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Association details:
| Biomarker: | MAP2K1 F129L |
|---|---|
| Cancer: | Melanoma |
| Drug: | Zelboraf (vemurafenib) (BRAF inhibitor, BRAF V600E inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors
Excerpt:
In addition, expression of MEK1F129L (allosteric binding site mutant with enhanced activity; refs. 17, 21) or MEK1DD (constitutively active mutant with aspartic acid replacement of activating loop serine residues; ref. 17) all mediated resistance to PLX4032 (Supplementary Fig. S8)
DOI:
10.1158/2159-8290.CD-13-0070
