aurora kinase C | Aurora kinase (Aur) family | IUPHAR/BPS Guide to PHARMACOLOGY

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aurora kinase C

Target not currently curated in GtoImmuPdb

Target id: 1938

Nomenclature: aurora kinase C

Abbreviated Name: AurC

Family: Aurora kinase (Aur) 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 - 309 19q13.3-qter AURKC aurora kinase C
Mouse - 315 7 A2-A3 Aurkc aurora kinase C
Rat - 111 1 q12 Aurkc aurora kinase C
Previous and Unofficial Names
AIK3 | ARK3 | Aurora 3 | serine/threonine-protein kinase 13 | STK13
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1

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
GSK1070916 Hs Inhibition 8.8 pKi 1
pKi 8.8 (Ki 1.5x10-9 M) [1]
tozasertib Hs Inhibition 8.3 pKi 9
pKi 8.3 (Ki 4.6x10-9 M) [9]
AMG-900 Hs Inhibition 9.0 pIC50 10
pIC50 9.0 (IC50 1x10-9 M) [10]
ilorasertib 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 Hs Inhibition 7.9 pIC50 11
pIC50 7.9 (IC50 1.21x10-8 M) [11]
SU6656 Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.7x10-8 M) [3]
danusertib Hs Inhibition 7.2 pIC50 6
pIC50 7.2 (IC50 6.1x10-8 M) [6]
compound 38 [PMID: 20817473] Hs Inhibition 7.2 pIC50 4
pIC50 7.2 (IC50 6.2x10-8 M) [4]
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: 5,13

Key to terms and symbols Click column headers to sort
Target used in screen: AURKC
Ligand Sp. Type Action Value Parameter
axitinib Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Hs Inhibitor Inhibition 8.4 pKd
barasertib-hQPA Hs Inhibitor Inhibition 8.4 pKd
tozasertib Hs Inhibitor Inhibition 8.2 pKd
foretinib Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 7.6 pKd
MLN-8054 Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.5 pKd
tamatinib Hs Inhibitor Inhibition 7.4 pKd
KW-2449 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
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 Hs Inhibitor Inhibition 5.2 3.0 1.0
K-252a Hs Inhibitor Inhibition 7.3 2.0 1.0
midostaurin Hs Inhibitor Inhibition 12.0 62.0 20.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 16.2 -2.0 0.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 20.7 1.0 2.0
JNJ-7706621 Hs Inhibitor Inhibition 28.3 6.0 1.0
JAK inhibitor I Hs Inhibitor Inhibition 29.3 11.0 7.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 30.2 13.0 1.0
PKR inhibitor Hs Inhibitor Inhibition 31.4 18.0 -1.0
SU6656 Hs Inhibitor Inhibition 33.8 75.0 52.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Tissue Distribution
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:  12
Physiological Functions
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
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:  12
Clinically-Relevant Mutations and Pathophysiology
Disease:  Spermatogenic failure 5; SPGF5
Synonyms: Male infertility due to large-headed multiflagellar polyploid spermatozoa [Orphanet: ORPHA137893]
OMIM: 243060
Orphanet: ORPHA137893

References

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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. 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]

13. 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 23/04/2018. Accessed on 21/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1938.