Insights into BRAF resistance in melanoma lead to potential new drug targets

Melanoma is a common form of skin cancer in which 60% of patients have the V600E mutation of the serine/threonine kinase B-RAF (BRAF)

Melanomas with a V600E BRAF mutation are dependent on mitogen-activated protein kinase (MAPK) and have been shown to respond to inhibition of the RAF and MEK signaling pathway.

PLX4032 (vemurafenib) is a B-RAF(V600E) inhibitor that has achieved some spectacular results.

However, resistance to BRAF inhibitors such as PLX4032 occurs, so understanding the mechanism of BRAF resistance is key to finding new druggable targets that may overcome this.

Sally Church has written one of her most insightful posts of 2011 on Pharma Strategy Blog that discusses recent research on BRAF resistance to melanoma.

In a post entitled, “COT drives resistance to PLX4032 through MAPK reactivation”, Sally discusses results published in a Nature Letter.

She also reviews the recent plenary talk by Keith Flaherty at the recent American Association for Cancer Research (AACR) annual meeting and provides insights on the next generation of BRAF inhibitors.

Sally concludes that it looks like “metastatic melanoma will be a hot topic at ASCO.” You can read more about new products in development for melanoma on Pharma Strategy Blog.

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