Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.

doi:10.1016/j.ccell.2015.08.002

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Article

Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.

Cancer cell - 14 Sept 2015

Peng Sheng-Bin, Henry James R, Kaufman Michael D, Lu Wei-Ping, Smith Bryan D, Vogeti Subha, Rutkoski Thomas J, Wise Scott, Chun Lawrence, Zhang Youyan, Van Horn Robert D, Yin Tinggui, Zhang Xiaoyi, Yadav Vipin, Chen Shih-Hsun, Gong Xueqian, Ma Xiwen, Webster Yue, Buchanan Sean, Mochalkin Igor, Huber Lysiane, Kays Lisa, Donoho Gregory P, Walgren Jennie, McCann Denis, Patel Phenil, Conti Ilaria, Plowman Gregory D, Starling James J, Flynn Daniel L

Abstract excerpt

LY3009120 is a pan-RAF and RAF dimer inhibitor that inhibits all RAF isoforms and occupies both protomers in RAF dimers. Biochemical and cellular analyses revealed that LY3009120 inhibits ARAF, BRAF, and CRAF isoforms with similar affinity, while vemurafenib or dabrafenib have little or modest CRAF activity compared to their BRAF activities. LY3009120 induces BRAF-CRAF dimerization but inhibits the...

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PMID: 26343583
DOI: 10.1016/j.ccell.2015.08.002

Genes

BRAF
ARAF
KRAS
NRAS

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