Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Ralf Glatthar"'
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:
Ralf Glatthar, Robert H. Arch
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery. :1-71
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::70f634245c6cb332c96ffee577d0ca9a
https://doi.org/10.1002/0471266949.bmc274
https://doi.org/10.1002/0471266949.bmc274
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:
Ralf Glatthar, John E. Peel, Henri Mattes, Gabriele Fendrich, Helmut Sparrer, Henrik Möbitz, Jeff Hornfeld, Rene Beerli, Peter Drückes, Fiona Spence, Aleksandar Stojanovic, Ernst Gassmann, Georg Martiny-Baron, Troxler Thomas J, Joachim Blanz, Sascha Gutmann
Publikováno v:
Journal of medicinal chemistry. 59(16)
Cancer Osaka thyroid (COT) kinase is an important regulator of pro-inflammatory cytokines in macrophages. Thus, pharmacologic inhibition of COT should be a valid approach to therapeutically intervene in the pathogenesis of macrophage-driven inflammat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6bb3994705533230375f27d365ac651b
https://pubmed.ncbi.nlm.nih.gov/27502541
https://pubmed.ncbi.nlm.nih.gov/27502541
Autor:
Sandrine Desrayaud, David Carcache, Ivan-Toma Vranesic, Ralf Glatthar, Joachim Blanz, Markus Fendt
Publikováno v:
ACS Medicinal Chemistry Letters. 2:58-62
A focused chemical optimization effort of compound 1 based on metabolite elucidation is described, resulting in 15i, a highly potent and selective mGlu5 receptor antagonist with an improved pharmacokinetic profile compared to 1. Characterization of 1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e0a06b6ff89ad2b4f21d09b8e30c6c0
https://doi.org/10.1021/ml100215b
https://doi.org/10.1021/ml100215b
Autor:
Ivo Vranesic, Markus Fendt, Ralf Glatthar, Troxler Thomas J, David Orain, Carsten Spanka, Sandrine Desrayaud
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:184-188
High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa426c0b25e7903d5f635267036e47bf
https://doi.org/10.1016/j.bmcl.2009.11.001
https://doi.org/10.1016/j.bmcl.2009.11.001
Autor:
Niko Schmiedeberg, Gabriele Fendrich, Ralf Glatthar, Henrik Möbitz, André Strauss, Sascha Gutmann, Silvio Ofner, Peter Drückes, Sylvie Antz, Aleksandar Stojanovic, Helmut Sparrer, S. Rieffel, Henri Mattes, Alexandra Hinniger, Troxler Thomas J
Publikováno v:
The Journal of biological chemistry. 290(24)
Macrophages are important cellular effectors in innate immune responses and play a major role in autoimmune diseases such as rheumatoid arthritis. Cancer Osaka thyroid (COT) kinase, also known as mitogen-activated protein kinase kinase kinase 8 (MAP3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b3e5b0ee5576c7802d57675ce481965
https://pubmed.ncbi.nlm.nih.gov/25918157
https://pubmed.ncbi.nlm.nih.gov/25918157
Autor:
Ralf Glatthar, Philip M. Harrington, Scott E. Schaus, Elaine Y. Kuo, Jia-Ning Xiang, Jun Liang, Andrew G. Myers, Yusheng Wu, Marlys Hammond
Publikováno v:
Journal of the American Chemical Society. 124:5380-5401
A convergent, enantioselective synthetic route to the natural product neocarzinostatin chromophore (1) is described. Synthesis of the chromophore aglycon (2) was targeted initially. Chemistry previously developed for the synthesis of a neocarzinostat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2939c1449c8a7b46670fbb47c048a723
https://doi.org/10.1021/ja012487x
https://doi.org/10.1021/ja012487x
Autor:
Ivo Vranesic, Markus Fendt, Silvio Ofner, Kaspar Zimmermann, Ralf Glatthar, Grit Laue, Daniel Peterlik, Klemens Kaupmann, Dominik Feuerbach, Christine E. Gee, Rochdi Bouhelal, Peter J. Flor, Herman van der Putten, Christoph Neuhäuser, Nicole Uschold-Schmidt, John F. Cryan
Publikováno v:
The Journal of biological chemistry. 289(16)
The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. mGlu7 function has been linked to autism, drug abuse, anxiety, and depression. Despite this, it has been difficult
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35d470b156affce7a8cb2c77a1868896
https://pubmed.ncbi.nlm.nih.gov/24596089
https://pubmed.ncbi.nlm.nih.gov/24596089
Autor:
Wolfgang Damm, Martin Spichty, Andreas Gugger, Rohit Batra, Ralf Glatthar, Bernd Giese, Matthias Mohr, Hendrik Zipse
Publikováno v:
Tetrahedron. 56:4117-4128
In order to understand the heterolytic cleavage of 4′-DNA radical 1 and the regioselective attack of nucleophiles at the intermediate DNA radical cation 3, the chemistry of model radical 8 was studied. It turned out that the heterolytic cleavage in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::86fe18dccf9c2d84c7fcf544693f9ed5
https://doi.org/10.1016/s0040-4020(00)00335-5
https://doi.org/10.1016/s0040-4020(00)00335-5