Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Roland Feifel"'
Autor:
Claudia Betschart, Michael Faller, Florence Zink, René Hemmig, Jutta Blank, Eric Vangrevelinghe, Marjorie Bourrel, Ralf Glatthar, Dirk Behnke, Kerstin Barker, Andreas Heizmann, Daniela Angst, Pierre Nimsgern, Sébastien Jacquier, Tobias Junt, Géraldine Zipfel, Giulia Ruzzante, Pius Loetscher, Sarah Limonta, Stuart Hawtin, Cedric Bernard Andre, Thomas Boulay, Roland Feifel, Thomas Knoepfel
Publikováno v:
ACS Med Chem Lett
[Image: see text] Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. Here we report on the efficient structure-based optimization of the inhibition of TLR8, starting from a co-crystal stru
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33fee8bacdcd6ab213f658c3a1348d56
https://doi.org/10.1021/acsmedchemlett.1c00696
https://doi.org/10.1021/acsmedchemlett.1c00696
Autor:
Stuart Hawtin, Cédric André, Géraldine Collignon-Zipfel, Simone Appenzeller, Bettina Bannert, Lea Baumgartner, Damian Beck, Claudia Betschart, Thomas Boulay, Hermine I. Brunner, Melanie Ceci, Jonathan Deane, Roland Feifel, Enrico Ferrero, Diego Kyburz, Frederique Lafossas, Pius Loetscher, Christina Merz-Stoeckle, Pierre Michellys, Barbara Nuesslein-Hildesheim, Friedrich Raulf, James S. Rush, Giulia Ruzzante, Thomas Stein, Samantha Zaharevitz, Grazyna Wieczorek, Richard Siegel, Peter Gergely, Tamas Shisha, Tobias Junt
Publikováno v:
Cell Reports Medicine. 4:101036
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::951c34b5b48eafcb29d9636e9e49f20e
https://doi.org/10.1016/j.xcrm.2023.101036
https://doi.org/10.1016/j.xcrm.2023.101036
Autor:
Jonathan A. Deane, Stuart Hawtin, Roland Feifel, Pius Loetscher, Sarah Limonta, Tobias Junt, Ralf Glatthar, Michellys Pierre-Yves, Marjorie Bourrel, Thomas Knoepfel, Cedric Bernard Andre, Thomas Boulay, Pierre Nimsgern, Sebastien Jacquier, Eric Vangrevelinghe, Michael Faller, Claudia Betschart, Jutta Blank, Phillip B. Alper, Geraldine Collignon Zipfel, Dirk Behnke
Publikováno v:
Journal of Medicinal Chemistry. 63:8276-8295
Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a TLR8 antagonist competition assay and its application for hit generation of dual
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98a6d30a18c77cefd130b9738cd75108
https://doi.org/10.1021/acs.jmedchem.0c00130
https://doi.org/10.1021/acs.jmedchem.0c00130
Autor:
Nello Mainolfi, Takeru Ehara, Rajeshri G. Karki, Karen Anderson, Aengus Mac Sweeney, Sha-Mei Liao, Upendra A. Argikar, Keith Jendza, Chun Zhang, James Powers, Daniel W. Klosowski, Maura Crowley, Toshio Kawanami, Jian Ding, Myriam April, Cornelia Forster, Michael Serrano-Wu, Michael Capparelli, Rrezarta Ramqaj, Catherine Solovay, Frederic Cumin, Thomas M. Smith, Luciana Ferrara, Wendy Lee, Debby Long, Melissa Prentiss, Andrea De Erkenez, Louis Yang, Fang Liu, Holger Sellner, Finton Sirockin, Eric Valeur, Paulus Erbel, Daniela Ostermeier, Paul Ramage, Bernd Gerhartz, Anna Schubart, Stefanie Flohr, Nathalie Gradoux, Roland Feifel, Barbara Vogg, Christian Wiesmann, Jürgen Maibaum, Jörg Eder, Richard Sedrani, Richard A. Harrison, Muneto Mogi, Bruce D. Jaffee, Christopher M. Adams
Publikováno v:
Journal of Medicinal Chemistry. 63:5697-5722
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::161530bd60ced781537b4b5cf97869fc
https://doi.org/10.1021/acs.jmedchem.9b01870
https://doi.org/10.1021/acs.jmedchem.9b01870
Autor:
Roland Feifel, Ernst Blum, Richard Heng, Achim Schlapbach, Juraj Velcicky, Daniel Pflieger, Laszlo Revesz, Stuart Hawtin, Rene Hersperger, Christine Huppertz
Publikováno v:
ACS Medicinal Chemistry Letters. 9:392-396
