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Conformationally constrained peptides target the allosteric kinase dimer interface and inhibit EGFR activation

Although EGFR is a highly sought-after drug target, inhibitor resistance remains a challenge. As an alternative strategy for kinase inhibition, we sought to explore whether allosteric activation mechanisms could effectively be disrupted. The kinase domain of EGFR forms an atypical asymmetric dimer v...

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Pubblicato in:Bioorg Med Chem
Autori principali: Fulton, Melody D., Hanold, Laura E., Ruan, Zheng, Patel, Sneha, Beedle, Aaron M., Kannan, Natarajan, Kennedy, Eileen J.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2017
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5837902/
https://ncbi.nlm.nih.gov/pubmed/28911855
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2017.08.051
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