Search Results - "Roques, Bernard Pierre"

NCp7 Activates HIV-1Lai RNA Dimerization by Converting a Transient Loop-Loop Complex into a Stable Dimer by Muriaux, Delphine, De Rocquigny, Hugues, Roques, Bernard-Pierre, Paoletti, Jacques

“…Nucleocapsid protein 7 (NCp7), the human immunodeficiency virus type 1 (HIV-1) nucleocapsid protein, was shown to strongly potentiate the dimerization of the…”
Get full text

Modeling of inhibitor-metalloenzyme interactions and selectivity using molecular mechanics grounded in quantum chemistry by Garmer, David R., Gresh, Nohad, Roques, Bernard-Pierre

“…We investigated the binding properties of the metalloprotease inhibitors hydroxamate, methanethiolate, and methylphosphoramidate to a model coordination site…”
Get full text

Interactions of a new α-aminophosphinic derivative inside the active site of TLN (thermolysin): a model for zinc-metalloendopeptidase inhibition by Selkti, Mohamed, Tomas, Alain, Gaucher, Jean-François, Prangé, Thierry, Fournié-Zaluski, Marie-Claude, Chen, Huixiong, Roques, Bernard-Pierre

“…A new α‐aminophosphinic compound able to inhibit both zinc‐containing exopeptidases and endopeptidases has been crystallized with TLN as a model in order to…”
Get full text

Crystal structure of leukotriene A4 hydrolase in complex with kelatorphan, implications for design of zinc metallopeptidase inhibitors by Tholander, Fredrik, Roques, Bernard-Pierre, Fournié-Zaluski, Marie-Claude, Thunnissen, Marjolein M.G.M., Haeggström, Jesper Z.

“…Leukotriene A4 hydrolase (LTA4H) is a key enzyme in the inflammatory process of mammals. It is an epoxide hydrolase and an aminopeptidase of the M1 family of…”
Get full text

Structure of the zinc finger domain encompassing residues 13-51 of the nucleocapsid protein from simian immunodeficiency virus by Morellet, Nelly, Meudal, Hervé, Bouaziz, Serge, Roques, Bernard Pierre

“…The NCps (nucleocapsid proteins) of HIV-1 (HIV type 1), HIV-2 and SIV (simian immunodeficiency virus) are small highly basic proteins, characterized by the…”
Get full text

Structure-Based Dissection of the Active Site Chemistry of Leukotriene A4 Hydrolase: Implications for M1 Aminopeptidases and Inhibitor Design by Tholander, Fredrik, Muroya, Ayumo, Roques, Bernard-Pierre, Fournié-Zaluski, Marie-Claude, Thunnissen, Marjolein M.G.M., Haeggström, Jesper Z.

“…M1 aminopeptidases comprise a large family of biologically important zinc enzymes. We show that peptide turnover by the M1 prototype, leukotriene A4…”
Get full text

Intramolecular chelation of Zn2+ by α- and β-mercaptocarboxamides. A parallel ab initio and polarizable molecular mechanics investigation. Assessment of the role of multipole transferability by Tiraboschi, Gilles, Fournié-Zaluski, Marie-Claude, Roques, Bernard-Pierre, Gresh, Nohad

“…α‐ and β‐mercaptocarboxamides constitute the Zn2+‐ligating entity of several highly potent metalloenzyme inhibitors. We have studied their interaction energies…”
Get full text

N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities by Inguimbert, Nicolas, Poras, Hervé, Teffo, Franck, Beslot, Françoise, Selkti, Mohamed, Tomas, Alain, Scalbert, Elizabeth, Bennejean, Caroline, Renard, Pierre, Fournié-Zaluski, Marie-Claude, Roques, Bernard-Pierre

“…We have previously reported the design of a lead compound 1a for the joint inhibition of neprilysin (NEP, EC 3.4.24.11), angiotensin converting enzyme (ACE, EC…”
Get full text

Joint quantum chemical and polarizable molecular mechanics investigation of formate complexes with penta- and hexahydrated Zn2+: Comparison between energetics of model bidentate, monodentate, and through-water Zn2+ binding modes and evaluation of nonadditivity effects by Tiraboschi, Gilles, Roques, Bernard-Pierre, Gresh, Nohad

“…In order to gain an understanding of the energetics of polycoordinated Zn2+ binding to the formate anion (the end side chain of the Asp and Glu residues of…”
Get full text

Further evidence for the interaction of μ- and δ-opioid receptors in the antinociceptive effects of the dual inhibitor of enkephalin catabolism, RB101(S): A spinal c-Fos protein study in the rat under carrageenin inflammation by Le Guen, Stéphanie, Catheline, Gwénaëlle, Fournié-Zaluski, Marie-Claude, Roques, Bernard-Pierre, Besson, Jean-Marie, Buritova, Jaroslava

“…We have previously shown that RB101, a dual inhibitor of enkephalin-degrading enzymes, decreased carrageenin-evoked c-Fos protein expression at the spinal cord…”
Get full text

