Search Results - "Betschart, Claudia"

Target-Based Identification and Optimization of 5‑Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay by Knoepfel, Thomas, Nimsgern, Pierre, Jacquier, Sébastien, Bourrel, Marjorie, Vangrevelinghe, Eric, Glatthar, Ralf, Behnke, Dirk, Alper, Phil B, Michellys, Pierre-Yves, Deane, Jonathan, Junt, Tobias, Zipfel, Géraldine, Limonta, Sarah, Hawtin, Stuart, Andre, Cedric, Boulay, Thomas, Loetscher, Pius, Faller, Michael, Blank, Jutta, Feifel, Roland, Betschart, Claudia

“…Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the…”
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The mTOR kinase inhibitor Everolimus decreases S6 kinase phosphorylation but fails to reduce mutant huntingtin levels in brain and is not neuroprotective in the R6/2 mouse model of Huntington's disease by Fox, Jonathan H, Connor, Teal, Chopra, Vanita, Dorsey, Kate, Kama, Jibrin A, Bleckmann, Dorothee, Betschart, Claudia, Hoyer, Daniel, Frentzel, Stefan, Difiglia, Marian, Paganetti, Paolo, Hersch, Steven M

“…Huntington's disease (HD) is a progressive neurodegenerative disorder caused by a CAG repeat expansion within the huntingtin gene. Mutant huntingtin protein…”
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Distinct effects of IPSU and suvorexant on mouse sleep architecture by Hoyer, Daniel, Dürst, Thomas, Fendt, Markus, Jacobson, Laura H, Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Laue, Grit, Ofner, Silvio, Legangneux, Eric, Gee, Christine E

“…Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, SB-649868, suvorexant (MK-4305), and filorexant (MK-6096), have shown promise for the…”
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Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors by Callander, Gabrielle E, Olorunda, Morenike, Monna, Dominique, Schuepbach, Edi, Langenegger, Daniel, Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Fendt, Markus, Laue, Grit, Ofner, Silvio, Briard, Emmanuelle, Gee, Christine E, Jacobson, Laura H, Hoyer, Daniel

“…Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in…”
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Huntingtin cleavage product A forms in neurons and is reduced by gamma-secretase inhibitors by Kegel, Kimberly B, Sapp, Ellen, Alexander, Jonathan, Reeves, Patrick, Bleckmann, Dorothee, Sobin, Linsday, Masso, Nicholas, Valencia, Antonio, Jeong, Hyunkyung, Krainc, Dimitri, Palacino, James, Curtis, Daniel, Kuhn, Rainer, Betschart, Claudia, Sena-Esteves, Miguel, Aronin, Neil, Paganetti, Paolo, Difiglia, Marian

“…The mutation in Huntington's disease is a polyglutamine expansion near the N-terminus of huntingtin. Huntingtin expressed in immortalized neurons is cleaved…”
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Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture for the Treatment of Insomnia by Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Fendt, Markus, Gee, Christine E, Jacobson, Laura H, Laue, Grit, Ofner, Silvio, Chaudhari, Vinod, Badiger, Sangamesh, Pandit, Chetan, Wagner, Juergen, Hoyer, Daniel

“…Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep…”
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Structure-Based and Property-Driven Optimization of N‑Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors by Hoegenauer, Klemens, Kallen, Joerg, Jiménez-Núñez, Eloísa, Strang, Ross, Ertl, Peter, Cooke, Nigel G, Hintermann, Samuel, Voegtle, Markus, Betschart, Claudia, McKay, Daniel J. J, Wagner, Juergen, Ottl, Johannes, Beerli, Christian, Billich, Andreas, Dawson, Janet, Kaupmann, Klemens, Streiff, Markus, Gobeau, Nathalie, Harlfinger, Stephanie, Stringer, Rowan, Guntermann, Christine

