MT1 dimers up to 3-fold vs. control 4.•3a-e do not change BRET signals at MT2 dimers compared…”
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16
Orphan GPR61, GPR62 and GPR135 receptors and the melatonin MT 2 receptor reciprocally modulate their signaling functions
Published in Scientific reports (21-08-2017)“…Understanding the function of orphan G protein-coupled receptors (GPCRs), whose cognate ligand is unknown, is of major importance as GPCRs are privileged drug…”
Get full text
Journal Article -
17
By Interacting with the C-terminal Phe of Apelin, Phe255 and Trp259 in Helix VI of the Apelin Receptor Are Critical for Internalization
Published in The Journal of biological chemistry (15-10-2010)“…Apelin is the endogenous ligand of the orphan seven-transmembrane domain (TM) G protein-coupled receptor APJ. Apelin is involved in the regulation of body…”
Get full text
Journal Article