[Image: see text] MAP-activated protein kinase 2 (MK2) plays an important role in the regulation of innate immune response as well as in cell survival upon DNA damage. Despite its potential for the treatment of inflammation and cancer, to date no MK2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eaf9d762d801fcd1e9dbcf6f7a5780a5
https://doi.org/10.1021/acsmedchemlett.8b00098
https://doi.org/10.1021/acsmedchemlett.8b00098
Autor:
Roland Feifel, Philip C. Smith, Ursula Bodendorf, Robert Epple, Philippe Couttet, Reiner Aichholz, Danilo Guerini, Ina Dix, Ben Wen, Bo Liu, Peter Wipfli, Juraj Velcicky, Toni Widmer, Trixi Brandl, Daniel R. Beisner, Pascal Rigollier
Publikováno v:
Journal of Medicinal Chemistry. 61:865-880
Signal peptide peptidase-like 2a (SPPL2a) is an aspartic intramembrane protease which has recently been shown to play an important role in the development and function of antigen presenting cells such as B lymphocytes and dendritic cells. In this pap
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f019f401a7282949702f439bc69e4e37
https://doi.org/10.1021/acs.jmedchem.7b01371
https://doi.org/10.1021/acs.jmedchem.7b01371
Autor:
Klaus Weigand, Andrea Vaupel, Roland Feifel, Berndt Oberhauser, Janet Dawson King, Mark Nash, Pius Loetscher, Amanda Littlewood-Evans, David Orain, Wolfgang Miltz, Juraj Velcicky
Publikováno v:
Journal of Medicinal Chemistry. 60:3672-3683
A novel, selective, and efficacious GPR4 antagonist 13 was developed starting from lead compound 1a. While compound 1a showed promising efficacy in several disease models, its binding to a H3 receptor as well as a hERG channel prevented it from furth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d140d7ef0960f3398069f19f6c5bc89f
https://doi.org/10.1021/acs.jmedchem.6b01703
https://doi.org/10.1021/acs.jmedchem.6b01703
Autor:
Mark Nash, Janet Dawson, Arndt Meyer, Berndt Oberhauser, Klaus Seuwen, Juraj Velcicky, Pius Loetscher, Amanda Littlewood-Evans, Wolfgang Miltz, Daniela Gabriel, Marie-Gabrielle Ludwig, Roland Feifel
Publikováno v:
Bioorganicmedicinal chemistry. 25(16)
GPR4, a G-protein coupled receptor, functions as a proton sensor being activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. An orally active GPR4 antagoni
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8cc6c03181dbdf3b83e947377cef6b8
https://pubmed.ncbi.nlm.nih.gov/28689977
https://pubmed.ncbi.nlm.nih.gov/28689977
Autor:
Nicolas Soldermann, Gregory Hollingworth, Christina Hebach, Frédéric Zecri, Pascal Furet, Sascha Gutmann, Roland Feifel, Romain M. Wolf, Klemens Hoegenauer, Ian Lewis, Christoph Burkhart, Alexander Baxter Smith, Gabriele Rummel, Nadege Graveleau, Joachim Blanz, Frédéric Stauffer, Mark Knapp
Inhibition of the lipid kinase PI3Kδ is a promising principle to treat B and T cell driven inflammatory diseases. Using a scaffold deconstruction–reconstruction strategy, we identified 4-aryl quinazolines that were optimized into potent PI3Kδ iso
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8da9dae3e977fa85e7ce87fa0dd5426b
https://europepmc.org/articles/PMC4983741/
https://europepmc.org/articles/PMC4983741/
Autor:
Laszlo Revesz, Achim Schlapbach, Reiner Aichholz, Roland Feifel, Stuart Hawtin, Richard Heng, Peter Hiestand, Wolfgang Jahnke, Guido Koch, Markus Kroemer, Henrik Möbitz, Clemens Scheufler, Juraj Velcicky, Christine Huppertz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4715-4718
Pyrrolo[2,3-f]isoquinoline based amino acids, tetracyclic lactams and cyclic ketone analogues are described as novel MK2 inhibitors with IC(50) as low as 5nM and good selectivity profiles against a number of related kinases including ERK, p38alpha an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0fac2d9fd29dbe422fca2ca8db35aa03
https://doi.org/10.1016/j.bmcl.2010.04.024
https://doi.org/10.1016/j.bmcl.2010.04.024