Zobrazeno 1 - 10
of 429
pro vyhledávání: '"Victoria, Head"'
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
Supplementary Data from Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d58af020ff3289026b12e3df1b9a0f4
https://doi.org/10.1158/2159-8290.22541471.v1
https://doi.org/10.1158/2159-8290.22541471.v1
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
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
Autor:
Thomas, Ullrich, Luca, Arista, Sven, Weiler, Sylvie, Teixeira-Fouchard, Valérie, Broennimann, Nikolaus, Stiefl, Victoria, Head, Ina, Kramer, Sabine, Guth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 64:128667
Inhibition of mutant activin A type-1 receptor ACVR1 (ALK2) signaling by small-molecule drugs is a promising therapeutic approach to treat fibrodysplasia ossificans progressiva (FOP), an ultra-rare disease leading to progressive soft tissue heterotop
Autor:
Mark Freeman, Victoria Head, Binesh Shrestha, Michael Faller, Elizabeth Hardaker, Mark R Dowling, Rene Hemmig, Lucy Elphick, Johan C. Hill, Darren Le Grand, David D. Pascoe, Florence Zink, Christopher Thomson, Andrew Lister, S. Rieffel, David Beattie, Oliver Ross Steward
Publikováno v:
Bioorganicmedicinal chemistry letters. 31
A series of inhibitors of Autotaxin (ATX) have been developed from a high throughput screening hit, 1a, which shows an alternative binding mode to known catalytic site inhibitors. Selectivity over the hERG channel and microsomal clearance were depend
Autor:
Nicholas James Devereux, Anne-Marie D’Souza, Valerie Boissel, Vidal Agnes, Mark Nash, Ardem Patapoutian, Ryan West, J. Martin Verkuyl, Andrew M. Schumacher, Brian T. Masick, Victoria Head, H. Michael Petrassi, Rowan Stringer, Lisa Ann Rooney, Natalie Stoakley, Moh Panesar, David C. Tully, Jianmin Lao, Matt Petrus
Publikováno v:
Journal of medicinal chemistry. 57(12)
A high throughput screening campaign identified 5-(2-chlorophenyl)indazole compound 4 as an antagonist of the transient receptor potential A1 (TRPA1) ion channel with IC50 = 1.23 μM. Hit to lead medicinal chemistry optimization established the SAR a
Autor:
Malinen, KelleyAnne1 kelleyanne.malinen@msvu.ca, Matta, Chérif F.2 cherif.matta@msvu.ca
Publikováno v:
Foundations of Chemistry. Oct2018, Vol. 20 Issue 3, p265-268. 4p.
Publikováno v:
Gastroenterology. 134:A-544
Autor:
CICHOWOLSKI, MARCELA1 mcicho@gl.fcen.uba.ar, VACCARI, N. EMILIO2 evaccari@unc.edu.ar, POHLE, ALEXANDER3 alexander.pohle@rub.de, MORÓN ALFONSO, DANIEL A.1 paleokarzis@gmail.com, VAUCHER, ROMAIN4 romain.vaucher88@gmail.com, WAISFELD, BEATRIZ G.2 bwaisfeld@unc.edu.ar
Publikováno v:
Palaeontologia Polonica. 2023, Vol. 68 Issue 4, p583-601. 19p.