Property Summary

NCBI Gene PubMed Count 482
Grant Count 311
R01 Count 188
Funding $31,783,904.99
PubMed Score 1176.34
PubTator Score 931.92

Knowledge Summary

Patent (74,781)

Expression

  Differential Expression (12)

Disease log2 FC p
malignant mesothelioma 1.800 0.000
osteosarcoma -1.120 0.042
sonic hedgehog group medulloblastoma 1.300 0.001
atypical teratoid / rhabdoid tumor 1.200 0.000
glioblastoma 1.200 0.003
medulloblastoma, large-cell 1.700 0.000
non-small cell lung cancer 1.839 0.000
breast carcinoma 1.400 0.000
lung adenocarcinoma 1.200 0.000
inflammatory breast cancer 3.000 0.000
invasive ductal carcinoma 1.200 0.000
psoriasis 1.900 0.000

Synonym

Accession P53350 Q15153 Q99746
Symbols PLK
STPK13

Gene

PDB

1Q4K   1Q4O   1UMW   2OGQ   2OJX   2OU7   2OWB   2RKU   2V5Q   2YAC   3BZI   3C5L   3FC2   3FVH   3HIH   3HIK   3KB7   3P2W   3P2Z   3P34   3P35   3P36   3P37   3Q1I   3RQ7   3THB   4A4L   4A4O   4DFW   4E67   4E9C   4E9D   4H5X   4H71   4HAB   4HCO   4HY2   4J52   4J53   4LKL   4LKM   4O56   4O6W   4O9W   4RCP   4WHH   4WHK   4WHL   4X9R   4X9V   4X9W   5J19  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

MLP Assay (17)

AID Type Active / Inconclusive / Inactive Description
619 screening 518 / 0 / 96591 Fluorescence polarization assay for PLK1 inhibitors
693 screening 127 / 0 / 96922 High throughput fluorescence polarization-based assay to screen for small molecule inhibitors of the Polo box domain (PBD) of Plk1.
744 screening 42 / 3 / 164 Fluorescence polarization assay for PLK1 confirmation assay
756 other 2 / 0 / 207 Fluorescence Polarization assay for Plk1: compound interference assay
785 confirmatory 39 / 1 / 0 Fluorescence Polarization assay for Plk1: IC50 Dose Response Assay
876 confirmatory 4 / 0 / 115 Concentration Response Redox Cycling H2O2 Generation assay to characterize small molecule inhibitors identified in the Polo box domain (PBD) of Plk1 Primary HTS.
877 confirmatory 15 / 0 / 102 Concentration Response fluorescence polarization-based assay to confirm small molecule inhibitors identified in the Polo box domain (PBD) of Plk1 Primary HTS.
936 confirmatory 2 / 0 / 117 Concentration Response Redox Cycling H2O2 Generation assay, 1 mM DTT, to characterize small molecule inhibitors identified in the Polo box domain (PBD) of Plk1 Primary HTS.
1053 screening 2 / 0 / 182 High throughput fluorescence polarization-based assay to screen for small molecule inhibitors of the Polo box domain (PBD) of Plk1 to follow up on purchased Analogs of Selected Hits from the screen.
1057 confirmatory 0 / 0 / 33 Concentration Response fluorescence polarization-based assay to test PMLSC Chemistry Core synthesized analogs of confirmed hits from the Polo box domain (PBD) of Plk1 Primary HTS.
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Gene RIF (432)

PMID Text
27102712 Augmented expression of Aurora kinase-A and Polo-like kinase-1 at the lactogenic switch likely mediates the formation of binucleated cells.
27002166 MLL5 preserves spindle bipolarity through maintaining cytosolic PLK1 in a nonaggregated form.
26919439 Mutation of the T-loop activating residue T210 and adjacent T214 are lethal, but individual mutation of the remaining 32 posttranslational modification sites did not disrupt the essential functions of Plk1.
26912231 Bub1-Plk1-mediated phosphorylation of Cdc20 constitutes an anaphase-promoting complex or cyclosome-inhibitory mechanism that is parallel, but not redundant, to mitotic checkpoint complex formation.
26794530 PLK1 is overexpressed in osteosarcoma and GSK461364 exerted its cytotoxic effect on osteosarcoma by inducing mitotic arrest and subsequent apoptosis and induced cellular senescence
26786872 Perturbations in PLK functions have disease implications, such as cancer in humans, and thus human PLK1 is targeted for cancer therapeutics
26647647 PCNT has to be phosphorylated by PLK1 to be a suitable substrate of separase.
26608325 The authers have identified the serine/threonine kinase Polo-like kinase 1 (PLK1) as a host kinase that phosphorylates mumps virus P and have found that phosphorylation of P by PLK1 is enhanced by mumps virus NP.
26595675 Suggest that the p53-p21-DREAM-CDE/CHR pathway regulates p53-dependent repression of Survivin, CDC25C, and PLK1 in HCT116 cells.
26576650 FOXM1 is overexpressed in a large proportion of gastric carcinomas at the protein level and FOXM1 and PLK1 are concomitantly overexpressed at the mRNA level in this cancer type
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AA Sequence

MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEI      1 - 70
SDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSLLE     71 - 140
LHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDLEVKIGDFGLATKVEYDGERKKT    141 - 210
LCGTPNYIAPEVLSKKGHSFEVDVWSIGCIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAAS    211 - 280
LIQKMLQTDPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENP    281 - 350
LPERPREKEEPVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDK    351 - 420
YGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLKYFRNYMSEHL    421 - 490
LKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTKLILCPLMAAVTYIDEKRDFR    491 - 560
TYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRLKAS                               561 - 603
//

Text Mined References (498)

PMID Year Title
27173435 2016 An organelle-specific protein landscape identifies novel diseases and molecular mechanisms.
27102712 2016 Essential role for a novel population of binucleated mammary epithelial cells in lactation.
27002166 2016 MLL5 maintains spindle bipolarity by preventing aberrant cytosolic aggregation of PLK1.
26919439 2016 The Functional Significance of Posttranslational Modifications on Polo-Like Kinase 1 Revealed by Chemical Genetic Complementation.
26912231 2016 The Bub1-Plk1 kinase complex promotes spindle checkpoint signalling through Cdc20 phosphorylation.
26794530 2016 Cytotoxic mechanism of PLK1 inhibitor GSK461364 against osteosarcoma: Mitotic arrest, apoptosis, cellular senescence, and synergistic effect with paclitaxel.
26786872 2016 Functions of Polo-Like Kinases: A Journey From Yeast To Humans.
26647647 2015 PLK1 regulation of PCNT cleavage ensures fidelity of centriole separation during mitotic exit.
26638075 2015 A Dynamic Protein Interaction Landscape of the Human Centrosome-Cilium Interface.
26608325 2015 Mumps Virus Nucleoprotein Enhances Phosphorylation of the Phosphoprotein by Polo-Like Kinase 1.
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