Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Joachim Blanz"'
Autor:
Ying Huang, Martin Sendzik, Jeff Zhang, Zhenting Gao, Yongfeng Sun, Long Wang, Justin Gu, Kehao Zhao, Zhengtian Yu, Lijun Zhang, Qiong Zhang, Joachim Blanz, Zijun Chen, Valérie Dubost, Douglas Fang, Lijian Feng, Xingnian Fu, Michael Kiffe, Ling Li, Fangjun Luo, Xiao Luo, Yuan Mi, Prakash Mistry, David Pearson, Alessandro Piaia, Clemens Scheufler, Remi Terranova, Andreas Weiss, Jue Zeng, Hailong Zhang, Jiangwei Zhang, Mengxi Zhao, Michael P. Dillon, Sebastien Jeay, Wei Qi, Jonathan Moggs, Carole Pissot-Soldermann, En Li, Peter Atadja, Andreas Lingel, Counde Oyang
Publikováno v:
Journal of Medicinal Chemistry. 65:5317-5333
Polycomb Repressive Complex 2 (PRC2) plays an important role in transcriptional regulation during animal development and in cell differentiation, and alteration of PRC2 activity has been associated with cancer. On a molecular level, PRC2 catalyzes me
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e8a2d3773ad89ebc7852a400a3f915e
https://doi.org/10.1021/acs.jmedchem.1c02148
https://doi.org/10.1021/acs.jmedchem.1c02148
Autor:
Thomas Vorherr, Felix Huth, Ian Lewis, Joachim Blanz, Joerg Berghausen, Kirsten Schroer, Michael Schaefer, Reiner Aichholz, Roman Wille, Thomas Lochmann
Publikováno v:
American Journal of Medicinal Chemistry. :1-10
Following up on a previous publication in which we reported a high liver first pass effect in rats for the cyclic peptide (1) [Ala-Leu-NMe-D-Leu-NMe-Leu-Leu-D-Pro], we decided to investigate the type of metabolites formed and to suggest solutions to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1f337c425ea2a95d90ab391e881c27ba
https://doi.org/10.31487/j.ajmc.2019.01.01
https://doi.org/10.31487/j.ajmc.2019.01.01
Autor:
Ji Yue Jeff Zhang, Jiang Wei Zhang, Yi Jin, Counde Oyang, C. Zhang, Markus Walles, Lijun Zhang, Joachim Blanz, Jerôme Dayer, Michael Kiffe, Ying Huang, Arevalo Sanchez
Publikováno v:
Xenobiotica; the fate of foreign compounds in biological systems. 52(1)
1. MAK683 (N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine) is a potent and orally bioavailable EED inhibitor for the potential treatment in oncology. Pharmacokinetics (PK) in preclinic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9722094e59dabab5ac1a99b6b8357560
https://pubmed.ncbi.nlm.nih.gov/34761729
https://pubmed.ncbi.nlm.nih.gov/34761729
Autor:
Joachim Blanz, Philippe Ramstein, Thierry Délémonté, Reiner Aichholz, Werner Gertsch, Markus Trunzer, Jerôme Dayer, David Pearson, Gareth Williams
Publikováno v:
Journal of Mass Spectrometry. 52:210-217
Drug metabolism studies are performed in drug discovery to identify metabolic soft spots, detect potentially toxic or reactive metabolites and provide an early insight into potential species differences. The relative peak area approach is often used
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::10057a80e3525bd31fdc3bdd8631b7ac
https://doi.org/10.1002/jms.3918
https://doi.org/10.1002/jms.3918
Autor:
Ross Strang, Siem Jacob Veenstra, Christian C. Lee, Hans-Günter Zerwes, Joachim Blanz, Gebhard Thoma, Eric Vangrevelinghe, Jörg Berghausen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25(20):4642-4647
Design and optimization of benzo- and pyrido-thiazoles/isothiazoles are reported leading to the discovery of the potent, orally bioavailable Syk inhibitor 5, which was found to be active in a rat PK/PD model. Compound 5 showed acceptable overall kina
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30b0294df6a2a05cd50e0efbdca8f711
Autor:
Amanda Littlewood-Evans, Ross Strang, Nicolas Soldermann, Klemens Hoegenauer, Sascha Gutmann, Gabriele Rummel, Greg Hollingworth, Frédéric Zecri, Romain M. Wolf, Christoph Burkhart, Nigel Graham Cooke, Alexander Baxter Smith, Nadege Graveleau, Joachim Blanz
Publikováno v:
ACS medicinal chemistry letters. 8(9)
The predominant expression of phosphoinositide 3-kinase δ (PI3Kδ) in leukocytes and its critical role in B and T cell functions led to the hypothesis that selective inhibitors of this isoform would have potential as therapeutics for the treatment o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca7a12eb7e1f78c670cdafb54756b9c7
https://pubmed.ncbi.nlm.nih.gov/28947947
https://pubmed.ncbi.nlm.nih.gov/28947947
Autor:
Joachim, Blanz, Gareth, Williams, Jerôme, Dayer, Thierry, Délémonté, Werner, Gertsch, Philippe, Ramstein, Reiner, Aichholz, Markus, Trunzer, David, Pearson
Publikováno v:
Journal of mass spectrometry : JMS. 52(4)
Drug metabolism studies are performed in drug discovery to identify metabolic soft spots, detect potentially toxic or reactive metabolites and provide an early insight into potential species differences. The relative peak area approach is often used
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::9fd1584bb27f564a72a6d59bf79cac55
https://pubmed.ncbi.nlm.nih.gov/28152561
https://pubmed.ncbi.nlm.nih.gov/28152561
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:
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:
Joachim Nozulak, Klemens Kaupmann, Reiner Aichholz, Samuel Hintermann, Joachim Blanz, Johannes Mosbacher, Konstanze Hurth, Marina Tintelnot-Blomley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1523-1526
A novel series of agonists at the benzodiazepine binding site of the GABAA receptor was prepared by functionalizing a known template. Adding substituents to the pyrazolone-oxygen of CGS-9896 led to a number of compounds with selectivities for either
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05cd6fb8c518d6565fc67d6b454e58c3
https://doi.org/10.1016/j.bmcl.2010.12.107
https://doi.org/10.1016/j.bmcl.2010.12.107