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Description

Dual specificity mitogen-activated protein kinase kinase 1 (EC 2.7.12.2, UniProt Q02750, also known as ERK activator kinase 1, MAP kinase kinase 1, MAPK/ERK kinase 1, MAPKK 1, MEK 1, MKK1) is encoded by the MAP2K1 (also known as CFC3, MAPKK1, MEK1, MKK1, PRKMK1) gene (Gene ID 5604) in human. MEK1 and the related MEK2 are dual specificity kinases of the MAP2K/STE7 kinase family. MEK1 and MEK2 share a high degree of sequence homology and perform similar functions. Upon activation by RAF, MEK1/2 catalyze the dual phosphorylation of threonine and tyrosine residues on ERK (MAPK) within a specific Thr-Glu-Tyr sequence at codons 202 to 204. This locks the kinase domain of MAPK into a catalytically competent conformation, ultimately leading to nuclear signals that regulate cellular growth and proliferation. MEK1/2 mutations have been reported to be associated with cardiofaciocutaneous syndrome 3 (CFC3) and cancers, including lung cancer, colorectal cancer, and melanomas.