P63086

Background

Protein Name
Mitogen-activated protein kinase 1
Gene Name
Mapk1
Organism
Rattus norvegicus

Annotations

Function
Acts as a transcriptional repressor. Binds to a [GC]AAA[GC] consensus sequence. Repress the expression of interferon gamma-induced genes. Seems to bind to the promoter of CCL5, DMP1, IFIH1, IFITM1, IRF7, IRF9, LAMP3, OAS1, OAS2, OAS3 and STAT1. Transcriptional activity is independent of kinase activity (By similarity). 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 plays also 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 a variety of other signaling-related molecules (like ARHGEF2, DCC, FRS2 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 respons to EGF stimulation. May play a role in the spindle assembly checkpoint. Phosphorylates PML and promotes its interaction with PIN1, leading to PML degradation (By similarity).

Mapping Statistics

Site
Maximum Consensus Site Population
Minimum Consensus Site Population
Median Consensus Site Population
EDI 29 2 11.0
MT3 28 2 14.0
PIF 21 3 13.0
ATP 13 1 6.0
DEF 11 2 10.0
DRS 9 2 3.0
AAS 14 4 9.0
DFG 11 2 7.5
LBP 24 1 5.5
PDIG 12 2 3.0

Mapping Results

PDB ID
Maximum Consensus Site Population
EDI site
MT3 site
PIF site
ATP site
DEF site
DRS site
AAS site
MPP site
DFG site
LBP site
CMP site
PDIG site
PMP site
Total Druggable Structures per Site 16 12 4 0 0 0 0 0 0 5 0 0 0
1ERK 15 14 0 2 0 0 0 0 0 22 0 0 0
1GOL 13 0 0 0 0 0 0 0 0 15 0 0 0
2ERK 14 20 0 0 0 0 0 0 0 2 0 0 0
2FYS 26 14 0 6 0 9 0 0 0 9 0 0 0
2GPH 13 0 0 13 10 0 0 0 0 7 0 0 0
2Z7L 16 28 0 2 0 0 0 0 0 15 0 2 0
3C9W 8 17 0 7 0 0 0 0 2 15 0 0 0
3ERK 0 0 0 0 0 6 0 0 0 24 0 3 0
3O71 16 18 0 2 0 3 0 0 0 9 0 0 0
3QYW 15 0 0 0 0 2 0 0 11 0 0 0 0
3QYZ 11 16 0 0 0 3 0 0 0 16 0 0 0
3R63 29 0 0 0 0 3 0 0 11 14 0 0 0
3ZU7 18 0 12 8 0 0 0 0 0 8 0 0 0
3ZUV 13 13 0 6 0 0 0 0 0 0 0 0 0
4ERK 9 9 0 4 0 0 0 0 0 17 0 3 0
4GSB 21 18 0 7 0 0 0 0 0 13 0 0 0
4GT3 18 23 0 2 0 0 0 0 0 19 0 0 0
4GVA 14 14 0 0 0 3 0 0 0 3 0 0 0
4I5H 10 0 0 3 11 0 0 0 6 0 0 12 0
4N4S 12 21 0 0 0 4 0 0 0 0 0 0 0
4QYY 16 19 0 6 0 0 0 0 0 2 0 0 0
4S2Z 16 0 0 0 0 0 0 0 0 7 0 0 0
4S30 16 0 0 0 0 0 0 0 0 8 0 0 0
4S31 22 0 0 6 0 3 0 0 0 6 0 3 0
4S32 17 9 14 0 0 0 0 0 0 2 0 3 0
4S33 19 13 0 0 0 4 0 0 0 7 0 2 0
4S34 14 5 0 0 0 3 0 0 9 11 0 0 0
4XNE 15 0 0 0 0 0 0 0 0 3 0 0 0
4XOY 13 0 21 0 0 0 14 0 4 0 0 0 0
4XOZ 14 0 20 1 0 0 0 0 0 5 0 0 0
4XP0 15 0 0 7 0 6 0 0 2 0 0 0 0
4XP2 16 0 0 6 0 4 0 0 10 0 0 0 0
4XP3 12 0 15 0 0 0 0 0 0 3 0 0 0
4XRJ 15 0 0 0 0 3 0 0 0 4 0 0 0
4XRL 15 16 0 4 0 3 0 0 0 2 0 0 0
5HD4 16 20 17 11 0 0 0 0 0 0 0 0 0
5HD7 16 16 14 11 0 2 0 0 0 0 0 0 0
5KE0 14 2 17 10 0 2 0 0 0 5 0 0 0
AFP63086 0 0 0 0 0 0 0 0 0 0 0 0 0