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Design and Synthesis of Type IV Inhibitors of BRAF Kinase that block dimerization and overcome paradoxical MEK/ERK activation

Despite the clinical success of BRAF inhibitors like vemurafenib in treating metastatic melanoma, resistance has emerged through “paradoxical MEK/ERK signaling” where transactivation of one protomer occurs as a result of drug inhibition of the other partner in the activated dimer. The importance of...

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Bibliografiska uppgifter
I publikationen:J Med Chem
Huvudupphovsmän: Beneker, Chad M., Rovoli, Magdalina, Kontopidis, George, Röring, Michael, Galda, Simone, Brown, Sandra, Brummer, Tilman, McInnes, Campbell
Materialtyp: Artigo
Språk:Inglês
Publicerad: 2019
Ämnen:
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC6750704/
https://ncbi.nlm.nih.gov/pubmed/30977659
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01288
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