polo like kinase 3 | Polo-like kinase (PLK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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polo like kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2170

Nomenclature: polo like kinase 3

Abbreviated Name: PLK3

Family: Polo-like kinase (PLK) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 646 1p34.1 PLK3 polo like kinase 3
Mouse - 648 4 D1 Plk3 polo like kinase 3
Rat - 647 5 q36 Plk3 polo-like kinase 3
Previous and Unofficial Names
PRK | CNK | cytokine inducible kinase | FGF-inducible kinase | FNK | polo-like kinase 3
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.21

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BI-2536 Hs Inhibition 8.1 pIC50 5
pIC50 8.1 (IC50 9x10-9 M) [5]
NMS-P937 Hs Inhibition <5.0 pIC50 2
pIC50 <5.0 (IC50 >1x10-5 M) [2]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: PLK3
Ligand Sp. Type Action Value Parameter
BI-2536 Hs Inhibitor Inhibition 8.4 pKd
tamatinib Hs Inhibitor Inhibition 8.3 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
ruxolitinib Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Hs Inhibitor Inhibition 6.1 pKd
staurosporine Hs Inhibitor Inhibition 6.0 pKd
fedratinib Hs Inhibitor Inhibition 5.8 pKd
PD-173955 Hs Inhibitor Inhibition 5.7 pKd
lestaurtinib Hs Inhibitor Inhibition 5.6 pKd
PP-242 Hs Inhibitor Inhibition 5.6 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: Plk3/PLK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
JAK inhibitor I Hs Inhibitor Inhibition 11.0 55.0 64.0
wortmannin Hs Inhibitor Inhibition 14.4
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 28.5 76.0 12.0
staurosporine Hs Inhibitor Inhibition 37.8 86.0 46.5
K-252a Hs Inhibitor Inhibition 45.7 90.0 54.0
isogranulatimide Hs Inhibitor Inhibition 48.2 55.0 31.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 48.5 93.0 57.0
SB 218078 Hs Inhibitor Inhibition 52.5 88.0 94.0
aminopurvalanol A Hs Inhibitor Inhibition 62.8 99.0 77.0
AG 112 Hs Inhibitor Inhibition 63.6 79.0 27.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E et al.. (2011) NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg. Med. Chem. Lett., 21 (10): 2969-74. [PMID:21470862]

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Steegmaier M, Hoffmann M, Baum A, Lénárt P, Petronczki M, Krssák M, Gürtler U, Garin-Chesa P, Lieb S, Quant J et al.. (2007) BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Curr. Biol., 17 (4): 316-22. [PMID:17291758]

6. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Polo-like kinase (PLK) family: polo like kinase 3. Last modified on 29/01/2016. Accessed on 31/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2170.