Target name

P28482: Mitogen-activated protein kinase 1


  Protein 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 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.

  Database links

Uniprot primary ID P28482
PDB ID 2OJG 1TVO 4N0S 5BUE 4QP8 3W55 5BUI 4FUY 4FUX 2OJI 4QP1 3I5Z 4QP3 4QP2 4QP4 4QP7 4QP6 4QP9 3D44 3D42 3I60 4IZ7 4IZA 3TEI 4O6E 5BUJ 4FV8 4FV9 4FV4 4FV5 4FV6 4FV7 4FV0 4FV1 4FV2 4FV3 5BVF 5BVE 5BVD 1PME 2OJJ 4ZZM 4ZZN 4ZZO 4QTE 4QTA 4IZ5 1WZY 4QPA 4XJ0 4FMQ
DrugBank ID DB01169 DB01064
BioGrid ID 111580
GuidetoPHARMACOLOGY ID 1495
PharmGKB ID PA30616
KEGG ID hsa:5594
DIP ID DIP-519N
STRING ID 9606.ENSP00000215832
IntAct ID P28482
DMDM 119554
BRENDA 2.7.11.24
Reactome R-HSA-2559585 R-HSA-445144 R-HSA-2871796 R-HSA-111995 R-HSA-2559580 R-HSA-198753 R-HSA-56547 R-HSA-881907 R-HSA-5654733 R-HSA-5674499 R-HSA-437239 R-HSA-5654727 R-HSA-444257 R-HSA-5654726 R-HSA-982772 R-HSA-5673001 R-HSA-442742 R-HSA-2559582 R-HSA-5663213
SignaLink P28482
BioCyc
Entrez Gene (Gene ID) 5594
BindingDB P28482

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.790 0.000 0.990 0.005 0.890 0.000 0.880 0.000 0.940 0.000 0.804 0.005 Download
Estate fingerprints 0.837 0.007 0.937 0.003 0.887 0.005 0.882 0.004 0.929 0.003 0.778 0.006 Download
MACCS fingerprints 0.825 0.005 0.949 0.004 0.887 0.005 0.880 0.000 0.940 0.000 0.782 0.004 Download
Daylight fingerprints 0.780 0.000 1.000 0.000 0.890 0.000 0.880 0.000 0.940 0.000 0.800 0.000 Download
ECFP2 fingerprints 0.800 0.000 1.000 0.000 0.900 0.000 0.889 0.003 0.960 0.000 0.812 0.004 Download
ECFP4 fingerprints 0.790 0.000 0.990 0.000 0.890 0.000 0.880 0.000 0.964 0.005 0.810 0.000 Download
ECFP6 fingerprints 0.790 0.000 0.990 0.000 0.890 0.000 0.880 0.000 0.960 0.000 0.800 0.000 Download

  Download datasets

Positive dataset Negative dataset


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School of Pharmaceutical Sciences, Central South University. All rights reserved.

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