General Information of Binding Target of SBP (BTS) (ID: ST00205)
BTS Name
Aurora kinase A
Synonyms
EC 2.7.11.1; Aurora 2; Aurora/IPL1-related kinase 1; ARK-1; Aurora-related kinase 1; hARK1; Breast tumor-amplified kinase; Serine/threonine-protein kinase 15; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase aurora-A
BTS Type
Protein
Family
Protein kinase superfamily;
Ser/Thr protein kinase family;
Aurora subfamily
Gene Name
AURKA
Organism
Homo sapiens (Human)
Function
Mitotic serine/threonine kinase that contributes to the regulation of cell cycle progression Associates with the centrosome and the spindle microtubules during mitosis and plays a critical role in various mitotic events including the establishment of mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis Required for normal spindle positioning during mitosis and for the localization of NUMA1 and DCTN1 to the cell cortex during metaphase Required for initial activation of CDK1 at centrosomes Phosphorylates numerous target proteins, including ARHGEF2, BORA, BRCA1, CDC25B, DLGP5, HDAC6, KIF2A, LATS2, NDEL1, PARD3, PPP1R2, PLK1, RASSF1, TACC3, p53/TP53 and TPX2 Regulates KIF2A tubulin depolymerase activity Important for microtubule formation and/or stabilization Required for normal axon formation Plays a role in microtubule remodeling during neurite extension Also acts as a key regulatory component of the p53/TP53 pathway, and particularly the checkpoint-response pathways critical for oncogenic transformation of cells, by phosphorylating and destabilizing p53/TP53 Phosphorylates its own inhibitors, the protein phosphatase type 1 (PP1) isoforms, to inhibit their activity Necessary for proper cilia disassembly prior to mitosis Regulates protein levels of the anti-apoptosis protein BIRC5 by suppressing the expression of the SCF(FBXL7) E3 ubiquitin-protein ligase substrate adapter FBXL7 through the phosphorylation of the transcription factor FOXP1
UniProt ID
O14965
UniProt Entry
AURKA_HUMAN
PFam
PF00069
Gene ID
6790
Sequence
MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRVPLQ
AQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKN
EESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRR
EVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITEL
ANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEM
IEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLI
SRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
Sequence Length
403
Synthetic Binding Protein (SBP) Targeting This BTS
SBP Name Highest Status Mechanism Affinity Application Details Ref
Monobody anti-AurA clone 1 Research Activator Kd: 170 nM Tools for allosteric modulation of a human protein kinase
SBP Info
[1], [2]
Monobody anti-AurA clone 2 Research Inhibitor Kd: 1000 nM Tools for allosteric modulation of a human protein kinase
SBP Info
[1], [2], [3]
Monobody anti-AurA clone 3 Research Inhibitor Kd: 160 nM Tools for allosteric modulation of a human protein kinase
SBP Info
[1], [2]
Monobody anti-AurA clone 4 Research Inhibitor Kd: 3300 nM Tools for allosteric modulation of a human protein kinase
SBP Info
[1], [2]
Monobody anti-AurA clone 5 Research Inhibitor Kd: 80 nM Tools for allosteric modulation of a human protein kinase
SBP Info
[1], [2]
Monobody anti-AurA clone 6 Research Inhibitor Kd: 8 nM Tools for allosteric modulation of a human protein kinase
SBP Info
[1], [2]
VNAR anti-AurA D01 Research Inhibitor Kd: 2000 nM Solid tumour/cancer [ICD-11: 2A00-2F9Z]
SBP Info
[4]
References
1 Allosteric modulation of a human protein kinase with monobodies. Proc Natl Acad Sci U S A. 2019 Jul 9;116(28):13937-13942.
2 A potent and highly specific FN3 monobody inhibitor of the Abl SH2 domain. Nat Struct Mol Biol. 2010 Apr;17(4):519-27.
3 Dynamics of human protein kinase Aurora A linked to drug selectivity. Elife. 2018 Jun 14;7:e36656.
4 Allosteric inhibition of Aurora-A kinase by a synthetic vNAR domain. Open Biol. 2016 Jul;6(7):160089.