Exploiting allosteric properties of RAF and MEK inhibitors to target therapy-resistant tumors driven by oncogenic BRAF signaling

Current clinical RAF inhibitors (RAFi) inhibit monomeric BRAF (mBRAF), but are less potent against dimeric BRAF (dBRAF). RAFi equipotent for mBRAF and dBRAF have been developed, but are predicted to have lower therapeutic index. Here we identify a third class of RAFi that selectively inhibits dBRAF...

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Vydáno v:Cancer Discov
Hlavní autoři: Adamopoulos, Christos, Ahmed, Tamer A., Tucker, Maxwell R., Ung, Peter M.U., Xiao, Min, Karoulia, Zoi, Amabile, Angelo, Wu, Xuewei, Aaronson, Stuart A., Ang, Celina, Rebecca, Vito W., Brown, Brian D., Schlessinger, Avner, Herlyn, Meenhard, Wang, Qi, Shaw, David E., Poulikakos, Poulikos I.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2021
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC8295204/
https://ncbi.nlm.nih.gov/pubmed/33568355
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1158/2159-8290.CD-20-1351
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