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Association details:
| Biomarker: | PAK4 overexpression |
|---|---|
| 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:
To test whether ERK blockade was efficacious in the context of these clinically observed resistance mechanisms, stable cell lines expressing each of these variants were engineered in a BRAFV600E A375 background. As shown in Fig. 3D, overexpression of KRASG13D (positive control), BRAFV600E (to simulate amplification), or BRAFV600EΔ2-8 all conferred resistance to PLX4032, whereas overexpression of MEK1P124L (residue proximal to N-terminal negative inhibitory domain) conferred resistance to GSK1120212.
DOI:
10.1158/2159-8290.CD-13-0070
