Article
Cell lines expressing recombinant transmembrane domain-activated receptor kinases as tools for drug discovery.
Journal of biomolecular screening - 1 Dec 2014
Weber Holger, Müller Daniel, Müller Melanie, Ortiz Alexandra, Birkle Marianne, Umber Sarah, Ketterer Constance, Siedentopf Oliver, Feger Daniel, Totzke Frank, Kubbutat Michael, Schaechtele Christoph, Ballmer-Hofer Kurt, Ehlert Jan Erik, Graeser Ralph
Abstract excerpt
Many receptor tyrosine kinases (RTKs) represent bona fide drug targets in oncology. Effective compounds are available, but treatment invariably leads to resistance, often due to RTK mutations. The discovery of second-generation inhibitors requires cellular models of resistant RTKs. An approach using artificial transmembrane domains (TMDs) to activate RTKs was explored for the rapid generation of simple,...
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