“…Retinoic acid receptor-related orphan receptor gamma-t (RORγt) is considered to be the master transcription factor for the development of Th17 cells that…”
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Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway by Alper, Phil B., Deane, Jonathan, Betschart, Claudia, Buffet, David, Collignon Zipfel, Géraldine, Gordon, Perry, Hampton, Janice, Hawtin, Stuart, Ibanez, Maureen, Jiang, Tao, Junt, Tobias, Knoepfel, Thomas, Liu, Bo, Maginnis, Jillian, McKeever, Una, Michellys, Pierre-Yves, Mutnick, Daniel, Nayak, Bishnu, Niwa, Satoru, Richmond, Wendy, Rush, James S., Syka, Peter, Zhang, Yi, Zhu, Xuefeng

“…[Display omitted] Antagonism of the Toll-like receptors (TLRs) 7 and TLR8 has been hypothesized to be beneficial to patients suffering from autoimmune…”
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Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases by Alper, Phil, Betschart, Claudia, André, Cédric, Boulay, Thomas, Cheng, Dai, Deane, Jonathan, Faller, Michael, Feifel, Roland, Glatthar, Ralf, Han, Dong, Hemmig, Rene, Jiang, Tao, Knoepfel, Thomas, Maginnis, Jillian, Mutnick, Daniel, Pei, Wei, Ruzzante, Giulia, Syka, Peter, Zhang, Guobao, Zhang, Yi, Zink, Florence, Zipfel, Géraldine, Hawtin, Stuart, Junt, Tobias, Michellys, Pierre-Yves

“…Toll-like receptor (TLR) 7 and TLR8 are endosomal sensors of the innate immune system that are activated by GU-rich single stranded RNA (ssRNA). Multiple…”
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Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist by Betschart, Claudia, Faller, Michael, Zink, Florence, Hemmig, René, Blank, Jutta, Vangrevelinghe, Eric, Bourrel, Marjorie, Glatthar, Ralf, Behnke, Dirk, Barker, Kerstin, Heizmann, Andreas, Angst, Daniela, Nimsgern, Pierre, Jacquier, Sébastien, Junt, Tobias, Zipfel, Géraldine, Ruzzante, Giulia, Loetscher, Pius, Limonta, Sarah, Hawtin, Stuart, Andre, Cedric Bernard, Boulay, Thomas, Feifel, Roland, Knoepfel, Thomas

“…Inappropriate activation of TLR7 and TLR8 is linked to several auto­immune diseases, such as lupus erythema­tosus. Here we report on the efficient…”
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Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs) by Behnke, Dirk, Cotesta, Simona, Hintermann, Samuel, Fendt, Markus, Gee, Christine E., Jacobson, Laura H., Laue, Grit, Meyer, Arndt, Wagner, Trixie, Badiger, Sangamesh, Chaudhari, Vinod, Chebrolu, Murali, Pandit, Chetan, Hoyer, Daniel, Betschart, Claudia

“…[Display omitted] Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent…”
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Preclinical characterization of the Toll-like receptor 7/8 antagonist MHV370 for lupus therapy by Hawtin, Stuart, André, Cédric, Collignon-Zipfel, Géraldine, Appenzeller, Simone, Bannert, Bettina, Baumgartner, Lea, Beck, Damian, Betschart, Claudia, Boulay, Thomas, Brunner, Hermine I., Ceci, Melanie, Deane, Jonathan, Feifel, Roland, Ferrero, Enrico, Kyburz, Diego, Lafossas, Frederique, Loetscher, Pius, Merz-Stoeckle, Christina, Michellys, Pierre, Nuesslein-Hildesheim, Barbara, Raulf, Friedrich, Rush, James S., Ruzzante, Giulia, Stein, Thomas, Zaharevitz, Samantha, Wieczorek, Grazyna, Siegel, Richard, Gergely, Peter, Shisha, Tamas, Junt, Tobias

