Search Results - "Bihel, F"

TSPO ligands stimulate ZnPPIX transport and ROS accumulation leading to the inhibition of P. falciparum growth in human blood by Marginedas-Freixa, I., Hattab, C., Bouyer, G., Halle, F., Chene, A., Lefevre, S. D., Cambot, M., Cueff, A., Schmitt, M., Gamain, B., Lacapere, J. J., Egee, S., Bihel, F., Le Van Kim, C., Ostuni, M. A.

“…After invading red blood cells (RBCs), Plasmodium falciparum ( Pf ) can export its own proteins to the host membrane and activate endogenous channels that are…”
Get full text

Involvement of neuropeptide FF receptors in neuroadaptive responses to acute and chronic opiate treatments by Elhabazi, K, Trigo, JM, Mollereau, C, Moulédous, L, Zajac, J‐M, Bihel, F, Schmitt, M, Bourguignon, JJ, Meziane, H, Petit‐demoulière, B, Bockel, F, Maldonado, R, Simonin, F

“…BACKGROUND AND PURPOSE Opiates remain the most effective compounds for alleviating severe pain across a wide range of conditions. However, their use is…”
Get full text

The effect of neuropeptide FF in the amygdala kindling model by Buffel, I., Meurs, A., Portelli, J., Raedt, R., De Herdt, V., Poppe, L., De Meulenaere, V., Wadman, W., Bihel, F., Schmitt, M., Vonck, K., Bourguignon, J.-J., Simonin, F., Smolders, I., Boon, P.

“…Objective Neuropeptide FF (NPFF) and its receptors (NPFF1R and NPFF2R) are differentially distributed throughout the central nervous system. NPFF reduces…”
Get full text

New 2-bromomethyl-8-substituted-benzo[ c]chromen-6-ones. Synthesis and biological properties by Garino, Cédrik, Bihel, Frédéric, Pietrancosta, Nicolas, Laras, Younes, Quéléver, Gilles, Woo, Irene, Klein, Peter, Bain, Jenny, Boucher, Jean-Luc, Kraus, Jean-Louis

“…[Display omitted] New 2-bromomethyl-8-substituted-benzo[ c]chromen-6-ones have been synthesized and their bioactive properties have been evaluated on different…”
Get full text

Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new β-amyloid peptide production inhibitors and their activities on various classes of protease by Bihel, Frédéric, Quéléver, Gilles, Lelouard, Hugues, Petit, Agnès, Alvès da Costa, Cristine, Pourquié, Olivier, Checler, Frédéric, Thellend, Annie, Pierre, Philippe, Kraus, Jean-Louis

“…A series of new 7-substituted-4-chloro-3-alkoxy isocoumarin derivatives were synthesized and evaluated as inhibitors of representative classes of proteases:…”
Get full text

Substituted thiazolamide coupled to a redox delivery system: a new gamma-secretase inhibitor with enhanced pharmacokinetic profile by Laras, Younes, Quéléver, Gilles, Garino, Cédrik, Pietrancosta, Nicolas, Sheha, Mahmoud, Bihel, Frédéric, Wolfe, Michael S, Kraus, Jean-Louis

“…Inhibition of gamma-secretase, one of the enzymes responsible for the cleavage of the amyloid precursor protein (APP) to produce pathogenic A beta peptides, is…”
Get more information

New 3‘-Azido-3‘-deoxythymidin-5‘-yl O-(ω-Hydroxyalkyl) Carbonate Prodrugs:  Synthesis and Anti-HIV Evaluation by Vlieghe, Patrick, Bihel, Frédéric, Clerc, Thierry, Pannecouque, Christophe, Witvrouw, Myriam, De Clercq, Erik, Salles, Jean-Pierre, Chermann, Jean-Claude, Kraus, Jean-Louis

“…Prodrugs of zidovudine (AZT) have been synthesized in an effort to enhance its uptake by HIV-1 infected cells and its anti-HIV activity. The 5‘-OH function of…”
Get full text

Reactivity studies of 3-alkoxy-7-amino-4-chloroisocoumarins (beta-amyloid peptide inhibitors) versus different classes of amines by Bihel, Frédéric, Faure, Robert, Kraus, Jean-Louis

“…3-Alkoxy-7-amino-4-chloroisocoumarins have been shown to lower the beta-amyloid secretion (a major component of the senile plaques involved in Alzheimer's…”
Get more information

New beta-strand macrocyclic peptidomimetic analogues containing alpha-(O-, S- or NH-)aryl substituted glycine residues: synthesis, chemical and enzymatic properties by Quéléver, Gilles, Bihel, Frédéric, Kraus, Jean-Louis

“…In so much as bis-macrocyclic peptidomimetics have been recognized as high affinity substrates for HIV-1 protease, we were interested in the design and…”
Get more information

N-Acyl substituted 7-amino-4-chloroisocoumarin: A peptide degradation model via an imide mechanism by Garino, Cédrik, Bihel, Frédéric, Souard, Florence, Quéléver, Gilles, Kraus, Jean-Louis

“…During the coupling reaction between 3-alkoxy-7-amino-4-chloroisocoumarin and N-acyl alanine dipeptide, an unexpected deamidation reaction was observed. The…”
Get full text

Saving dopaminergic neurons from endoplasmic reticulum (ER) stress - A breakthrough approach to fight Parkinson's disease by Gentile, L., Nasir, A., Sinane, M., Conan, P., Ückert, A.-K., Leist, M., Friocourt, G., Trollet, C., Bihel, F., Voisset, C.

