The KRAS gene is an oncogene that encodes a GTPase transductor protein, K-Ras. The mutant KRAS regulates Myc, a transcription factor in MAPK/ERK signaling pathway, via ERK1/2-dependent and independent mechanisms in pancreatic ductal adenocarcinoma. MEK5 is a key component in MAPK pathway that phosphorylates and activates non-classical MAPK ERK5. GW284543, also known as UNC10225170, is a 4-anilinoquin(az)oline chemotype that selectively inhibits MEK5. Treatment of MIA PaCa-2 cells with GW284543 (10 and 20 μM) for 6 h decreased the expression of endogenous Myc protein in a concentration-dependent manner. The GW284543 treatment (10 and 20 μM) also dose-dependently inhibited MEK5 in MIA PaCa-2 cells, as indicated by the reduction in phosphorylated ERK5[1].
搜索
