Search Results - "Quancard, Jean"

Palladium-Catalyzed Enantioselective C-3 Allylation of 3-Substituted-1H-Indoles Using Trialkylboranes by Trost, Barry M, Quancard, Jean

“…We have developed a new enantioselective C-3 allylation of 3-substituted indoles using allyl alcohol and trialkylboranes. Asymmetric syntheses of…”
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An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient by Quancard, Jean, Klein, Theo, Fung, Shan-Yu, Renatus, Martin, Hughes, Nicola, Israël, Laura, Priatel, John J., Kang, Sohyeong, Blank, Michael A., Viner, Rosa I., Blank, Jutta, Schlapbach, Achim, Erbel, Paul, Kizhakkedathu, Jayachandran, Villard, Frédéric, Hersperger, René, Turvey, Stuart E., Eder, Joerg, Bornancin, Frédéric, Overall, Christopher M.

“…MALT1 paracaspase is central for lymphocyte antigen-dependent responses including NF-κB activation. We discovered nanomolar, selective allosteric inhibitors of…”
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Targeted inhibition of the COP9 signalosome for treatment of cancer by Schlierf, Anita, Altmann, Eva, Quancard, Jean, Jefferson, Anne B., Assenberg, René, Renatus, Martin, Jones, Matthew, Hassiepen, Ulrich, Schaefer, Michael, Kiffe, Michael, Weiss, Andreas, Wiesmann, Christian, Sedrani, Richard, Eder, Jörg, Martoglio, Bruno

“…The COP9 signalosome (CSN) is a central component of the activation and remodelling cycle of cullin-RING E3 ubiquitin ligases (CRLs), the largest enzyme family…”
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Pharmacological Inhibition of MALT1 Protease Leads to a Progressive IPEX-Like Pathology by Martin, Kea, Junker, Ursula, Tritto, Elaine, Sutter, Esther, Rubic-Schneider, Tina, Morgan, Hannah, Niwa, Satoru, Li, Jianping, Schlapbach, Achim, Walker, Dana, Bigaud, Marc, Beerli, Christian, Littlewood-Evans, Amanda, Rudolph, Bettina, Laisney, Marc, Ledieu, David, Beltz, Karen, Quancard, Jean, Bornancin, Frédéric, Zamurovic Ribrioux, Natasa, Calzascia, Thomas

“…Genetic disruption or short-term pharmacological inhibition of MALT1 protease is effective in several preclinical models of autoimmunity and B cell…”
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Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism by Bigaud, Marc, Dincer, Zuhal, Bollbuck, Birgit, Dawson, Janet, Beckmann, Nicolau, Beerli, Christian, Fishli-Cavelti, Gina, Nahler, Michaela, Angst, Daniela, Janser, Philipp, Otto, Heike, Rosner, Elisabeth, Hersperger, Rene, Bruns, Christian, Quancard, Jean

“…Homeostasis of vascular barriers depends upon sphingosine 1-phosphate (S1P) signaling via the S1P1 receptor. Accordingly, S1P1 competitive antagonism is known…”
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Amino−Zinc−Enolate Carbometalation Reactions:  Application to Ring Closure of Terminally Substituted Olefin for the Asymmetric Synthesis of cis- and trans-3-Prolinoleucine by Karoyan, Philippe, Quancard, Jean, Vaissermann, Jacqueline, Chassaing, Gérard

“…The amino−zinc−enolate cyclization reaction is a straightforward route for the synthesis of 3-substituted prolines. As classical intramolecular carbometalation…”
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Asymmetric Synthesis of 3-Substituted Proline Chimeras Bearing Polar Side Chains of Proteinogenic Amino Acids by Quancard, Jean, Labonne, Aurélie, Jacquot, Yves, Chassaing, Gérard, Lavielle, Solange, Karoyan, Philippe

“…The amino−zinc−ene−enolate cyclization reaction is a straightforward route to the synthesis of 3-substituted prolines. Herein we report the application of this…”
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The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit Generation by Quancard, Jean, Vulpetti, Anna, Bach, Anders, Cox, Brian, Guéret, Stéphanie M., Hartung, Ingo V., Koolman, Hannes F., Laufer, Stefan, Messinger, Josef, Sbardella, Gianluca, Craft, Russell

