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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Hlavní autoři: 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
Médium: Artigo
Jazyk:Inglês
Vydáno: National Academy of Sciences 2014
Témata:
Biological Sciences
On-line přístup: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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