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
PharmGKB ID PA30584
KEGG ID hsa:5604
Entrez Gene (Gene ID) 5604
STRING 9606ENSP00000302486
IntAct Q02750
DMDM 400274
BREDNA 27122
Rectome 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
BindingDB Q02750

  Model Performance Metrics

Fingerprint type F1_CV AUC_CV Accuracy_CV Sensitivity_CV Specificity_CV F1_test AUC_test Accuracy_test Sensitivity_test Specificity_test Download model
FP2 fingerprints 0.882 0.920 0.890 0.817 0.964 0.918 0.948 0.925 0.876 0.970 Download
MACCS fingerprints 0.827 0.920 0.835 0.783 0.888 0.873 0.953 0.877 0.884 0.871 Download
Daylight fingerprints 0.853 0.881 0.861 0.799 0.924 0.868 0.900 0.881 0.818 0.939 Download
ECFP2 fingerprints 0.896 0.945 0.899 0.868 0.930 0.936 0.970 0.941 0.901 0.977 Download
ECFP4 fingerprints 0.901 0.937 0.906 0.850 0.962 0.931 0.963 0.937 0.893 0.977 Download
ECFP6 fingerprints 0.898 0.929 0.904 0.844 0.964 0.931 0.949 0.937 0.893 0.977 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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