The dual peptidase inhibitor RB101 induces a long-lasting increase in the extracellular level of Met-enkephalin-like material in the nucleus accumbens of freely moving rats by Daugé, V, Mauborgne, A, Cesselin, F, Fournié-Zaluski, M C, Roques, B P

“…This study was carried out to analyze the extracellular levels of Met-enkephalin-like material in the nucleus accumbens, a brain structure involved in the…”
Get more information

Thermolysin-inhibitor binding: Effect of the His231 → Ala mutation on the relative affinities of thiolate versus phosphoramidate inhibitors-a model theoretical investigation incorporating a continuum reaction field hydration model by Gresh, Nohad, Roques, Bernard-Pierre

“…A series of site‐directed mutagenesis experiments have been performed in our laboratory, bearing on the Zn2+ metalloprotease from Bacillus stearothermophillus,…”
Get full text

The effects of RB101, a mixed inhibitor of enkephalin-catabolizing enzymes, on carrageenin-induced spinal c-Fos expression are completely blocked by β-funaltrexamine, a selective μ-opioid receptor antagonist by Le Guen, Stéphanie, Honoré, Prisca, Catheline, Gwénaëlle, Fournié-Zaluski, Marie-Claude, Roques, Bernard-Pierre, Besson, Jean-Marie

“…We have demonstrated that pre-administered RB101 (40 mg/kg, i.v.), a mixed inhibitor of enkephalin-catabolizing enzymes, decreased spinal c-Fos expression…”
Get full text

Differential Interactions of the Growth Factor Receptor-bound Protein 2 N-SH3 Domain with Son of Sevenless and Dynamin by Vidal, Michel, Montiel, José-Luis, Cussac, Didier, Cornille, Fabrice, Duchesne, Marc, Parker, Fabienne, Tocqué, Bruno, Roques, Bernard-Pierre, Garbay, Christiane

“…In this paper, we show that the 36–45 surface-exposed sequence WYKAELNGKD of growth factor receptor-bound protein 2 (Grb2) N-SH3 domain inhibits the…”
Get full text

Structure-Activity Relationships in a Series of 5-[(2,5-Dihydroxybenzyl)amino]salicylate Inhibitors of EGF-Receptor-Associated Tyrosine Kinase: Importance of Additional Hydrophobic Aromatic Interactions by Chen, Huixiong, Boiziau, Janine, Parker, Fabienne, Mailliet, Patrick, Commercon, Alain, Tocque, Bruno, Le Pecq, Jean-Bernard, Roques, Bernard-Pierre, Garbay, Christiane

“…Potent inhibitors of EGF-dependent protein tyrosine kinase (PTK) activity were synthesized in a series of 5-[(2,5-dihydroxybenzyl)amino]salicylates. Several of…”
Get full text

Cleavage of L-leucine-containing dipeptides by Clostridium butyricum by Khelifa, Nasser, Brik, Mohabeddine, Tessedre, Annie-Claude, De Rocquigny, Hugues, Roques, Bernard-Pierre, Courtieu, Jacques, Rimbault, Alain

“…The ability of Clostridium butyricum cultures to hydrolyze three L-leucine-containing dipeptides (Leu-Leu, Leu-Gly and Gly-Leu) in a synthetic minimal medium…”
Get full text

Human brain aminopeptidase A: biochemical properties and distribution in brain nuclei by de Mota, Nadia, Iturrioz, Xavier, Claperon, Cedric, Bodineau, Laurence, Fassot, Celine, Roques, Bernard Pierre, Palkovits, Miklos, Llorens-Cortes, Catherine

“…Aminopeptidase A (APA) generated brain angiotensin III, one of the main effector peptides of the brain renin angiotensin system, exerting a tonic stimulatory…”
Get full text

Crystal structure of leukotriene A 4 hydrolase in complex with kelatorphan, implications for design of zinc metallopeptidase inhibitors by Tholander, Fredrik, Roques, Bernard-Pierre, Fournié-Zaluski, Marie-Claude, Thunnissen, Marjolein M.G.M., Haeggström, Jesper Z.

“…Leukotriene A 4 hydrolase (LTA4H) is a key enzyme in the inflammatory process of mammals. It is an epoxide hydrolase and an aminopeptidase of the M1 family of…”
Get full text

Mutant mice lacking the cholecystokinin2 receptor show a dopamine-dependent hyperactivity and a behavioral sensitization to morphine by DAUGE, Valérie, BESLOT, Francoise, MATSUI, Toshimitsu, ROQUES, Bernard Pierre

“…Cholecystokinin2 (CCK2) receptor-deficient mice were used to analyze the in vivo function of CCK2 receptor and especially the incidence of this gene…”
Get full text

Mutant mice lacking the cholecystokinin 2 receptor show a dopamine-dependent hyperactivity and a behavioral sensitization to morphine by Daugé, Valérie, Beslot, Françoise, Matsui, Toshimitsu, Roques, Bernard Pierre

“…Cholecystokinin 2 (CCK 2) receptor-deficient mice were used to analyze the in vivo function of CCK 2 receptor and especially the incidence of this gene…”
Get full text