Mitogen-activated protein kinase 1
Also known as: ERK2, MAPK1, PRKM1, PRKM2
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Many of these substrates are localized in the nucleus, and seem to participate in the regulation of transcription upon stimulation. However, other substrates are found in the cytosol as well as in other cellular organelles, and those are responsible for processes such as translation, mitosis and apoptosis. Moreover, the MAPK/ERK cascade is also involved in the regulation of the endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC); as well as in the fragmentation of the Golgi apparatus during mitosis. The substrates include transcription factors (such as ATF2, BCL6, ELK1, ERF, FOS, HSF4 or SPZ1), cytoskeletal elements (such as CANX, CTTN, GJA1, MAP2, MAPT, PXN, SORBS3 or STMN1), regulators of apoptosis (such as BAD, BTG2, CASP9, DAPK1, IER3, MCL1 or PPARG), regulators of translation (such as EIF4EBP1 and FXR1) and a variety of other signaling-related molecules (like ARHGEF2, DCC, FRS2, GLI1 or GRB10). Protein kinases (such as RAF1, RPS6KA1/RSK1, RPS6KA3/RSK2, RPS6KA2/RSK3, RPS6KA6/RSK4, SYK, MKNK1/MNK1, MKNK2/MNK2, RPS6KA5/MSK1, RPS6KA4/MSK2, MAPKAPK3 or MAPKAPK5) and phosphatases (such as DUSP1, DUSP4, DUSP6 or DUSP16) are other substrates which enable the propagation the MAPK/ERK signal to additional cytosolic and nuclear targets, thereby extending the specificity of the cascade. Mediates phosphorylation of TPR in response to EGF stimulation. May play a role in the spindle assembly checkpoint. Phosphorylates PML and promotes its interaction with PIN1, leading to PML degradation. Phosphorylates CDK2AP2 (By similarity). Phosphorylates phosphoglycerate kinase PGK1 under hypoxic conditions to promote its targeting to the mitochondrion and suppress the formation of acetyl-coenzyme A from pyruvate. Phosphorylates GJA1 at 'Ser-279' and 'Ser-282' resulting in an increase in GJA1 ubiquitination and ultimately lysosomal degradation (By similarity). Acts as a positive regulator of smoothened signaling by mediating phosphorylation of GLI1 in response to smoothened activation, promoting its dissociation from SUFU inhibitor and translocation to the nucleus.
Classification
- Family (Pfam)
- PF00069 Pkinase
- InterPro
- Kinase-like_dom_sf, MAP_kinase_CS, MAPK, MAPK_ERK1/2, Prot_kinase_dom, Protein_kinase_ATP_BS, Ser/Thr_kinase_AS
- Functional cluster
- Serine/Threonine Protein Kinases
Experimental structures · PDB · 157
- 1PME X-ray 2.00A
- 1TVO X-ray 2.50A
- 1WZY X-ray 2.50A
- 2OJG X-ray 2.00A
- 2OJI X-ray 2.60A
- 2OJJ X-ray 2.40A
- 2Y9Q X-ray 1.55A
- 3D42 X-ray 2.46A
- 3D44 X-ray 1.90A
- 3I5Z X-ray 2.20A
- 3I60 X-ray 2.50A
- 3SA0 X-ray 1.59A
- … and 145 more
A predicted model is available from AlphaFold.
Gene Ontology · 64
- GO:0035578 azurophil granule lumen
- GO:0005901 caveola
- GO:0005813 centrosome
- GO:0005737 cytoplasm
- GO:0005856 cytoskeleton
- GO:0005829 cytosol
- GO:0005769 early endosome
- GO:0005788 endoplasmic reticulum lumen
- GO:0005576 extracellular region
- GO:1904813 ficolin-1-rich granule lumen
- GO:0005925 focal adhesion
- GO:0005794 Golgi apparatus
- GO:0005770 late endosome
- GO:0005739 mitochondrion
- GO:0072686 mitotic spindle
- GO:0005654 nucleoplasm
- GO:0005634 nucleus
- GO:0005886 plasma membrane
- GO:0031143 pseudopodium
- GO:0045202 synapse
- GO:0005524 ATP binding
- GO:0003677 DNA binding
- GO:0042802 identical protein binding
- GO:0004707 MAP kinase activity
- GO:0019902 phosphatase binding
- GO:0001784 phosphotyrosine residue binding
- GO:0106310 protein serine kinase activity
- GO:0004674 protein serine/threonine kinase activity
- GO:0008353 RNA polymerase II CTD heptapeptide repeat kinase activity
- GO:0006915 apoptotic process
- GO:0072584 caveolin-mediated endocytosis
- GO:0007166 cell surface receptor signaling pathway
- GO:0034198 cellular response to amino acid starvation
- GO:0007268 chemical synaptic transmission
- GO:0070098 chemokine-mediated signaling pathway
- GO:0006935 chemotaxis
- GO:0006351 DNA-templated transcription
- GO:0007173 epidermal growth factor receptor signaling pathway
- GO:0038127 ERBB signaling pathway
- GO:0038133 ERBB2-ERBB3 signaling pathway
