Target name

P53350: Serine/threonine-protein kinase PLK1

  Protein function

Serine/threonine-protein kinase that performs several important functions throughout M phase of the cell cycle, including the regulation of centrosome maturation and spindle assembly, the removal of cohesins from chromosome arms, the inactivation of anaphase-promoting complex/cyclosome (APC/C) inhibitors, and the regulation of mitotic exit and cytokinesis. Polo-like kinase proteins acts by binding and phosphorylating proteins are that already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates BORA, BUB1B/BUBR1, CCNB1, CDC25C, CEP55, ECT2, ERCC6L, FBXO5/EMI1, FOXM1, KIF20A/MKLP2, CENPU, NEDD1, NINL, NPM1, NUDC, PKMYT1/MYT1, KIZ, PPP1R12A/MYPT1, PRC1, RACGAP1/CYK4, SGOL1, STAG2/SA2, TEX14, TOPORS, p73/TP73, TPT1 and WEE1. Plays a key role in centrosome functions and the assembly of bipolar spindles by phosphorylating KIZ, NEDD1 and NINL. NEDD1 phosphorylation promotes subsequent targeting of the gamma-tubulin ring complex (gTuRC) to the centrosome, an important step for spindle formation. Phosphorylation of NINL component of the centrosome leads to NINL dissociation from other centrosomal proteins. Involved in mitosis exit and cytokinesis by phosphorylating CEP55, ECT2, KIF20A/MKLP2, CENPU, PRC1 and RACGAP1. Recruited at the central spindle by phosphorylating and docking PRC1 and KIF20A/MKLP2; creates its own docking sites on PRC1 and KIF20A/MKLP2 by mediating phosphorylation of sites subsequently recognized by the POLO box domains. Phosphorylates RACGAP1, thereby creating a docking site for the Rho GTP exchange factor ECT2 that is essential for the cleavage furrow formation. Promotes the central spindle recruitment of ECT2. Plays a central role in G2/M transition of mitotic cell cycle by phosphorylating CCNB1, CDC25C, FOXM1, CENPU, PKMYT1/MYT1, PPP1R12A/MYPT1 and WEE1. Part of a regulatory circuit that promotes the activation of CDK1 by phosphorylating the positive regulator CDC25C and inhibiting the negative regulators WEE1 and PKMYT1/MYT1. Also acts by mediating phosphorylation of cyclin-B1 (CCNB1) on centrosomes in prophase. Phosphorylates FOXM1, a key mitotic transcription regulator, leading to enhance FOXM1 transcriptional activity. Involved in kinetochore functions and sister chromatid cohesion by phosphorylating BUB1B/BUBR1, FBXO5/EMI1 and STAG2/SA2. PLK1 is high on non-attached kinetochores suggesting a role of PLK1 in kinetochore attachment or in spindle assembly checkpoint (SAC) regulation. Required for kinetochore localization of BUB1B. Regulates the dissociation of cohesin from chromosomes by phosphorylating cohesin subunits such as STAG2/SA2. Phosphorylates SGOL1: required for spindle pole localization of isoform 3 of SGOL1 and plays a role in regulating its centriole cohesion function. Mediates phosphorylation of FBXO5/EMI1, a negative regulator of the APC/C complex during prophase, leading to FBXO5/EMI1 ubiquitination and degradation by the proteasome. Acts as a negative regulator of p53 family members: phosphorylates TOPORS, leading to inhibit the sumoylation of p53/TP53 and simultaneously enhance the ubiquitination and subsequent degradation of p53/TP53. Phosphorylates the transactivation domain of the transcription factor p73/TP73, leading to inhibit p73/TP73-mediated transcriptional activation and pro-apoptotic functions. Phosphorylates BORA, and thereby promotes the degradation of BORA. Contributes to the regulation of AURKA function. Also required for recovery after DNA damage checkpoint and entry into mitosis. Phosphorylates MISP, leading to stabilization of cortical and astral microtubule attachments required for proper spindle positioning (PubMed:8991084, PubMed:11202906, PubMed:12207013, PubMed:12447691, PubMed:12524548, PubMed:12738781, PubMed:12852856, PubMed:12939256, PubMed:14532005, PubMed:14734534, PubMed:15070733, PubMed:15148369, PubMed:15469984, PubMed:16198290, PubMed:16247472, PubMed:16980960, PubMed:17081991, PubMed:17351640, PubMed:17376779, PubMed:17617734, PubMed:18174154, PubMed:18331714, PubMed:18418051, PubMed:18477460, PubMed:18521620, PubMed:18615013, PubMed:19160488, PubMed:19351716, PubMed:19468300, PubMed:19468302, PubMed:19473992, PubMed:19509060, PubMed:19597481, PubMed:23455478, PubMed:23509069). Together with MEIKIN, acts as a regulator of kinetochore function during meiosis I: required both for mono-orientation of kinetochores on sister chromosomes and protection of centromeric cohesin from separase-mediated cleavage (By similarity).

  Database links

Uniprot primary ID P53350
PDB ID 2YAC 2RKU 4O56 3P34 3P35 3P36 3P37 1UMW 4E9C 2OWB 4H71 4E9D 4HY2 4E67 3KB7 2OJX 4A4L 4A4O 3RQ7 3P2Z 3P2W 3FC2 4HAB 4WHL 4WHK 4HCO 4WHH 4LKM 4DFW 4O6W 3THB 4H5X 4X9R 2V5Q 4X9W 4X9V 4J53 4J52 4LKL 1Q4K 1Q4O 3HIK 3HIH 2OU7 3BZI 3FVH 4RCP 2OGQ 4O9W 3Q1I 3C5L
DrugBank ID
BioGrid ID 111362
PharmGKB ID PA33410
KEGG ID hsa:5347
STRING ID 9606.ENSP00000300093
IntAct ID P53350
DMDM 1709658
Reactome R-HSA-380270 R-HSA-5663220 R-HSA-2500257 R-HSA-174178 R-HSA-2467813 R-HSA-162658 R-HSA-156711 R-HSA-176412 R-HSA-176417 R-HSA-5620912 R-HSA-68884 R-HSA-2565942 R-HSA-2299718 R-HSA-68881 R-HSA-380259 R-HSA-69273 R-HSA-2980767 R-HSA-68877
SignaLink P53350
Entrez Gene (Gene ID) 5347
BindingDB P53350

  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 0.813 0.009 0.935 0.000 0.874 0.005 0.868 0.006 0.937 0.005 0.758 0.008 Download
Estate fingerprints 0.775 0.011 0.779 0.005 0.777 0.007 0.776 0.008 0.854 0.005 0.551 0.013 Download
MACCS fingerprints 0.878 0.004 0.778 0.003 0.828 0.004 0.835 0.005 0.910 0.000 0.657 0.005 Download
Daylight fingerprints 0.778 0.006 0.826 0.005 0.802 0.004 0.797 0.005 0.863 0.005 0.608 0.006 Download
ECFP2 fingerprints 0.866 0.008 0.916 0.005 0.891 0.006 0.888 0.006 0.952 0.004 0.782 0.009 Download
ECFP4 fingerprints 0.852 0.006 0.970 0.005 0.911 0.006 0.905 0.005 0.960 0.000 0.827 0.008 Download
ECFP6 fingerprints 0.813 0.005 0.981 0.003 0.897 0.005 0.887 0.005 0.950 0.000 0.806 0.005 Download

  Download datasets

Positive dataset Negative dataset

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