Function
Mitogen-activated protein kinase kinase (MAP2K) are serine/threonine kinases which regulate various cellular activities in response to extracellular stimuli by mitogens, heat shock and more. MAP2K is part of the MAPK cascade which consists also of MAPK and MAP3K which are activated by phosphorylation. MAP2K activates MAPK[1].
Relevance
MAP2K is activated in melanoma and its inhibitors are tested as therapeutical agents[2].
3D Structures of Mitogen-activated protein kinase kinase
Updated on 28-April-2016
References
- ↑ Weyman CM, Wolfman A. Mitogen-activated protein kinase kinase (MEK) activity is required for inhibition of skeletal muscle differentiation by insulin-like growth factor 1 or fibroblast growth factor 2. Endocrinology. 1998 Apr;139(4):1794-800. PMID:9528964 doi:http://dx.doi.org/10.1210/endo.139.4.5950
- ↑ Falchook GS, Lewis KD, Infante JR, Gordon MS, Vogelzang NJ, DeMarini DJ, Sun P, Moy C, Szabo SA, Roadcap LT, Peddareddigari VG, Lebowitz PF, Le NT, Burris HA 3rd, Messersmith WA, O'Dwyer PJ, Kim KB, Flaherty K, Bendell JC, Gonzalez R, Kurzrock R, Fecher LA. Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial. Lancet Oncol. 2012 Aug;13(8):782-9. doi: 10.1016/S1470-2045(12)70269-3. Epub 2012, Jul 16. PMID:22805292 doi:http://dx.doi.org/10.1016/S1470-2045(12)70269-3
