Target name

Q02750: Dual specificity mitogen-activated protein kinase kinase 1


  Protein function

Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones to their cell-surface receptors activates RAS and this initiates RAF1 activation. RAF1 then further activates the dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2. Both MAP2K1/MEK1 and MAP2K2/MEK2 function specifically in the MAPK/ERK cascade, and catalyze the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2, leading to their activation and further transduction of the signal within the MAPK/ERK cascade. Depending on the cellular context, this pathway mediates diverse biological functions such as cell growth, adhesion, survival and differentiation, predominantly through the regulation of transcription, metabolism and cytoskeletal rearrangements. One target of the MAPK/ERK cascade is peroxisome proliferator-activated receptor gamma (PPARG), a nuclear receptor that promotes differentiation and apoptosis. MAP2K1/MEK1 has been shown to export PPARG from the nucleus. The MAPK/ERK cascade is also involved in the regulation of 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.

  Database links

Uniprot primary ID Q02750
PDB ID 4ARK 3EQI 3EQH 3EQC 3EQB 3EQG 3EQF 3E8N 3EQD 3ZLY 3ZLX 3ZLS 2P55 4U81 4U80 3SLS 1S9J 3ZLW 3WIG 3MBL 3DV3 4AN9 3ZM4 3VVH 3OS3 4ANB 3PP1 3DY7 4U7Z 3V01 3W8Q 3V04 4AN3 4LMN 4MNE 3ORN 4AN2
DrugBank ID DB06616 DB08911
BioGrid ID 111590
GuidetoPHARMACOLOGY ID 2062
PharmGKB ID PA30584
KEGG ID hsa:5604
DIP ID DIP-201N
STRING ID 9606.ENSP00000302486
IntAct ID Q02750
DMDM 400274
BRENDA 2.7.12.2
Reactome R-HSA-445144 R-HSA-450294 R-HSA-446652 R-HSA-5654738 R-HSA-5654736 R-HSA-5674499 R-HSA-5674135 R-HSA-110056 R-HSA-5210891 R-HSA-5654743 R-HSA-5673000 R-HSA-5654741
SignaLink Q02750
BioCyc
Entrez Gene (Gene ID) 5604
BindingDB Q02750

  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 0.824 0.005 0.974 0.000 0.899 0.003 0.890 0.000 0.950 0.000 0.803 0.005 Download
Estate fingerprints 0.869 0.003 0.871 0.005 0.870 0.000 0.870 0.000 0.920 0.000 0.734 0.005 Download
MACCS fingerprints 0.857 0.007 0.897 0.005 0.877 0.005 0.877 0.005 0.933 0.005 0.757 0.008 Download
Daylight fingerprints 0.750 0.000 0.970 0.003 0.860 0.000 0.843 0.005 0.918 0.004 0.744 0.005 Download
ECFP2 fingerprints 0.871 0.003 0.967 0.004 0.919 0.003 0.911 0.003 0.960 0.000 0.836 0.005 Download
ECFP4 fingerprints 0.873 0.005 0.987 0.000 0.930 0.000 0.927 0.005 0.961 0.003 0.867 0.005 Download
ECFP6 fingerprints 0.853 0.007 0.991 0.000 0.922 0.004 0.919 0.003 0.960 0.000 0.855 0.005 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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