Search Results - "Denoyelle, Severine"

Synthesis of [1,2,4]Triazolo[4,3‑a]piperazin-6-ones: An Approach to the Triazole-Fused Ketopiperazine Scaffold by Ben Haj Salah, Khoubaib, Legrand, Baptiste, Bibian, Mathieu, Wenger, Emmanuel, Fehrentz, Jean-Alain, Denoyelle, Séverine

“…A stereoconservative synthesis to access the triazole-fused ketopiperazine (TKP) scaffold is presented. This underexplored platform offers a wide range of…”
Get full text

Circulating ghrelin crosses the blood-cerebrospinal fluid barrier via growth hormone secretagogue receptor dependent and independent mechanisms by Uriarte, Maia, De Francesco, Pablo N., Fernández, Gimena, Castrogiovanni, Daniel, D'Arcangelo, Micaela, Imbernon, Mónica, Cantel, Sonia, Denoyelle, Severine, Fehrentz, Jean-Alain, Praetorius, Jeppe, Prevot, Vincent, Perello, Mario

“…Ghrelin is a peptide hormone mainly secreted from gastrointestinal tract that acts via the growth hormone secretagogue receptor (GHSR), which is highly…”
Get full text

Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex by Damian, Marjorie, Mary, Sophie, Maingot, Mathieu, M’Kadmi, Céline, Gagne, Didier, Leyris, Jean-Philippe, Denoyelle, Séverine, Gaibelet, Gérald, Gavara, Laurent, de Souza Costa, Mauricio Garcia, Perahia, David, Trinquet, Eric, Mouillac, Bernard, Galandrin, Ségolène, Galès, Céline, Fehrentz, Jean-Alain, Floquet, Nicolas, Martinez, Jean, Marie, Jacky, Banères, Jean-Louis

“…Significance G protein-coupled receptors (GPCRs), one of the largest cell surface receptor families, transmit their signals through the coupling of…”
Get full text

Role of symmetry in 3,3-diphenyl-1,3-dihydroindol-2-one derivatives as inhibitors of translation initiation by Yang, Hongwei, Chen, Ting, Denoyelle, Séverine, Chen, Limo, Fan, Jing, Zhang, Yingzhen, Halperin, José A., Chorev, Michael, Aktas, Bertal H.

“…[Display omitted] •Transforming the chiral DDOI 3-phenyl,3-(2-hydroxy, 4-tert-butyl)phenyl-1,3-dihydroindol-2-one, into achiral…”
Get full text

A Novel Truncated Liver Enriched Antimicrobial Peptide-2 Palmitoylated at its N-Terminal Antagonizes Effects of Ghrelin by Holá, Lucie, Železná, Blanka, Karnošová, Alena, Kuneš, Jaroslav, Fehrentz, Jean-Alain, Denoyelle, Séverine, Cantel, Sonia, Blechová, Miroslava, Sýkora, David, Myšková, Aneta, Maletínská, Lenka

“…Ghrelin is secreted in the stomach during fasting and targets the growth hormone secretagogue receptor (GHSR1a) in the hypothalamus and brainstem to exert its…”
Get full text

GHSR-D2R heteromerization modulates dopamine signaling through an effect on G protein conformation by Damian, Marjorie, Pons, Véronique, Renault, Pedro, M’Kadmi, Céline, Delort, Bartholomé, Hartmann, Lucie, Kaya, Ali I., Louet, Maxime, Gagne, Didier, Salah, Khoubaib Ben Haj, Denoyelle, Séverine, Ferry, Gilles, Boutin, Jean A., Wagner, Renaud, Fehrentz, Jean-Alain, Martinez, Jean, Marie, Jacky, Floquet, Nicolas, Galès, Céline, Mary, Sophie, Hamm, Heidi E., Banères, Jean-Louis

“…The growth hormone secretagogue receptor (GHSR) and dopamine receptor (D2R) have been shown to oligomerize in hypothalamic neurons with a significant effect on…”
Get full text