“…Hit generation is a crucial step in drug discovery that will determine the speed and chance of success of identifying drug candidates. Many strategies are now…”
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Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood by Quancard, Jean, Simic, Oliver, Pissot Soldermann, Carole, Aichholz, Reiner, Blatter, Markus, Renatus, Martin, Erbel, Paulus, Melkko, Samu, Endres, Ralf, Sorge, Mickael, Kieffer, Laurence, Wagner, Trixie, Beltz, Karen, Mcsheehy, Paul, Wartmann, Markus, Régnier, Catherine H, Calzascia, Thomas, Radimerski, Thomas, Bigaud, Marc, Weiss, Andreas, Bornancin, Frédéric, Schlapbach, Achim

“…The paracaspase MALT1 has gained increasing interest as a target for the treatment of subsets of lymphomas as well as autoimmune diseases, and there is a need…”
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Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing by Pissot Soldermann, Carole, Simic, Oliver, Renatus, Martin, Erbel, Paulus, Melkko, Samu, Wartmann, Markus, Bigaud, Marc, Weiss, Andreas, McSheehy, Paul, Endres, Ralf, Santos, Paulo, Blank, Jutta, Schuffenhauer, Ansgar, Bold, Guido, Buschmann, Nicole, Zoller, Thomas, Altmann, Eva, Manley, Paul W, Dix, Ina, Buchdunger, Elisabeth, Scesa, Julien, Quancard, Jean, Schlapbach, Achim, Bornancin, Frédéric, Radimerski, Thomas, Régnier, Catherine H

“…MALT1 plays a central role in immune cell activation by transducing NF-κB signaling, and its proteolytic activity represents a key node for therapeutic…”
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The T‐cell fingerprint of MALT1 paracaspase revealed by selective inhibition by Bardet, Maureen, Unterreiner, Adeline, Malinverni, Claire, Lafossas, Frédérique, Vedrine, Corinne, Boesch, Danielle, Kolb, Yeter, Kaiser, Daniel, Glück, Anton, Schneider, Martin A, Katopodis, Andreas, Renatus, Martin, Simic, Oliver, Schlapbach, Achim, Quancard, Jean, Régnier, Catherine H, Bold, Guido, Pissot‐Soldermann, Carole, Carballido, José M, Kovarik, Jiri, Calzascia, Thomas, Bornancin, Frédéric

“…Mucosa‐associated lymphoid tissue lymphoma translocation protein 1 (MALT1) is essential for immune responses triggered by antigen receptors but the…”
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The European Federation for Medicinal Chemistry (EFMC) Best Practice Initiative: Validating Chemical Probes by Quancard, Jean, Cox, Brian, Finsinger, Dirk, Guéret, Stéphanie M., Hartung, Ingo V., Koolman, Hannes F., Messinger, Josef, Sbardella, Gianluca, Laufer, Stefan

“…As part of an initiative aimed to share best practices in Medicinal Chemistry, the European Federation for Medicinal Chemistry (EFMC) is preparing a series of…”
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The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Phenotypic Drug Discovery by Quancard, Jean, Bach, Anders, Cox, Brian, Craft, Russell, Finsinger, Dirk, Guéret, Stéphanie M., Hartung, Ingo V., Laufer, Stefan, Messinger, Josef, Sbardella, Gianluca, Koolman, Hannes F.

“…Phenotypic drug discovery has a long track record of delivering innovative drugs and has received renewed attention in the last few years. The promise of this…”
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Azaindoles as Zinc‐Binding Small‐Molecule Inhibitors of the JAMM Protease CSN5 by Altmann, Eva, Erbel, Paul, Renatus, Martin, Schaefer, Michael, Schlierf, Anita, Druet, Adelaide, Kieffer, Laurence, Sorge, Mickael, Pfister, Keith, Hassiepen, Ulrich, Jones, Matthew, Ruedisser, Simon, Ostermeier, Daniela, Martoglio, Bruno, Jefferson, Anne B., Quancard, Jean

“…CSN5 is the zinc metalloprotease subunit of the COP9 signalosome (CSN), which is an important regulator of cullin‐RING E3 ubiquitin ligases (CRLs). CSN5 is…”
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N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity by Schlapbach, Achim, Revesz, Laszlo, Pissot Soldermann, Carole, Zoller, Thomas, Régnier, Catherine H., Bornancin, Frédéric, Radimerski, Thomas, Blank, Jutta, Schuffenhauer, Ansgar, Renatus, Martin, Erbel, Paulus, Melkko, Samu, Heng, Richard, Simic, Oliver, Endres, Ralf, Wartmann, Markus, Quancard, Jean