“…Genetic and in vivo evidence suggests that aberrant recognition of RNA-containing autoantigens by Toll-like receptors (TLRs) 7 and 8 drives autoimmune…”
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Structure-Based Design and Synthesis of Macroheterocyclic Peptidomimetic Inhibitors of the Aspartic Protease β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) by Hanessian, Stephen, Yang, Gaoqiang, Rondeau, Jean-Michel, Neumann, Ulf, Betschart, Claudia, Tintelnot-Blomley, Marina

“…Based on the X-ray cocrystal structure of the Tang−Ghosh heptapeptide inhibitor 1 (OM00-3), a series of macroheterocyclic analogues were designed and…”
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Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application by Lerchner, Andreas, Machauer, Rainer, Betschart, Claudia, Veenstra, Siem, Rueeger, Heinrich, McCarthy, Clive, Tintelnot-Blomley, Marina, Jaton, Anne-Lise, Rabe, Sabine, Desrayaud, Sandrine, Enz, Albert, Staufenbiel, Matthias, Paganetti, Paolo, Rondeau, Jean-Michel, Neumann, Ulf

“…Starting from macrocyclic peptidic BACE-1 inhibitor 1, brain permeation was optimized for this series using a MDRI–MDCK assay to lead to NB-216 and analogues…”
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Structure-based design and synthesis of novel P2/P3 modified, non-peptidic β-secretase (BACE-1) inhibitors by Hanessian, Stephen, Shao, Zhihui, Betschart, Claudia, Rondeau, Jean-Michel, Neumann, Ulf, Tintelnot-Blomley, Marina

“…Starting from peptidomimetic BACE-1 inhibitors, the P2 amino acid including the P2/P3 peptide bond was replaced by a rigid 3-aminomethyl cyclohexane carboxylic…”
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Corrigendum to “Structure-based design and synthesis of novel P2/P3 modified, non-peptidic β-secretase (BACE-1) inhibitors” [Bioorg. Med. Chem. Lett. 20 (2010) 1924–1927] by Hanessian, Stephen, Shao, Zhihui, Betschart, Claudia, Rondeau, Jean-Michel, Neumann, Ulf, Tintelnot-Blomley, Marina

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Structure-based design and synthesis of macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors by Machauer, Rainer, Veenstra, Siem, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Betschart, Claudia, Neumann, Ulf, Paganetti, Paolo

“…An X-ray co-crystal structure of 1 with BACE-1 allowed the design and syntheses of a series of macrocyclic analogues 3a– h. These inhibitors show improved…”
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Discovery of 1 H -pyrazolo[3,4- b ]pyridines as potent dual orexin receptor antagonists (DORAs) by Behnke, Dirk, Cotesta, Simona, Hintermann, Samuel, Fendt, Markus, Gee, Christine E., Jacobson, Laura H., Laue, Grit, Meyer, Arndt, Wagner, Trixie, Badiger, Sangamesh, Chaudhari, Vinod, Chebrolu, Murali, Pandit, Chetan, Hoyer, Daniel, Betschart, Claudia

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Macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors with activity in vivo by Machauer, Rainer, Laumen, Kurt, Veenstra, Siem, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Betschart, Claudia, Jaton, Anne-Lise, Desrayaud, Sandrine, Staufenbiel, Matthias, Rabe, Sabine, Paganetti, Paolo, Neumann, Ulf

“…The macrocyclic peptidic BACE-1 inhibitors 2a– c were optimized to the highly potent and selective inhibitor 3. This compound shows inhibition of BACE-1 in the…”
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2-Cyano-pyrimidines:  A New Chemotype for Inhibitors of the Cysteine Protease Cathepsin K by Altmann, Eva, Aichholz, Reiner, Betschart, Claudia, Buhl, Thomas, Green, Jonathan, Irie, Osamu, Teno, Naoki, Lattmann, René, Tintelnot-Blomley, Marina, Missbach, Martin

“…Starting from the purine lead structure 1, a new series of cathepsin K inhibitors based on a pyrimidine scaffold have been explored. Investigations of P3 and…”
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