Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRAS(G12C)

Covalent inhibitors of KRAS(G12C) have shown antitumor activity against advanced/metastatic KRAS(G12C)-mutated cancers, though resistance emerges and additional strategies are needed to improve outcomes. JDQ443 is a structurally unique covalent inhibitor of GDP-bound KRAS(G12C) that forms novel inte...

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Detalles Bibliográficos
Autores principales: Weiss, Andreas, Lorthiois, Edwige, Barys, Louise, Beyer, Kim S., Bomio-Confaglia, Claudio, Burks, Heather, Chen, Xueying, Cui, Xiaoming, de Kanter, Ruben, Dharmarajan, Lekshmi, Fedele, Carmine, Gerspacher, Marc, Guthy, Daniel Alexander, Head, Victoria, Jaeger, Ashley, Núñez, Eloísa Jiménez, Kearns, Jeffrey D., Leblanc, Catherine, Maira, Sauveur-Michel, Murphy, Jason, Oakman, Helen, Ostermann, Nils, Ottl, Johannes, Rigollier, Pascal, Roman, Danielle, Schnell, Christian, Sedrani, Richard, Shimizu, Toshio, Stringer, Rowan, Vaupel, Andrea, Voshol, Hans, Wessels, Peter, Widmer, Toni, Wilcken, Rainer, Xu, Kun, Zecri, Frederic, Farago, Anna F., Cotesta, Simona, Brachmann, Saskia M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Association for Cancer Research 2022
Materias:
Research Articles
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9394399/
https://www.ncbi.nlm.nih.gov/pubmed/35404998
http://dx.doi.org/10.1158/2159-8290.CD-22-0158

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