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Assays & screens

Screening platform for detecting RAF dimerization in cells

A high throughput screening platform for RAF dimerization could help identify bona fide inhibitors of RAF signaling. ATP-competitive inhibitors of RAF kinases can paradoxically stimulate RAF signaling and tumor cell growth by inducing Ras-dependent RAF dimerization. The current screening approach uses membrane tethered RAF kinase domains and quantitatively detects RAF dimerization in cells. A high throughput screen using the platform identified activators and inhibitors of RAF dimerization. Researchers did not disclose next steps, which could include using the screen to identify kinase inhibitors that induce RAF dimerization and evaluating compounds that inhibit RAF dimerization in cancer models.

SciBX 6(23); doi:10.1038/scibx.2013.584
Published online June 13, 2013

Patented; licensing status undisclosed

Lavoie, H. et al. Nat. Chem. Biol.; published online May 19, 2013;
doi:10.1038/nchembio.1257
Contact: Marc Therrien, University of Montreal, Montreal, Quebec, Canada
e-mail:
marc.therrien@umontreal.ca

Contact: Frank Sicheri, Mount Sinai Hospital, Toronto, Ontario, Canada
e-mail:
sicheri@lunenfeld.ca