Growth hormone secretagogues modulate inflammation and fibrosis in mdx mouse model of Duchenne muscular dystrophy by Boccanegra, Brigida, Cappellari, Ornella, Mantuano, Paola, Trisciuzzi, Daniela, Mele, Antonietta, Tulimiero, Lisamaura, De Bellis, Michela, Cirmi, Santa, Sanarica, Francesca, Cerchiara, Alessandro Giovanni, Conte, Elena, Meanti, Ramona, Rizzi, Laura, Bresciani, Elena, Denoyelle, Severine, Fehrentz, Jean-Alain, Cruciani, Gabriele, Nicolotti, Orazio, Liantonio, Antonella, Torsello, Antonio, De Luca, Annamaria

“…Growth hormone secretagogues (GHSs) exert multiple actions, being able to activate GHS-receptor 1a, control inflammation and metabolism, to enhance…”
Get full text

Development of a novel fluorescent ligand of growth hormone secretagogue receptor based on the N-Terminal Leap2 region by Barrile, Franco, M'Kadmi, Céline, De Francesco, Pablo N., Cabral, Agustina, García Romero, Guadalupe, Mustafá, Emilio R., Cantel, Sonia, Damian, Marjorie, Mary, Sophie, Denoyelle, Séverine, Banères, Jean-Louis, Marie, Jacky, Raingo, Jesica, Fehrentz, Jean-Alain, Perelló, Mario

“…Liver-expressed antimicrobial peptide 2 (LEAP2) was recently recognized as an endogenous ligand for the growth hormone secretagogue receptor (GHSR), which also…”
Get full text

Design and characterization of a triazole-based growth hormone secretagogue receptor modulator inhibiting the glucoregulatory and feeding actions of ghrelin by Péraldi-Roux, Sylvie, Bayle, Morgane, M'Kadmi, Céline, Damian, Marjorie, Vaillé, Justine, Fernandez, Gimena, Cornejo, Maria Paula, Marie, Jacky, Banères, Jean-Louis, Ben Haj Salah, Khoubaib, Fehrentz, Jean-Alain, Cantel, Sonia, Perello, Mario, Denoyelle, Séverine, Oiry, Catherine, Neasta, Jérémie

“…[Display omitted] The growth hormone secretagogue receptor (GHSR) is a G protein-coupled receptor that regulates essential physiological functions. In…”
Get full text

Evaluation of amidoxime derivatives as prodrug candidates of potent bis-cationic antimalarials by Berger, Olivier, Ortial, Stéphanie, Wein, Sharon, Denoyelle, Séverine, Bressolle, Françoise, Durand, Thierry, Escale, Roger, Vial, Henri J., Vo-Hoang, Yen

“…[Display omitted] Plasmodium falciparum is responsible for most of the cases of malaria and its resistance to established antimalarial drugs is a major issue…”
Get full text

Selective C-Acylation of 2-Aminoimidazo[1,2-a]pyridine: Application to the Synthesis of Imidazopyridine-Fused [1,3]Diazepinones by Masurier, Nicolas, Aruta, Roberta, Gaumet, Vincent, Denoyelle, Séverine, Moreau, Emmanuel, Lisowski, Vincent, Martinez, Jean, Maillard, Ludovic T

“…A series of 20 optically pure 3,4-dihydro-5H-pyrido[1′,2′:1,2]imidazo[4,5-d][1,3]diazepin-5-ones which form a new family of azaheterocycle-fused…”
Get full text

The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist by Moulin, Aline, Brunel, Luc, Boeglin, Damien, Demange, Luc, Ryan, Johanne, M’Kadmi, Céline, Denoyelle, Séverine, Martinez, Jean, Fehrentz, Jean-Alain

“…Ghrelin is a 28-residue peptide acylated with an n -octanoyl group on the Ser 3 residue, predominantly produced by the stomach. Ghrelin displays strong growth…”
Get full text

Concerted conformational dynamics and water movements in the ghrelin G protein-coupled receptor by Louet, Maxime, Casiraghi, Marina, Damian, Marjorie, Costa, Mauricio Gs, Renault, Pedro, Gomes, Antoniel As, Batista, Paulo R, M'Kadmi, Céline, Mary, Sophie, Cantel, Sonia, Denoyelle, Severine, Ben Haj Salah, Khoubaib, Perahia, David, Bisch, Paulo M, Fehrentz, Jean-Alain, Catoire, Laurent J, Floquet, Nicolas, Banères, Jean-Louis

