Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance

Covalent inhibition is a reemerging paradigm in kinase drug design, but the roles of inhibitor binding affinity and chemical reactivity in overall potency are not well-understood. To characterize the underlying molecular processes at a microscopic level and determine the appropriate kinetic constant...

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Detalhes bibliográficos
Main Authors: Schwartz, Phillip A., Kuzmic, Petr, Solowiej, James, Bergqvist, Simon, Bolanos, Ben, Almaden, Chau, Nagata, Asako, Ryan, Kevin, Feng, Junli, Dalvie, Deepak, Kath, John C., Xu, Meirong, Wani, Revati, Murray, Brion William
Formato: Artigo
Idioma:Inglês
Publicado em: National Academy of Sciences 2014
Assuntos:
Biological Sciences
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3890870/
https://ncbi.nlm.nih.gov/pubmed/24347635
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1313733111
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