Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Ruben, de Kanter"'
Autor:
Saskia M. Brachmann, Simona Cotesta, Anna F. Farago, Frederic Zecri, Kun Xu, Rainer Wilcken, Toni Widmer, Peter Wessels, Hans Voshol, Andrea Vaupel, Rowan Stringer, Toshio Shimizu, Richard Sedrani, Christian Schnell, Danielle Roman, Pascal Rigollier, Johannes Ottl, Nils Ostermann, Helen Oakman, Jason Murphy, Sauveur-Michel Maira, Catherine Leblanc, Jeffrey D. Kearns, Eloísa Jiménez Núñez, Ashley Jaeger, Victoria Head, Daniel Alexander Guthy, Marc Gerspacher, Carmine Fedele, Lekshmi Dharmarajan, Ruben de Kanter, Xiaoming Cui, Xueying Chen, Heather Burks, Claudio Bomio-Confaglia, Kim S. Beyer, Louise Barys, Edwige Lorthiois, Andreas Weiss
Covalent inhibitors of KRASG12C have shown antitumor activity against advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and additional strategies are needed to improve outcomes. JDQ443 is a structurally unique covalent inhibitor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::090908cffff39039ae33828ed26022f4
https://doi.org/10.1158/2159-8290.c.6549647
https://doi.org/10.1158/2159-8290.c.6549647
Autor:
Andreas Weiss, Edwige Lorthiois, Louise Barys, Kim S. Beyer, Claudio Bomio-Confaglia, Heather Burks, Xueying Chen, Xiaoming Cui, Ruben de Kanter, Lekshmi Dharmarajan, Carmine Fedele, Marc Gerspacher, Daniel Alexander Guthy, Victoria Head, Ashley Jaeger, Eloísa Jiménez Núñez, Jeffrey D. Kearns, Catherine Leblanc, Sauveur-Michel Maira, Jason Murphy, Helen Oakman, Nils Ostermann, Johannes Ottl, Pascal Rigollier, Danielle Roman, Christian Schnell, Richard Sedrani, Toshio Shimizu, Rowan Stringer, Andrea Vaupel, Hans Voshol, Peter Wessels, Toni Widmer, Rainer Wilcken, Kun Xu, Frederic Zecri, Anna F. Farago, Simona Cotesta, Saskia M. Brachmann
Publikováno v:
Cancer Discovery. 12:1500-1517
Covalent inhibitors of KRASG12C have shown antitumor activity against advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and additional strategies are needed to improve outcomes. JDQ443 is a structurally unique covalent inhibitor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2edd83624df412b8b1d836bfe665fa6
https://doi.org/10.1158/2159-8290.cd-22-0158
https://doi.org/10.1158/2159-8290.cd-22-0158
Autor:
Olivier Bezençon, Thomas Pfeifer, Johannes Mosbacher, Isabelle Reymond, Eric A. Ertel, Ruben de Kanter, Bruno Capeleto, Elvire Fournier, Markus Rey, Luca Moccia, Michael Toeroek-Schafroth, René Roscher, Richard Moon, John Gatfield, Melanie Kessler, Romain Siegrist, Bibia Heidmann, Davide Pozzi, Simon Stamm, Luboš Remeň, Sylvia Richard, Lloyd Simons, Rick Gaston, Dennis Downing, Corinna Grisostomi, Catherine Roch, Benno Schindelholz
Publikováno v:
CHIMIA, Vol 71, Iss 10 (2017)
We describe the discovery and optimization of new, brain-penetrant T-type calcium channel blockers. We present optimized compounds with excellent efficacy in a rodent model of generalized absence-like epilepsy. Along the fine optimization of a chemic
Externí odkaz:
https://doaj.org/article/77760779eafd425e854518b6109e1f36
Autor:
Amélie Le Bihan, Ruben de Kanter, Iñigo Angulo-Barturen, Christoph Binkert, Christoph Boss, Reto Brun, Ralf Brunner, Stephan Buchmann, Jeremy Burrows, Koen J Dechering, Michael Delves, Sonja Ewerling, Santiago Ferrer, Christoph Fischli, Francisco Javier Gamo-Benito, Nina F Gnädig, Bibia Heidmann, María Belén Jiménez-Díaz, Didier Leroy, Maria Santos Martínez, Solange Meyer, Joerg J Moehrle, Caroline L Ng, Rintis Noviyanti, Andrea Ruecker, Laura María Sanz, Robert W Sauerwein, Christian Scheurer, Sarah Schleiferboeck, Robert Sinden, Christopher Snyder, Judith Straimer, Grennady Wirjanata, Jutta Marfurt, Ric N Price, Thomas Weller, Walter Fischli, David A Fidock, Martine Clozel, Sergio Wittlin
Publikováno v:
PLoS Medicine, Vol 13, Iss 10, p e1002138 (2016)
BackgroundArtemisinin resistance observed in Southeast Asia threatens the continued use of artemisinin-based combination therapy in endemic countries. Additionally, the diversity of chemical mode of action in the global portfolio of marketed antimala
Externí odkaz:
https://doaj.org/article/c760742987d34859b710bc8b89e29d3c
Autor:
