Top ▲

aurora kinase C

Click here for help

Target id: 1938

Nomenclature: aurora kinase C

Abbreviated Name: AurC

Family: Aurora kinase (Aur) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 309 19q13.43 AURKC aurora kinase C
Mouse - 276 7 4.06 cM Aurkc aurora kinase C
Rat - 111 1 q12 Aurkc aurora kinase C
Previous and Unofficial Names Click here for help
AIK3 | ARK3 | Aurora 3 | serine/threonine-protein kinase 13 | STK13
Database Links Click here for help
Alphafold Q9UQB9 (Hs), O88445 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL3935 (Hs)
Ensembl Gene ENSG00000105146 (Hs), ENSMUSG00000070837 (Mm), ENSRNOG00000015825 (Rn)
Entrez Gene 6795 (Hs), 20871 (Mm), 292554 (Rn)
Human Protein Atlas ENSG00000105146 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:6795 (Hs), mmu:20871 (Mm), rno:292554 (Rn)
OMIM 603495 (Hs)
Orphanet ORPHA160048 (Hs)
Pharos Q9UQB9 (Hs)
RefSeq Nucleotide NM_001015878 (Hs), NM_001080965 (Mm), NM_001106221 (Rn)
RefSeq Protein NP_001015878 (Hs), NP_001074434 (Mm), NP_001099691 (Rn)
UniProtKB Q9UQB9 (Hs), O88445 (Mm)
Wikipedia AURKC (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
GSK1070916 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.8 pKi 1
⤷ pKi 8.8 (Ki 1.5x10-9 M) [1]
tozasertib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pKi 9
⤷ pKi 8.3 (Ki 4.6x10-9 M) [9]
AMG-900 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pIC50 10
⤷ pIC50 9.0 (IC50 1x10-9 M) [10]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pIC50 8
⤷ pIC50 9.0 (IC50 1x10-9 M) [8]
Description: Measuring inhibition of kinase activity in a biochemical assay.
MK-5108 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 11
⤷ pIC50 7.9 (IC50 1.21x10-8 M) [11]
BI-847325 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 12
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [12]
SU6656 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 3
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [3]
danusertib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 6
⤷ pIC50 7.2 (IC50 6.1x10-8 M) [6]
compound 38 [PMID: 20817473] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 4
⤷ pIC50 7.2 (IC50 6.2x10-8 M) [4]
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: 5,14
Key to terms and symbols Click column headers to sort
Target used in screen: AURKC
Ligand Sp. Type Action Value Parameter
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.4 pKd
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
MLN-8054 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.2 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: 2,7
Key to terms and symbols Click column headers to sort
Target used in screen: Aurora-C/Aurora C
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.2 3.0 1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 7.3 2.0 1.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 12.0 62.0 20.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.2 -2.0 0.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.7 1.0 2.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 28.3 6.0 1.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 29.3 11.0 7.0
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 30.2 13.0 1.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 31.4 18.0 -1.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 33.8 75.0 52.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Tissue Distribution Click here for help
Expression of Auroa kinase C is restricted to the testes and subcellular localisation is shown using mouse spermatocytes or squashed seminiferous tubules.
Species:  Mouse
Technique:  Immunofluorescence.
References:  13
Physiological Functions Click here for help
Aurora kinase C playes a role in controlling chromosome segregation during spermatogenesis.
Species:  Mouse
Tissue:  Meiotic germ cells.
References: 
Physiological Consequences of Altering Gene Expression Click here for help
Aurora kinase C knockout mice are viable, but display compromised male fertility caused by dysregulated meiotic division.
Species:  Mouse
Tissue: 
Technique:  Gene knock-out.
References:  13
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Spermatogenic failure 5; SPGF5
Synonyms: Male infertility due to large-headed multiflagellar polyploid spermatozoa [Orphanet: ORPHA137893]
OMIM: 243060
Orphanet: ORPHA137893

References

Show »

1. Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA et al.. (2010) Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem, 53 (10): 3973-4001. [PMID:20420387]

2. 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]

3. Bain J, Plater L, Elliott M, Shpiro N, Hastie CJ, McLauchlan H, Klevernic I, Arthur JS, Alessi DR, Cohen P. (2007) The selectivity of protein kinase inhibitors: a further update. Biochem J, 408 (3): 297-315. [PMID:17850214]

4. Bindi S, Fancelli D, Alli C, Berta D, Bertrand JA, Cameron AD, Cappella P, Carpinelli P, Cervi G, Croci V et al.. (2010) Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. Bioorg Med Chem, 18 (19): 7113-20. [PMID:20817473]

5. 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]

6. Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P et al.. (2006) 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem, 49 (24): 7247-51. [PMID:17125279]

7. 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]

8. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al.. (2012) Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther, 343 (3): 617-27. [PMID:22935731]

9. Harrington EA, Bebbington D, Moore J, Rasmussen RK, Ajose-Adeogun AO, Nakayama T, Graham JA, Demur C, Hercend T, Diu-Hercend A et al.. (2004) VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med, 10 (3): 262-7. [PMID:14981513]

10. Payton M, Bush TL, Chung G, Ziegler B, Eden P, McElroy P, Ross S, Cee VJ, Deak HL, Hodous BL et al.. (2010) Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 70 (23): 9846-54. [PMID:20935223]

11. Shimomura T, Hasako S, Nakatsuru Y, Mita T, Ichikawa K, Kodera T, Sakai T, Nambu T, Miyamoto M, Takahashi I et al.. (2010) MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther, 9 (1): 157-66. [PMID:20053775]

12. Sini P, Gürtler U, Zahn SK, Baumann C, Rudolph D, Baumgartinger R, Strauss E, Haslinger C, Tontsch-Grunt U, Waizenegger IC et al.. (2016) Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases. Mol Cancer Ther, 15 (10): 2388-2398. [PMID:27496137]

13. Tang CJ, Lin CY, Tang TK. (2006) Dynamic localization and functional implications of Aurora-C kinase during male mouse meiosis. Dev Biol, 290 (2): 398-410. [PMID:16386730]

14. 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

Aurora kinase (Aur) family: aurora kinase C. Last modified on 08/05/2023. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1938.