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RAF inhibitors

Thursday 4 March 2010

Tumours with mutant BRAF are dependent on the RAF-MEK-ERK signalling pathway for their growth.

ATP-competitive RAF inhibitors inhibit ERK signalling in cells with mutant BRAF, but unexpectedly enhance signalling in cells with wild-type BRAF.

RAF inhibitors do not inhibit ERK signalling in cells that coexpress BRAF-V600E and mutant RAS. (20179705)

Members

- vemurafenib
- dabrafenib
- LGX818
- TAK-632
- MLN2480
- PLX-4720

See also

- RAS-ERK pathway inhibitors

References

- http://www.nature.com/nrd/journal/v13/n12/fig_tab/nrd4281_T1.html

- RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N. Nature. 2010 Feb 23. PMID: 20179705