Get full text

Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors by Elhabazi, Khadija, Humbert, Jean-Paul, Bertin, Isabelle, Schmitt, Martine, Bihel, Frédéric, Bourguignon, Jean-Jacques, Bucher, Bernard, Becker, Jérôme A.J., Sorg, Tania, Meziane, Hamid, Petit-Demoulière, Benoit, Ilien, Brigitte, Simonin, Frédéric

“…Mammalian RF-amide peptides are encoded by five different genes and act through five different G protein-coupled receptors. RF-amide-related peptides-1 and -3,…”
Get full text

Fully Regiocontrolled Polyarylation of Pyridine by Doebelin, Christelle, Wagner, Patrick, Bihel, Frédéric, Humbert, Nicolas, Kenfack, Cyril Assongo, Mely, Yves, Bourguignon, Jean-Jacques, Schmitt, Martine

“…Starting from commercially available 2-chloro-3-hydroxypyridine, a new route leading to the first protypical pentaarylpyridine bearing five different…”
Get full text

A bifunctional-biased mu-opioid agonist–neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects by Drieu la Rochelle, Armand, Guillemyn, Karel, Dumitrascuta, Maria, Martin, Charlotte, Utard, Valérie, Quillet, Raphaëlle, Schneider, Séverine, Daubeuf, François, Willemse, Tom, Mampuys, Pieter, Maes, Bert U.W., Frossard, Nelly, Bihel, Frédéric, Spetea, Mariana, Simonin, Frédéric, Ballet, Steven

“…Opioid analgesics, such as morphine, oxycodone, and fentanyl, are the cornerstones for treating moderate to severe pain. However, on chronic administration,…”
Get full text

The Initial Substrate-Binding Site of γ-Secretase Is Located on Presenilin near the Active Site by Kornilova, Anna Y., Bihel, Frédéric, Das, Chittaranjan, Wolfe, Michael S., Frey, Perry A.

“…γ-Secretase is a structurally enigmatic multiprotein complex that catalyzes intramembrane proteolysis of a variety of substrates, including the amyloid…”
Get full text

Aminoguanidine Hydrazone Derivatives as Nonpeptide NPFF1 Receptor Antagonists Reverse Opioid Induced Hyperalgesia by Hammoud, Hassan, Elhabazi, Khadija, Quillet, Raphäelle, Bertin, Isabelle, Utard, Valérie, Laboureyras, Emilie, Bourguignon, Jean-Jacques, Bihel, Frédéric, Simonnet, Guy, Simonin, Frédéric, Schmitt, Martine

“…Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand neuropeptide FF have been shown previously to display antiopioid properties and to…”
Get full text

Design and validation of a homogeneous time-resolved fluorescence cell-based assay targeting the ligand-gated ion channel 5-HT3A by Blanc, Emilie, Wagner, Patrick, Plaisier, Fabrice, Schmitt, Martine, Durroux, Thierry, Bourguignon, Jean-Jacques, Partiseti, Michel, Dupuis, Elodie, Bihel, Frederic

“…Ligand-gated ion channels (LGICs) are considered as attractive protein targets in the search for new therapeutic agents. Nowadays, this strategy involves the…”
Get full text

Discovery of a Subnanomolar Helical d-Tridecapeptide Inhibitor of γ-Secretase by Bihel, Frédéric, Das, Chittaranjan, Bowman, Michael J, Wolfe, Michael S

“…γ-Secretase is the second of two proteolytic enzymes responsible for the release of the amyloid β-peptide implicated in the etiology of Alzheimer's disease…”
Get full text

Novel synthesis of 3,4-dihydro-5-bromo[1,4]oxazin-2-one derivatives, new protease inhibitor scaffold by Bihel, Frédéric, Kraus, Jean-Louis

“…We designed and synthesized a new class of serine protease inhibitors based on the oxazinone core. To this end, we first developed a short and efficient route…”
Get more information

Photoactivatable helical peptide inhibitors of y-secretase covalently bind to presenilin at a site close to but distinct from the active site by Kornilova, A.Y., Bihel, F., Das, C., Wolfe, M.S.

Get full text