- GO:0070371 ERK1 and ERK2 cascade
- GO:0008286 insulin receptor signaling pathway
- GO:0048009 insulin-like growth factor receptor signaling pathway
- GO:0061514 interleukin-34-mediated signaling pathway
- GO:0035556 intracellular signal transduction
- GO:0007611 learning or memory
- GO:0000165 MAPK cascade
- GO:0042552 myelination
- GO:0045542 positive regulation of cholesterol biosynthetic process
- GO:0010759 positive regulation of macrophage chemotaxis
- GO:0120041 positive regulation of macrophage proliferation
- GO:0150078 positive regulation of neuroinflammatory response
- GO:0010800 positive regulation of peptidyl-threonine phosphorylation
- GO:0032206 positive regulation of telomere maintenance
- GO:0006468 protein phosphorylation
- GO:0051493 regulation of cytoskeleton organization
- GO:2000641 regulation of early endosome to late endosome transport
- GO:0090170 regulation of Golgi inheritance
- GO:0032872 regulation of stress-activated MAPK cascade
- GO:0070849 response to epidermal growth factor
- GO:0035094 response to nicotine
- GO:0014044 Schwann cell development
- GO:0007165 signal transduction
- GO:0051403 stress-activated MAPK cascade
Disease associations
- Noonan syndrome 13 MONDO:0033669
Drugs targeting this protein · 6
- RAVOXERTINIB inhibitor
- ULIXERTINIB inhibitor
- MK-8353 inhibitor
- ASN007 inhibitor
- KO-947 inhibitor
- TEMUTERKIB inhibitor
Neighborhood · nearest proteins
Related proteins · sequence + function similarity
- Mitogen-activated protein kinase 1 1.00
- Mitogen-activated protein kinase 1 1.00
- Mitogen-activated protein kinase 1 1.00
- Mitogen-activated protein kinase 1 0.99
- Mitogen-activated protein kinase ERK-A 0.96
- Mitogen-activated protein kinase Pmk1 0.96
- Mitogen-activated protein kinase mpkB 0.95
- Mitogen-activated protein kinase 0.95
- Mitogen-activated protein kinase 3 0.95
- Mitogen-activated protein kinase 3 0.95
- Mitogen-activated protein kinase PMK1 0.95
- Mitogen-activated protein kinase 3 0.95
Co-cited proteins · studied together in the literature
- Mitogen-activated protein kinase 3 28 shared papers
- ETS domain-containing transcription factor ERF 1 shared papers
- Dual specificity protein phosphatase 7 1 shared papers
- Dual specificity protein phosphatase 16 1 shared papers
- Serine/threonine/tyrosine-interacting protein 1 shared papers
- Vinexin 1 shared papers
- MAP kinase-activated protein kinase 3 1 shared papers
- Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 3 shared papers
- Dual specificity protein phosphatase 1 1 shared papers
- Dual specificity protein phosphatase 2 1 shared papers
- Mitogen-activated protein kinase 4 1 shared papers
- ETS domain-containing protein Elk-1 1 shared papers
Literature · 74 cited papers
- ERK2 MAP kinase regulates SUFU binding by multisite phosphorylation of GLI1. Life. Sci Alliance · 2022
- TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination. Nat. Cell Biol. · 2021
- Enhanced MAPK1 function causes a neurodevelopmental disorder within the RASopathy clinical spectrum. Am. J. Hum. Genet. · 2020
- The EGFR-ZNF263 signaling axis silences SIX3 in glioblastoma epigenetically. Oncogene · 2020
- Mitochondria-Translocated PGK1 Functions as a Protein Kinase to Coordinate Glycolysis and the TCA Cycle in Tumorigenesis. Mol. Cell · 2016
- An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. J. Proteomics · 2014
- Pseudophosphatase STYX modulates cell-fate decisions and cell migration by spatiotemporal regulation of ERK1/2. Proc. Natl. Acad. Sci. U.S.A. · 2013
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- N-terminal acetylome analyses and functional insights of the N-terminal acetyltransferase NatB. Proc. Natl. Acad. Sci. U.S.A. · 2012
- Comparative large-scale characterisation of plant vs. mammal proteins reveals similar and idiosyncratic N-alpha acetylation features. Mol. Cell. Proteomics · 2012
- Mitogen-activated protein kinase extracellular signal-regulated kinase 2 phosphorylates and promotes Pin1 protein-dependent promyelocytic leukemia protein turnover. J. Biol. Chem. · 2011
- The ERK cascade: distinct functions within various subcellular organelles. Genes Cancer · 2011
- … and 62 more in the literature graph