Target name

P11309: Serine/threonine-protein kinase pim-1


  Protein function

Proto-oncogene with serine/threonine kinase activity involved in cell survival and cell proliferation and thus providing a selective advantage in tumorigenesis. Exerts its oncogenic activity through: the regulation of MYC transcriptional activity, the regulation of cell cycle progression and by phosphorylation and inhibition of proapoptotic proteins (BAD, MAP3K5, FOXO3). Phosphorylation of MYC leads to an increase of MYC protein stability and thereby an increase of transcriptional activity. The stabilization of MYC exerted by PIM1 might explain partly the strong synergism between these two oncogenes in tumorigenesis. Mediates survival signaling through phosphorylation of BAD, which induces release of the anti-apoptotic protein Bcl-X(L)/BCL2L1. Phosphorylation of MAP3K5, an other proapoptotic protein, by PIM1, significantly decreases MAP3K5 kinase activity and inhibits MAP3K5-mediated phosphorylation of JNK and JNK/p38MAPK subsequently reducing caspase-3 activation and cell apoptosis. Stimulates cell cycle progression at the G1-S and G2-M transitions by phosphorylation of CDC25A and CDC25C. Phosphorylation of CDKN1A, a regulator of cell cycle progression at G1, results in the relocation of CDKN1A to the cytoplasm and enhanced CDKN1A protein stability. Promote cell cycle progression and tumorigenesis by down-regulating expression of a regulator of cell cycle progression, CDKN1B, at both transcriptional and post-translational levels. Phosphorylation of CDKN1B,induces 14-3-3-proteins binding, nuclear export and proteasome-dependent degradation. May affect the structure or silencing of chromatin by phosphorylating HP1 gamma/CBX3. Acts also as a regulator of homing and migration of bone marrow cells involving functional interaction with the CXCL12-CXCR4 signaling axis.

  Database links

Uniprot primary ID P11309
PDB ID 3MA3 1YXV 1YXT 1YXU 2XJ2 3F2A 4RC4 4RC3 4RC2 1YXX 2BIK 4ALV 3DCV 2BIL 4N6Y 4N6Z 1YXS 3UIX 3JYA 4LMU 3UMX 3UMW 4WT6 3A99 3WE8 3CY3 3CY2 4DTK 4AS0 4JX3 3VBV 2BZJ 2BZK 2BZH 4IAA 4ALU 4ALW 4XHK 4LM5 4WRS 2XJ0 2XJ1 3BGP 3BGQ 4MBL 3BGZ 4MBI 2C3I 4JX7 1YI4 3T9I
DrugBank ID DB00131
BioGrid ID 111310
GuidetoPHARMACOLOGY ID 2158
PharmGKB ID PA33318
KEGG ID hsa:5292
DIP ID
STRING ID 9606.ENSP00000362608
IntAct ID P11309
DMDM 83305339
BRENDA
Reactome
SignaLink P11309
BioCyc
Entrez Gene (Gene ID) 5292
BindingDB P11309

  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 0.889 0.003 0.883 0.003 0.886 0.005 0.888 0.004 0.944 0.005 0.771 0.003 Download
Estate fingerprints 0.750 0.000 0.758 0.000 0.754 0.005 0.751 0.003 0.830 0.000 0.509 0.003 Download
MACCS fingerprints 0.862 0.004 0.738 0.000 0.800 0.000 0.810 0.000 0.870 0.000 0.600 0.000 Download
Daylight fingerprints 0.790 0.000 0.868 0.005 0.829 0.003 0.820 0.000 0.890 0.000 0.657 0.005 Download
ECFP2 fingerprints 0.949 0.003 0.881 0.004 0.915 0.005 0.920 0.000 0.980 0.000 0.831 0.003 Download
ECFP4 fingerprints 0.931 0.003 0.963 0.000 0.947 0.005 0.945 0.005 0.980 0.000 0.891 0.003 Download
ECFP6 fingerprints 0.891 0.003 0.989 0.005 0.940 0.000 0.936 0.005 0.980 0.000 0.880 0.000 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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