We describe the synthesis and optimisation of a series of new inhibitors of BRAF, a kinase whose mutant form (V600E) is implicated in several types of cancer, with particularly high frequency in melanoma. We designed and synthesised type II inhibitors interacting with the inactive conformation of the V600EBRAF.
The discovery of novel, highly potent inhibitors of BRAF / Niculescu Duvaz, I.; Menard, D; Niculescu Duvaz, D.; Zambon, Alfonso; Davies, L; Preece, N.; Kirk, R.; Whittaker, S.; Marais, R.; Springer, C.. - In: EUROPEAN JOURNAL OF CANCER. - ISSN 0959-8049. - (2010), pp. 139-139. [10.1016/S1359-6349(10)72148-0]
The discovery of novel, highly potent inhibitors of BRAF
ZAMBON, Alfonso;
2010
Abstract
We describe the synthesis and optimisation of a series of new inhibitors of BRAF, a kinase whose mutant form (V600E) is implicated in several types of cancer, with particularly high frequency in melanoma. We designed and synthesised type II inhibitors interacting with the inactive conformation of the V600EBRAF.
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