“…[Display omitted] •MALT1 plays a key role in NF-κB pathway activation.•A weak hit was optimized to potent and selective inhibitors of the MALT1.•Compounds show…”
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Requirement of Mucosa‐Associated Lymphoid Tissue Lymphoma Translocation Protein 1 Protease Activity for Fcγ Receptor–Induced Arthritis, but Not Fcγ Receptor–Mediated Platelet Elimination, in Mice by Martin, Kea, Touil, Ratiba, Cvijetic, Grozdan, Israel, Laura, Kolb, Yeter, Sarret, Sophie, Valeaux, Stéphanie, Degl'Innocenti, Elena, Le Meur, Thomas, Caesar, Nadja, Bardet, Maureen, Beerli, Christian, Zerwes, Hans‐Guenter, Kovarik, Jiri, Beltz, Karen, Schlapbach, Achim, Quancard, Jean, Régnier, Catherine H., Bigaud, Marc, Junt, Tobias, Wieczorek, Grazyna, Isnardi, Isabelle, Littlewood‐Evans, Amanda, Bornancin, Frédéric, Calzascia, Thomas

“…Objective Fcγ receptors (FcγR) play important roles in both protective and pathogenic immune responses. The assembly of the CBM signalosome encompassing…”
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Abstract 1879: Pyrazolopyrimidines as novel selective allosteric MALT1 inhibitors with in vivo activity in ABC-DLBCL by Weiss, Andreas, Radimerski, Thomas, Wyss, Daniel, Andraos, Rita, Buhles, Alexandra, Sterker, Dario, Quancard, Jean, Pissot, Carole, Simic, Oliver, Bigaud, Marc, Bornancin, Frederic, Schlapbach, Achim, Regnier, Catherine, McSheehy, Paul, Buchdunger, Elisabeth, Wartmann, Markus, Renatus, Martin, Endres, Ralf, Sellers, William, Hofmann, Francesco

“…Abstract Diffuse large B cell lymphoma (DLBCL) is the most common histological subtype of Non-Hodgkin's lymphoma, comprising 30% to 40% of all newly diagnosed…”
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An Oral Sphingosine 1‑Phosphate Receptor 1 (S1P1) Antagonist Prodrug with Efficacy in Vivo: Discovery, Synthesis, and Evaluation by Angst, Daniela, Janser, Philipp, Quancard, Jean, Buehlmayer, Peter, Berst, Frederic, Oberer, Lukas, Beerli, Christian, Streiff, Markus, Pally, Charles, Hersperger, Rene, Bruns, Christian, Bassilana, Frederic, Bollbuck, Birgit

“…A prodrug approach to optimize the oral exposure of a series of sphingosine 1-phosphate receptor 1 (S1P1) antagonists for chronic efficacy studies led to the…”
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The T‐cell fingerprint of MALT 1 paracaspase revealed by selective inhibition by Bardet, Maureen, Unterreiner, Adeline, Malinverni, Claire, Lafossas, Frédérique, Vedrine, Corinne, Boesch, Danielle, Kolb, Yeter, Kaiser, Daniel, Glück, Anton, Schneider, Martin A, Katopodis, Andreas, Renatus, Martin, Simic, Oliver, Schlapbach, Achim, Quancard, Jean, Régnier, Catherine H, Bold, Guido, Pissot‐Soldermann, Carole, Carballido, José M, Kovarik, Jiri, Calzascia, Thomas, Bornancin, Frédéric

“…Abstract Mucosa‐associated lymphoid tissue lymphoma translocation protein 1 (MALT1) is essential for immune responses triggered by antigen receptors but the…”
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The Sphingosine 1-Phosphate Receptor Subtype-1 Is the Primary Target of Fingolimod in the CNS: Interruption of the Pro-inflammatory S1P-S1P1 Cascade (P05.145) by Brinkmann, Volker, Streiff, Markus, Kaupmann, Klemens, Billich, Andreas, Faller, Thomas, Bollbuck, Birgit, Bigaud, Marc, Quancard, Jean, Kinzel, Bernd

“…Abstract only…”
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