“…There is increasing support for water molecules playing a role in signal propagation through G protein-coupled receptors (GPCRs). However, exploration of the…”
Get full text

Chemical genetics identify eIF2α kinase heme-regulated inhibitor as an anticancer target by Chen, Ting, Ozel, Duygu, Qiao, Yuan, Harbinski, Fred, Chen, Limo, Denoyelle, Séverine, He, Xiaoying, Zvereva, Nela, Supko, Jeffrey G, Chorev, Michael, Halperin, Jose A, Aktas, Bertal H

“…Overabundance of the eIF2–GTP–Met-tRNAi translational initiation complex has been linked to malignant transformation. N , N '-diarylurea chemical probes that…”
Get full text

Synthesis of Thieno[3,2-e][1,4]diazepin-2-ones: Application of an Uncatalysed Pictet-Spengler Reaction by Denoyelle, Séverine, Tambutet, Guillaume, Masurier, Nicolas, Maillard, Ludovic T., Martinez, Jean, Lisowski, Vincent

“…A series of 5‐substituted thieno[3,2‐e][1,4]diazepin‐2‐ones was synthesized in four steps from methyl 3‐aminothiophene‐2‐carboxylate. After the coupling of…”
Get full text

LEAP2 Impairs the Capability of the Growth Hormone Secretagogue Receptor to Regulate the Dopamine 2 Receptor Signaling by Mustafá, Emilio R., Cordisco González, Santiago, Damian, Marjorie, Cantel, Sonia, Denoyelle, Severine, Wagner, Renaud, Schiöth, Helgi B., Fehrentz, Jean-Alain, Banères, Jean-Louis, Perelló, Mario, Raingo, Jesica

“…The growth hormone secretagogue receptor (GHSR) signals in response to ghrelin, but also acts via ligand-independent mechanisms that include either…”
Get full text

In vitro inhibition of translation initiation by N,N′-diarylureas—potential anti-cancer agents by Denoyelle, Séverine, Chen, Ting, Chen, Limo, Wang, Yibo, Klosi, Edvin, Halperin, José A., Aktas, Bertal H., Chorev, Michael

“…Structure–activity relationship study on N,N′-diarylureas, potential anti-cancer drugs capable of inhibiting the translation initiation of mRNA in cancer cells…”
Get full text

Agonism, Antagonism, and Inverse Agonism Bias at the Ghrelin Receptor Signaling by M'Kadmi, Céline, Leyris, Jean-Philippe, Onfroy, Lauriane, Galés, Céline, Saulière, Aude, Gagne, Didier, Damian, Marjorie, Mary, Sophie, Maingot, Mathieu, Denoyelle, Séverine, Verdié, Pascal, Fehrentz, Jean-Alain, Martinez, Jean, Banères, Jean-Louis, Marie, Jacky

“…The G protein-coupled receptor GHS-R1a mediates ghrelin-induced growth hormone secretion, food intake, and reward-seeking behaviors. GHS-R1a signals through…”
Get full text

N‑Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor by M’Kadmi, Céline, Cabral, Agustina, Barrile, Franco, Giribaldi, Julien, Cantel, Sonia, Damian, Marjorie, Mary, Sophie, Denoyelle, Séverine, Dutertre, Sébastien, Péraldi-Roux, Sylvie, Neasta, Jérémie, Oiry, Catherine, Banères, Jean-Louis, Marie, Jacky, Perello, Mario, Fehrentz, Jean-Alain

“…The ghrelin receptor or growth hormone secretagogue receptor (GHSR) is a G-protein-coupled receptor that controls growth hormone and insulin secretion, food…”
Get full text

New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center by Maingot, Mathieu, Blayo, Anne-Laure, Denoyelle, Séverine, M’Kadmi, Céline, Damian, Marjorie, Mary, Sophie, Gagne, Didier, Sanchez, Pierre, Aicher, Babette, Schmidt, Peter, Müller, Gilbert, Teifel, Michael, Günther, Eckhard, Marie, Jacky, Banères, Jean-Louis, Martinez, Jean, Fehrentz, Jean-Alain

“…[Display omitted] Introducing a second chiral center on our previously described 1,2,4-triazole, allowed us to increase diversity and elongate the ‘C-terminal…”
Get full text