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polo like kinase 3

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Target id: 2170

Nomenclature: polo like kinase 3

Abbreviated Name: PLK3

Family: Polo-like kinase (PLK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 646 1p34.1 PLK3 polo like kinase 3
Mouse - 631 4 D1 Plk3 polo like kinase 3
Rat - 647 5q36 Plk3 polo-like kinase 3
Previous and Unofficial Names Click here for help
cytokine inducible kinase | FGF-inducible kinase | FNK | CNK | PRK | polo-like kinase 3
Database Links Click here for help
Alphafold Q9H4B4 (Hs), Q60806 (Mm), Q9R011 (Rn)
BRENDA 2.7.11.21
CATH/Gene3D 3.30.1120.30
ChEMBL Target CHEMBL4897 (Hs)
Ensembl Gene ENSG00000173846 (Hs), ENSMUSG00000028680 (Mm), ENSRNOG00000018484 (Rn)
Entrez Gene 1263 (Hs), 12795 (Mm), 58936 (Rn)
Human Protein Atlas ENSG00000173846 (Hs)
KEGG Enzyme 2.7.11.21
KEGG Gene hsa:1263 (Hs), mmu:12795 (Mm), rno:58936 (Rn)
OMIM 602913 (Hs)
Pharos Q9H4B4 (Hs)
RefSeq Nucleotide NM_004073 (Hs), NM_013807 (Mm), NM_022187 (Rn)
RefSeq Protein NP_004064 (Hs), NP_038835 (Mm), NP_071523 (Rn)
UniProtKB Q9H4B4 (Hs), Q60806 (Mm), Q9R011 (Rn)
Wikipedia PLK3 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.21

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BI-2536 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 5
⤷ pIC50 8.1 (IC50 9x10-9 M) [5]
onvansertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition <5.0 pIC50 2
⤷ pIC50 <5.0 (IC50 >1x10-5 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 6.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.6 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.0 55.0 64.0
wortmannin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 14.4
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 28.5 76.0 12.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 37.8 86.0 46.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 45.7 90.0 54.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 48.2 55.0 31.0
compound 52 [PMID: 9677190] Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 48.5 93.0 57.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 52.5 88.0 94.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 62.8 99.0 77.0
AG 112 Small molecule or natural product 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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2170.