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PP2 is a substance that has frequently been used in cancer research as a "selective" inhibitor for Src-family kinases. It strongly inhibits the kinases Lck ( IC 50 =4 nM ), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 μM) and JAK2 (50 μM).
Protein phosphatase 2 (PP2), also known as PP2A, is an enzyme that in humans is encoded by the PPP2CA gene. [ 2 ] [ 3 ] The PP2A heterotrimeric protein phosphatase is ubiquitously expressed, accounting for a large fraction of phosphatase activity in eukaryotic cells. [ 4 ]
The BRIM3 trial reported good updated results in 2012. [20] Further trials are planned including a trial of vemurafenib co-administered with GDC-0973 (cobimetinib), a MEK-inhibitor. [19] After good results in 2014, the combination was submitted to the European Medical Agency and the US Food and Drug Administration for marketing approval. [21]
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