Search Results - "Jnoff, Eric"

Binding Mode and Structure-Activity Relationships around Direct Inhibitors of the Nrf2-Keap1 Complex by Jnoff, Eric, Albrecht, Claudia, Barker, John J., Barker, Oliver, Beaumont, Edward, Bromidge, Steven, Brookfield, Frederick, Brooks, Mark, Bubert, Christian, Ceska, Tom, Corden, Vincent, Dawson, Graham, Duclos, Stephanie, Fryatt, Tara, Genicot, Christophe, Jigorel, Emilie, Kwong, Jason, Maghames, Rosemary, Mushi, Innocent, Pike, Richard, Sands, Zara A., Smith, Myron A., Stimson, Christopher C., Courade, Jean-Philippe

“…An X‐ray crystal structure of Kelch‐like ECH‐associated protein (Keap1) co‐crystallised with…”
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A highly efficient multicomponent synthesis of pyridones and pyrimidones by a [2+2+2] strategy by Ghosez, Léon, Jnoff, Eric, Bayard, Philippe, Sainte, Francy, Beaudegnies, Renaud

“…The reaction of N-silylated iminoethers with 2-substituted acetyl chlorides yields activated 2-azadienes. These were shown to react with electron-deficient…”
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Back-up strategies in drug discovery: what, how and when? by Provins, Laurent, Jnoff, Eric, Genicot, Christophe

“…•Back-up strategies and candidates in drug discovery are reviewed.•Progression of back-up candidates should depend on project key attributes.•Alignment of…”
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Front Cover: Identification of ß‐Glucocerebrosidase Activators for Glucosylceramide hydrolysis (ChemMedChem 7/2024) by Schulze, Monika‐Sarah E. D., Scholz, Diana, Jnoff, Eric, Hall, Adrian, Melin, Jonathan, Sands, Zara A., Rodriguez, Elizabeth, Andre, Veronique M.

“…The Front Cover illustrates the hydrolysis of the endogenous substrate glucosylceramide into glycosyl and ceramide by the enzyme glucocerebrosidase (GCase)…”
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Identification of ß-Glucocerebrosidase Activators for Glucosylceramide hydrolysis by Schulze, Monika-Sarah E D, Scholz, Diana, Jnoff, Eric, Hall, Adrian, Melin, Jonathan, Sands, Zara A, Rodriguez, Elizabeth, Andre, Veronique M

“…Several novel chemical series were identified that modulate glucocerebrosidase (GCase). Compounds from these series are active on glucosylceramide, unlike…”
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Discovery of a small molecule modulator of the Kv1.1/Kvβ1 channel complex that reduces neuronal excitability and in vitro epileptiform activity by Niespodziany, Isabelle, Mullier, Brice, André, Véronique Marie, Ghisdal, Philippe, Jnoff, Eric, Moreno‐Delgado, David, Swinnen, Dominique, Sands, Zara, Wood, Martyn, Wolff, Christian

“…Summary Aims Kv1.1 (KCNA1) channels contribute to the control of neuronal excitability and have been associated with epilepsy. Kv1.1 channels can associate…”
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Discovery of Heterocyclic Nonacetamide Synaptic Vesicle Protein 2A (SV2A) Ligands with Single-Digit Nanomolar Potency: Opening Avenues towards the First SV2A Positron Emission Tomography (PET) Ligands by Mercier, Joël, Archen, Laurence, Bollu, Véronique, Carré, Stéphane, Evrard, Yves, Jnoff, Eric, Kenda, Benoît, Lallemand, Bénédicte, Michel, Philippe, Montel, Florian, Moureau, Florence, Price, Nathalie, Quesnel, Yannick, Sauvage, Xavier, Valade, Anne, Provins, Laurent

“…The role of the synaptic vesicle protein 2A (SV2A) protein, target of the antiepileptic drug levetiracetam, is still mostly unknown. Considering its potential…”
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Multicomponent Reactions for the Synthesis of Complex Piperidine Scaffolds by Zhu, Wei, Mena, Marisa, Jnoff, Eric, Sun, Na, Pasau, Patrick, Ghosez, Léon

“…Creating diversity: Multicomponent reactions for the synthesis of complex piperidine scaffolds lead to high levels of skeletal, functional, and stereochemical…”
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5:00 PM NEGATIVE MODULATION OF THE SYNAPTIC VESICLE PROTEIN (SV2A): A NEW PHARMACOLOGICAL TARGET FOR COGNITIVE DEFICIT ASSOCIATED WITH SCHIZOPHRENIA by Laruelle, Marc, Detrait, Eric, Lamberty, Yves, Leclercq, Karine, Jnoff, Eric, Wood, Martin, Gillard, Michel, Jigorel, Emilie, Klitgaard, Henrik, Provins, Laurent

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Advantageous safety profile of a dual selective alpha2C agonist/alpha2A antagonist antinociceptive agent by Delaunois, Annie, De Ron, Pierrette, Dedoncker, Paul, Rosseels, Marie-Luce, Cornet, Miranda, Jnoff, Eric, Hanon, Etienne, Guyaux, Michel, Depelchin, Brigitte Olympe

