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Article ; Online: JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS

Lorthiois, Edwige / Gerspacher, Marc / Beyer, Kim S / Vaupel, Andrea / Leblanc, Catherine / Stringer, Rowan / Weiss, Andreas / Wilcken, Rainer / Guthy, Daniel A / Lingel, Andreas / Bomio-Confaglia, Claudio / Machauer, Rainer / Rigollier, Pascal / Ottl, Johannes / Arz, Dorothee / Bernet, Pascal / Desjonqueres, Gaëlle / Dussauge, Solene / Kazic-Legueux, Malika /
Lozac'h, Marie-Anne / Mura, Christophe / Sorge, Mickaël / Todorov, Milen / Warin, Nicolas / Zink, Florence / Voshol, Hans / Zecri, Frederic J / Sedrani, Richard C / Ostermann, Nils / Brachmann, Saskia M / Cotesta, Simona

Journal of medicinal chemistry

2022  Volume 65, Issue 24, Page(s) 16173–16203

Abstract: Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent ... ...

Abstract Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRAS
MeSH term(s) Animals ; Humans ; Mice ; Disease Models, Animal ; Drug Design ; Mutation ; Neoplasms/drug therapy ; Neoplasms/genetics ; Proto-Oncogene Proteins p21(ras) ; Pyrazoles/pharmacology ; Pyrazoles/therapeutic use
Chemical Substances KRAS protein, human ; Proto-Oncogene Proteins p21(ras) (EC 3.6.5.2) ; Pyrazoles ; JDQ443
Language English
Publishing date 2022-11-18
Publishing country United States
Document type Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID 218133-2
ISSN 1520-4804 ; 0022-2623
ISSN (online) 1520-4804
ISSN 0022-2623
DOI 10.1021/acs.jmedchem.2c01438
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Zs.B 151: Show issues Location:
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Database MEDical Literature Analysis and Retrieval System OnLINE

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