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Association details:
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Title:

Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120

Excerpt:
We have identified previously undiscovered BRAF in-frame deletions near the αC-helix region of the kinase domain in pancreatic, lung, ovarian, and thyroid cancers....Expression of L485-P490-deleted BRAF is able to transform NIH/3T3 cells in a BRAF dimer-dependent manner….in the H2405 xenograft model, treatment of LY3009120 at 15 or 30 mg/kg achieved almost complete tumor growth regression, whereas vemurafenib treatment at 20 mg/kg had no antitumor growth activity...Xenograft tumors with a BRAF deletion are sensitive to RAF dimer inhibitor LY3009120 and resistant to the BRAF monomer inhibitor vemurafenib...
DOI:
10.1158/2159-8290.CD-15-089