“…A selective α2C‐adrenoceptor (AR) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity from…”
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Advantageous safety profile of a dual selective alpha(2C) agonist/alpha(2A) antagonist antinociceptive agent by Delaunois, Annie, De Ron, Pierrette, Dedoncker, Paul, Rosseels, Marie-Luce, Cornet, Miranda, Jnoff, Eric, Hanon, Etienne, Guyaux, Michel, Depelchin, Brigitte Olympe

“…A selective α2C -adrenoceptor (AR) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity from…”
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Advantageous safety profile of a dual selective alpha 2C agonist/alpha 2A antagonist antinociceptive agent by Delaunois, Annie, De Ron, Pierrette, Dedoncker, Paul, Rosseels, Marie‐Luce, Cornet, Miranda, Jnoff, Eric, Hanon, Etienne, Guyaux, Michel, Depelchin, Brigitte Olympe

“…Abstract A selective α 2C ‐adrenoceptor ( AR ) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity…”
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Cover Picture: Multicomponent Reactions for the Synthesis of Complex Piperidine Scaffolds (Angew. Chem. Int. Ed. 32/2009) by Zhu, Wei, Mena, Marisa, Jnoff, Eric, Sun, Na, Pasau, Patrick, Ghosez, Léon

“…Multicomponent reactions …︁ open up a versatile and efficient route to mono‐ and polycyclic piperidine derivatives, which are common substructures in…”
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Discovery of Heterocyclic Nonacetamide Synaptic Vesicle Protein2A (SV2A) Ligands with Single-Digit Nanomolar Potency: Opening Avenues towards the First SV2A Positron Emission Tomography (PET) Ligands by Mercier, Joël, Archen, Laurence, Bollu, Véronique, Carre, Stéphane, Evrard, Yves, Jnoff, Eric, Kenda, Benoît, Lallemand, Bénédicte, Michel, Philippe, Montel, Florian, Moureau, Florence, Price, Nathalie, Quesnel, Yannick, Sauvage, Xavier, Valade, Anne, Provins, Laurent

“…The role of the synaptic vesicle protein2A (SV2A) protein, target of the antiepileptic drug levetiracetam, is still mostly unknown. Considering its potential…”
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Discovery of Selective Alpha 2C Adrenergic Receptor Agonists by Jnoff, Eric, Christophe, Bernard, Collart, Philippe, Coloretti, Francis, Debeuckelaere, Aurel, De Ryck, Marc, Fuks, Bruno, Genicot, Christophe, Gillard, Michel, Guyaux, Michel, Price, Nathalie, Vandergeten, Marie‐Christine, Vermeiren, Céline

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Discovery of Selective Alpha2C Adrenergic Receptor Agonists by Jnoff, Eric, Christophe, Bernard, Collart, Philippe, Coloretti, Francis, Debeuckelaere, Aurel, De Ryck, Marc, Fuks, Bruno, Genicot, Christophe, Gillard, Michel, Guyaux, Michel, Price, Nathalie, Vandergeten, Marie-Christine, Vermeiren, Céline

“…Something to ease the pain: Chemical modification of a 2‐amino‐oxazoline scaffold led to the identification of α2C adrenergic receptor (AR) agonists. These…”
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Inside Cover: Binding Mode and Structure-Activity Relationships around Direct Inhibitors of the Nrf2-Keap1 Complex (ChemMedChem 4/2014) by Jnoff, Eric, Albrecht, Claudia, Barker, John J., Barker, Oliver, Beaumont, Edward, Bromidge, Steven, Brookfield, Frederick, Brooks, Mark, Bubert, Christian, Ceska, Tom, Corden, Vincent, Dawson, Graham, Duclos, Stephanie, Fryatt, Tara, Genicot, Christophe, Jigorel, Emilie, Kwong, Jason, Maghames, Rosemary, Mushi, Innocent, Pike, Richard, Sands, Zara A., Smith, Myron A., Stimson, Christopher C., Courade, Jean-Philippe

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Discovery of selective alpha(2C) adrenergic receptor agonists by Jnoff, Eric, Christophe, Bernard, Collart, Philippe, Coloretti, Francis, Debeuckelaere, Aurel, De Ryck, Marc, Fuks, Bruno, Genicot, Christophe, Gillard, Michel, Guyaux, Michel, Price, Nathalie, Vandergeten, Marie-Christine, Vermeiren, Céline

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Penicillamine as a ligand in the catalytic asymmetric reduction of kettones by Hanessian, Stephen, Jnoff, Eric, Griffin, Andrew M

“…Amino acids derived from D-penicillamine and thiazolidines were studied as ligands for the catalytic asymmetric reduction of ketones with borane…”
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Multicomponent Reactions for the Synthesis of Complex Piperidine Scaffolds by Zhu, Wei, Mena, Marisa, Jnoff, Eric, Sun, Na, Pasau, Patrick, Ghosez, Léon

“…Auf direktem Weg zur Diversität: Mehrkomponentenreaktionen führen effizient zu Piperidinen mit vielfältigen Gerüsten, Funktionalisierungsmustern und…”
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