Andreas Weiss, Hans Voshol, Diana Graus Porta, Carmine Fedele, Dario Sterker, Ruben De Kanter, Rowan Stringer, Toni Widmer, Alice Loo, Daniel A. Guthy, Kim S. Beyer, Nils Ostermann, Catherine LeBlanc, Marc Gerspacher, Andrea Vaupel, Richard Sedrani, Frederic Zecri, Saveur-Michel Maria, Francesco Hofmann, Peter Hammerman, Jeff Engelman, Edwige Lorthiois, Simona Cotesta, Saskia M. Brachmann
Publikováno v:
Cancer Research. 82:4026-4026
Background: Oncogenic mutations occurring in the KRAS component of the RAS/MAPK pathway slow nucleotide cycling between its active (GTP-bound) and inactive (GDP-bound) states, shifting it towards the active state and increasing oncogenic signaling. A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::214f14f8dca262dae57cbef9b3bf8657
https://doi.org/10.1158/1538-7445.am2022-4026
https://doi.org/10.1158/1538-7445.am2022-4026
Autor:
Saskia M. Brachmann, Andreas Weiss, Daniel A. Guthy, Kim Beyer, Johannes Voshol, Michel Maira, Anirudh Prahallad, Diana Graus Porta, Christian Schnell, Nils Ostermann, Andrea Vaupel, Marc Gerspacher, Catherine Leblanc, Dirk Erdmann, Dario Sterker, Grainne Kerr, Giovannoni Jerome, Victoria Head, Rowan Stringer, Ruben De Kanter, Kearns Jeff, Danielle Roman, Toni Widmer, Peter Wessels, Eloisa Jimenez Nunez, Richard Sedrani, Frederic Zecri, Francesco Hofmann, Jeff Engleman, Edwige Lorthiois, Simona Cotesta
Publikováno v:
Molecular Cancer Therapeutics. 20:P124-P124
RAS is the most frequently mutated oncogene in cancer. KRAS G12C mutations are most prevalent in lung adenocarcinoma (~13%) and colorectal adenocarcinoma (~4%), and occur less commonly in other solid tumor malignancies. First generation KRASG12C inhi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ad4b8e929a5d91731e7278c2de32193c
https://doi.org/10.1158/1535-7163.targ-21-p124
https://doi.org/10.1158/1535-7163.targ-21-p124
Autor:
Thomas Weller, Martin Bolli, Claus Müller, Ruben de Kanter, Markus Rey, Magdalena Birker, Patrick Sieber, Cyrille Lescop, Christopher Kohl, Boris Mathys, Beat Steiner, Patrick Hess, Oliver Nayler
Publikováno v:
European Journal of Medicinal Chemistry. 116:222-238
In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound clas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dc8392021bea5d4bf4ef196324d4ad8
https://doi.org/10.1016/j.ejmech.2016.03.048
https://doi.org/10.1016/j.ejmech.2016.03.048
Autor:
Magdalena Birker, Jörg Velker, Patrick Hess, Ruben de Kanter, Oliver Nayler, Markus Rey, Beat Steiner, Martin Bolli, Patrick Sieber, Christopher Kohl, Cyrille Lescop, Thomas Weller
Publikováno v:
European Journal of Medicinal Chemistry. 115:326-341
In a previous communication we reported on the discovery of aminopyridine 1 as a potent, selective and orally active S1P1 receptor agonist. More detailed studies revealed that this compound is phototoxic in vitro. As a result of efforts aiming at eli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1efce13dfcace03905e7c2c4dd907002
https://doi.org/10.1016/j.ejmech.2016.03.020
https://doi.org/10.1016/j.ejmech.2016.03.020
Autor:
Alexander Treiber, Stephan Buchmann, Jérôme Segrestaa, Stephane Delahaye, Christopher Kohl, Patricia N. Sidharta, Ruben de Kanter, Carmela Gnerre
Publikováno v:
Clinical Pharmacokinetics. 55:369-380
Macitentan is a novel dual endothelin receptor antagonist for the treatment of pulmonary arterial hypertension (PAH). It is metabolized by cytochrome P450 (CYP) enzymes, mainly CYP3A4, to its active metabolite ACT-132577. A physiological-based pharma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::669f53028d4dc15d96cd127676fa208d
https://doi.org/10.1007/s40262-015-0322-y
https://doi.org/10.1007/s40262-015-0322-y
Autor:
Alexander Treiber, Swen Seeland, Tomohiko Ichikawa, Tetsuhiro Yamada, Päivi Äänismaa, Stephane Delahaye, Carmela Gnerre, Ruben de Kanter, Thomas Pfeifer, Jérôme Segrestaa
Publikováno v:
Xenobiotica; the fate of foreign compounds in biological systems. 48(7)
1. The metabolism of selexipag has been studied in vivo in man and the main excreted metabolites were identified. Also, metabolites circulating in human plasma have been structurally identified and quantified. 2. The main metabolic pathway of selexip
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0914760012925198a0329ac8a3bf9a1e
https://pubmed.ncbi.nlm.nih.gov/28737453
https://pubmed.ncbi.nlm.nih.gov/28737453