Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions

Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs), theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or exploited this potential advantage of event-driven pharmacology. Degraders of oncogenic EML4-ALK fusions were developed by conju...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 66; H. 8; S. 5524
Hauptverfasser:	Gao, Yang, Jiang, Baishan, Kim, Hellen, Berberich, Matthew J, Che, Jianwei, Donovan, Katherine A, Hatcher, John M, Huerta, Fidel, Kwiatkowski, Nicholas P, Liu, Yingpeng, Liuni, Peter P, Metivier, Rebecca J, Murali, Vineeth K, Nowak, Radosław P, Zhang, Tinghu, Fischer, Eric S, Gray, Nathanael S, Jones, Lyn H
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 27.04.2023
Schlagworte:	Anaplastic Lymphoma Kinase Antineoplastic Agents - pharmacology Drug Resistance, Neoplasm Humans Lung Neoplasms - drug therapy Mutation Oncogene Proteins, Fusion - genetics Protein Kinase Inhibitors - pharmacology Receptor Protein-Tyrosine Kinases
ISSN:	1520-4804, 1520-4804
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