Details of the Target

General Information of Target

Target ID LDTP13756
Target Name Aurora kinase C (AURKC)
Gene Name AURKC
Gene ID 6795
Synonyms
AIE2; AIK3; AIRK3; ARK3; STK13; Aurora kinase C; EC 2.7.11.1; Aurora 3; Aurora/IPL1-related kinase 3; ARK-3; Aurora-related kinase 3; Aurora/IPL1/Eg2 protein 2; Serine/threonine-protein kinase 13; Serine/threonine-protein kinase aurora-C
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSLSRSEEMHRLTENVYKTIMEQFNPSLRNFIAMGKNYEKALAGVTYAAKGYFDALVKMG
ELASESQGSKELGDVLFQMAEVHRQIQNQLEEMLKSFHNELLTQLEQKVELDSRYLSAAL
KKYQTEQRSKGDALDKCQAELKKLRKKSQGSKNPQKYSDKELQYIDAISNKQGELENYVS
DGYKTALTEERRRFCFLVEKQCAVAKNSAAYHSKGKELLAQKLPLWQQACADPSKIPERA
VQLMQQVASNGATLPSALSASKSNLVISDPIPGAKPLPVPPELAPFVGRMSAQESTPIMN
GVTGPDGEDYSPWADRKAAQPKSLSPPQSQSKLSDSYSNTLPVRKSVTPKNSYATTENKT
LPRSSSMAAGLERNGRMRVKAIFSHAAGDNSTLLSFKEGDLITLLVPEARDGWHYGESEK
TKMRGWFPFSYTRVLDSDGSDRLHMSLQQGKSSSTGNLLDKDDLAIPPPDYGAASRAFPA
QTASGFKQRPYSVAVPAFSQGLDDYGARSMSRNPFAHVQLKPTVTNDRCDLSAQGPEGRE
HGDGSARTLAGR
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family, Aurora subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Also plays a role in meiosis and more particularly in spermatogenesis. Has redundant cellular functions with AURKB and can rescue an AURKB knockdown. Like AURKB, AURKC phosphorylates histone H3 at 'Ser-10' and 'Ser-28'. AURKC phosphorylates the CPC complex subunits BIRC5/survivin and INCENP leading to increased AURKC activity. Phosphorylates TACC1, another protein involved in cell division, at 'Ser-228'.
TTD ID
T97592
Uniprot ID
Q9UQB9
DrugMap ID
TTLYXIT
Ensemble ID
ENST00000302804.12
HGNC ID
HGNC:11391
ChEMBL ID
CHEMBL3935

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO678 SNV: p.T22K DBIA    Probe Info 
FTC133 SNV: p.Q28R .
HCT116 SNV: p.P4H .
HCT15 SNV: p.G17C .
HT115 SNV: p.A153T .
LNCaP clone FGC Deletion: p.A266PfsTer4 .
MEWO SNV: p.C304Y DBIA    Probe Info 
SH4 SNV: p.K137N .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C235(2.40)  LDD3326  [1]
HHS-475
 Probe Info  		Y58(0.80)  LDD0264  [2]
IA-alkyne
 Probe Info  		C200(1.00)  LDD2207  [3]
HHS-465
 Probe Info  		N.A.  LDD2240  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0116  HHS-0101 DM93 Y58(0.80)  LDD0264  [2]
 LDCM0117  HHS-0201 DM93 Y58(0.55)  LDD0265  [2]
 LDCM0118  HHS-0301 DM93 Y58(0.78)  LDD0266  [2]
 LDCM0119  HHS-0401 DM93 Y58(0.65)  LDD0267  [2]
 LDCM0120  HHS-0701 DM93 Y58(1.62)  LDD0268  [2]
 LDCM0022  KB02 42-MG-BA C235(1.17)  LDD2244  [1]
 LDCM0023  KB03 A101D C235(2.81)  LDD2667  [1]
 LDCM0024  KB05 UACC62 C235(2.40)  LDD3326  [1]
 LDCM0628  OTUB2-COV-1 HEK-293T C200(1.00)  LDD2207  [3]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
3 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
4 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010