Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Peter Drückes"'
Autor:
Andrew C. Pearce, Sylvie Chamoin, Matthew Thomas, Loren Jon, Deborah Haggart, Sonia P. Roberts, Christopher Thomson, John Reilly, Vikki Furminger, Ian N. Bruce, Peter Drückes, Sarah Cross, Rowan Stringer, Ferheen Baig, Satish Dayal, Duncan Shaw, Irena Konstantinova, Alex Michael Saunders, Stephen Paul Collingwood, Ben Wen, Valentina Molteni, Christine Tomlins, Martin Hussey, Lilya Sviridenko, Pascal Furet, Vince Yeh
Publikováno v:
Journal of Medicinal Chemistry. 59:7901-7914
A series of potent PDGFR inhibitors has been identified. The series was optimized for duration of action in the lung. A novel kinase occupancy assay was used to directly measure target occupancy after i.t. dosing. Compound 25 shows 24 h occupancy of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d4a9f2b3687745cf42852d7db9e8174
https://doi.org/10.1021/acs.jmedchem.6b00703
https://doi.org/10.1021/acs.jmedchem.6b00703
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:
Markus Wartmann, Josef Brüggen, Guido Bold, Marion Burglin, Arnaud Goepfert, Jürgen Mestan, Paul W. Manley, Jacqueline Loretan, Jeanette Marjorie Wood, Andreas Theuer, Georg Martiny-Baron, Peter Drückes, Peter R. Allegrini, Ursula Dürler, Paul M.J. McSheehy, Pascal Furet, Amanda Littlewood-Evans, Christian Schnell, Beatrice Bauer-Probst, Robert Reuter
Publikováno v:
Journal of medicinal chemistry. 59(1)
This paper describes the identification of 6-(pyrimidin-4-yloxy)-naphthalene-1-carboxamides as a new class of potent and selective human vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase inhibitors. In biochemical and cellular as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17bed0347393c7c07fa972a8d2ca8ef8
https://pubmed.ncbi.nlm.nih.gov/26629594
https://pubmed.ncbi.nlm.nih.gov/26629594
Autor:
Gebhard Thoma, Peter Drückes, Friedrich Raulf, Catherine Rolvering, Iris Behrmann, Manuela Kapp, Hans-Günter Zerwes, Claude Haan
Publikováno v:
Chemistry & Biology. 18:314-323
SummaryGenetic deficiency of Jak3 leads to abrogation of signal transduction through the common gamma chain (γc) and thus to immunodeficiency suggesting that specific inhibition of Jak3 kinase may result in immunosuppression. Jak1 cooperates with Ja
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d89d519c6f6f3ae81c456ba3d53f45e1
https://doi.org/10.1016/j.chembiol.2011.01.012
https://doi.org/10.1016/j.chembiol.2011.01.012
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:
Felix Muth, Marcel Günther, Silke M. Bauer, Eva Döring, Sabine Fischer, Julia Maier, Peter Drückes, Jürgen Köppler, Jörg Trappe, Ulrich Rothbauer, Pierre Koch, Stefan A. Laufer
Publikováno v:
Journal of medicinal chemistry. 58(1)
Tetra-substituted imidazoles were designed as dual inhibitors of c-Jun N-terminal kinase (JNK) 3 and p38α mitogen-activated protein (MAP) kinase. A library of 45 derivatives was prepared and evaluated in a kinase activity assay for their ability to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::573a3fd1db03a843a8ddace1a04c121f
https://pubmed.ncbi.nlm.nih.gov/25719747
https://pubmed.ncbi.nlm.nih.gov/25719747
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(19)
Jak3, together with Jak1, is involved in signal transduction initiated by cytokines signaling through the common gamma chain which are important in immune homeostasis and immune pathologies. Based on genetic evidence Jak3 has been considered to be an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d854102fce9123a6ddee276ba2ea2dbd
https://pubmed.ncbi.nlm.nih.gov/25217444
https://pubmed.ncbi.nlm.nih.gov/25217444
Autor:
Jianwei John Che, Peter Drückes, Eric Vangrevelinghe, Alexander Baxter Smith, Hans-Günter Zerwes, Maurice Van Eis, Jin Yunho, Tetsuo Uno, Joachim Blanz, Peter Buhlmayer, Christian C. Lee, Xiaohui He, Matthias Kittelmann, Hong Liu, Gebhard Thoma, Pierre-Yves Michellys
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(10)
We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic assays, cellular assays and in primary cells in the presence of blood. Introduction of a 7-aminoindole substituent led to derivatives with good kinase s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34fee44d362711c1d8b04d94d4a833a8
https://pubmed.ncbi.nlm.nih.gov/24726806
https://pubmed.ncbi.nlm.nih.gov/24726806
Autor:
Kaspar Zimmermann, Derya R. Shimshek, Tatjana Schweizer, Giorgio Rovelli, Sandrine Desrayaud, Daniela Stauffer, Troxler Thomas J, Paulette Greenidge, Peter Drückes
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(14)
Mutations in leucine-rich repeat kinase-2 (LRRK2) are the most common genetic cause of Parkinson’s disease (PD). The most frequent kinase-enhancing mutation is the G2019S residing in the kinase activation domain. This opens up a promising therapeut
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e5afd35b4b5b71520acdcdbcfd43699
https://pubmed.ncbi.nlm.nih.gov/23768909
https://pubmed.ncbi.nlm.nih.gov/23768909
Autor:
Sabine Cecile Fischer, Pierre Koch, Ulrich Rothbauer, Julia Maier, Silke M. Bauer, Jürgen Köppler, Eva Döring, Stefan Laufer, Jörg Trappe, Felix Muth, Marcel Günther, Peter Drückes
Publikováno v:
Journal of Medicinal Chemistry. 58:2567-2567
Tetra-substituted imidazoles were designed as dual inhibitors of c-Jun N-terminal kinase (JNK) 3 and p38α mitogen-activated protein (MAP) kinase. A library of 45 derivatives was prepared and evaluated in a kinase activity assay for their ability to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5f601cbc8b4ebed5ce127e7c97c40144
https://doi.org/10.1021/acs.jmedchem.5b00235
https://doi.org/10.1021/acs.jmedchem.5b00235