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Target not currently curated in GtoImmuPdb
Target id: 2171
Nomenclature: polo like kinase 4
Abbreviated Name: PLK4
Family: Polo-like kinase (PLK) family
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 970 | 4q28.1 | PLK4 | polo like kinase 4 | |
Mouse | - | 925 | 3 B | Plk4 | polo like kinase 4 | |
Rat | - | 924 | 2q25 | Plk4 | polo-like kinase 4 |
Previous and Unofficial Names ![]() |
serine/threonine kinase 18 | serine/threonine-protein kinase Sak | STK18 | polo-like kinase 4 |
Database Links ![]() |
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Alphafold | O00444 (Hs), Q64702 (Mm), B2GUY1 (Rn) |
BRENDA | 2.7.11.21 |
CATH/Gene3D | 3.30.1120.30 |
ChEMBL Target | CHEMBL3788 (Hs) |
Ensembl Gene | ENSG00000142731 (Hs), ENSMUSG00000025758 (Mm), ENSRNOG00000011654 (Rn) |
Entrez Gene | 10733 (Hs), 20873 (Mm), 310344 (Rn) |
Human Protein Atlas | ENSG00000142731 (Hs) |
KEGG Enzyme | 2.7.11.21 |
KEGG Gene | hsa:10733 (Hs), mmu:20873 (Mm), rno:310344 (Rn) |
OMIM | 605031 (Hs) |
Pharos | O00444 (Hs) |
RefSeq Nucleotide | NM_001190799 (Hs), NM_011495 (Mm), NM_001107669 (Rn) |
RefSeq Protein | NP_055079 (Hs), NP_775261 (Mm), NP_001101139 (Rn) |
UniProtKB | O00444 (Hs), Q64702 (Mm), B2GUY1 (Rn) |
Wikipedia | PLK4 (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen ![]() |
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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: 2,7 |
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Target used in screen: PLK4 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Clinically-Relevant Mutations and Pathophysiology ![]() |
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1. Arquint C, Gabryjonczyk AM, Imseng S, Böhm R, Sauer E, Hiller S, Nigg EA, Maier T. (2015) STIL binding to Polo-box 3 of PLK4 regulates centriole duplication. Elife, 4. [PMID:26188084]
2. 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]
3. Laufer R, Forrest B, Li SW, Liu Y, Sampson P, Edwards L, Lang Y, Awrey DE, Mao G, Plotnikova O et al.. (2013) The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem, 56 (15): 6069-87. [PMID:23829549]
4. Mason JM, Lin DC, Wei X, Che Y, Yao Y, Kiarash R, Cescon DW, Fletcher GC, Awrey DE, Bray MR et al.. (2014) Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent. Cancer Cell, 26 (2): 163-76. [PMID:25043604]
5. Sun Y, Xue Y, Liu H, Mu S, Sun P, Sun Y, Wang L, Wang H, Wang J, Wu T et al.. (2023) Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia. J Med Chem, 66 (4): 2396-2421. [PMID:36734825]
6. Tovar C, Higgins B, Deo D, Kolinsky K, Liu JJ, Heimbrook DC, Vassilev LT. (2010) Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle, 9 (16): 3364-75. [PMID:20814247]
7. 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]
8. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell, 18 (3): 258-67. [PMID:20832753]
Polo-like kinase (PLK) family: polo like kinase 4. Last modified on 23/02/2023. Accessed on 19/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2171.