Mitogen-activated protein kinase kinase
| Mitogen-activated protein kinase kinase | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Identifiers | |||||||||
| EC no. | 2.7.12.2 | ||||||||
| Databases | |||||||||
| BRENDA | enzyme data | ||||||||
| ExPASy | NiceZyme view | ||||||||
| KEGG | enzyme entry | ||||||||
| MetaCyc | metabolic pathway | ||||||||
| Rhea | reactions | ||||||||
| PDB structures | RCSB PDB PDBe PDBsum | ||||||||
| |||||||||
Mitogen-activated protein kinase kinase (also known as MAP2K, MEK, MAPKK) is a dual-specificity kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK).
MAP2K is classified as EC 2.7.12.2.
There are seven genes:
- MAP2K1 (a.k.a. MEK1)
- MAP2K2 (a.k.a. MEK2)
- MAP2K3 (a.k.a. MKK3)
- MAP2K4 (a.k.a. MKK4)
- MAP2K5 (a.k.a. MKK5)
- MAP2K6 (a.k.a. MKK6)
- MAP2K7 (a.k.a. MKK7)
The activators of p38 (MKK3 and MKK6), JNK (MKK4 and MKK7), and ERK (MEK1 and MEK2) define independent MAP kinase signal transduction pathways.[1] The acronym MEK derives from MAPK/ERK Kinase.[2]
Role in melanoma
[edit]MEK is a member of the MAPK signaling cascade that is activated in melanoma.[3] When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced.
As a drug target
[edit]A number of MEK inhibitors (particularly dual MEK1/MEK2 inhibitors) have been developed to treat various types of cancers.[4][5]
See also
[edit]References
[edit]- ↑ Dérijard B, Raingeaud J, Barrett T, Wu IH, Han J, Ulevitch RJ, et al. (February 1995). "Independent human MAP-kinase signal transduction pathways defined by MEK and MKK isoforms". Science. 267 (5198). New York, N.Y.: 682–685. Bibcode:1995Sci...267..682D. doi:10.1126/science.7839144. PMID 7839144. S2CID 9153074.
- ↑ Dwivedi G, Kemp ML (February 2012). "Systemic redox regulation of cellular information processing". Antioxidants & Redox Signaling. 16 (4): 374–380. doi:10.1089/ars.2011.4034. PMC 3279717. PMID 21939387.
- ↑ Falchook GS, Lewis KD, Infante JR, Gordon MS, Vogelzang NJ, DeMarini DJ, et al. (August 2012). "Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial". The Lancet. Oncology. 13 (8): 782–789. doi:10.1016/S1470-2045(12)70269-3. PMC 4109286. PMID 22805292.
- ↑ Caunt CJ, Sale MJ, Smith PD, Cook SJ (October 2015). "MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road". Nature Reviews. Cancer. 15 (10): 577–592. doi:10.1038/nrc4000. PMID 26399658.
- ↑ Suryavanshi A, Vandana, Shukla YK, Kumar V, Gupta P, Asati V, et al. (October 2024). "MEK inhibitors in oncology: a patent review and update (2016 - present)". Expert Opinion on Therapeutic Patents. 34 (10): 963–1007. doi:10.1080/13543776.2024.2403634. PMID 39275922.
External links
[edit]- Mitogen-Activated+Protein+Kinase+Kinases at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
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