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文献和实验is a highly selective inhibitor of MEK1 and MEK2 with IC50 values of 4 ?M and 50 ?M respectively. PD98059 does not inhibit activation of other highly related dual-specificity protein kinases or the activity of over 18 other Ser/Thr protein kinases
Mutational and Functional Analysis in Human Ras/MAP Kinase Genetic Syndromes
) syndrome, is caused by germline mutations in BRAF , MAP2K1 (MEK1 ) and MAP2K2 (MEK2 ), and possibly KRAS genes. Here, we describe the laboratory protocols and methods that we used to identify mutations in BRAF and MEK1/2 genes as causative for CFC syndrome
蛋白Ras的GDP解离而结合GTP,从而激活Ras;激活的Ras进一步与丝/苏氨酸蛋白激酶Raf-1的氨基端结合,通过未知机制激活Raf-1;Raf-1可磷酸化MEK1/MEK2(MAP kinase/ERK kinase)上的二个调节性丝氨酸,从而激活MEKs;MEKs为双特异性激酶,可以使丝/苏氨酸和酪氨酸发生磷酸化,最终高度选择性地激活ERK1和ERK2(即p44MAPK和p42MAPK)。ERKs为脯氨酸导向的丝/苏氨酸激酶,可以磷酸化与脯氨酸相邻的丝/苏氨酸。在丝裂原刺激后,ERKs接受上游
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