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aurora kinase A

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Target not currently curated in GtoImmuPdb

Target id: 1936

Nomenclature: aurora kinase A

Abbreviated Name: AurA

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 - 403 20q13.2 AURKA aurora kinase A
Mouse - 395 2 94.84 cM Aurka aurora kinase A
Rat - 397 3q42 Aurka aurora kinase A
Previous and Unofficial Names Click here for help
ARK1 | AurA | Aurora 2 | Aurora family kinase 1 | ratAurA | serine/threonine kinase 15 | serine/threonine kinase 6 | STK15 | STK6
Database Links Click here for help
Alphafold O14965 (Hs), P97477 (Mm), P59241 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL4722 (Hs), CHEMBL2211 (Mm)
Ensembl Gene ENSG00000087586 (Hs), ENSMUSG00000027496 (Mm), ENSRNOG00000004479 (Rn)
Entrez Gene 6790 (Hs), 20878 (Mm), 261730 (Rn)
Human Protein Atlas ENSG00000087586 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:6790 (Hs), mmu:20878 (Mm), rno:261730 (Rn)
OMIM 603072 (Hs)
Pharos O14965 (Hs)
RefSeq Nucleotide NM_003600 (Hs), NM_011497 (Mm), NM_153296 (Rn)
RefSeq Protein NP_003591 (Hs), NP_035627 (Mm), NP_695208 (Rn)
SynPHARM 80348 (in complex with aurora kinase inhibitor III)
80836 (in complex with danusertib)
85589 (in complex with JNJ-7706621)
81109 (in complex with MK-5108)
81210 (in complex with MLN-8054)
81211 (in complex with MLN-8054)
81212 (in complex with tozasertib)
81214 (in complex with tozasertib)
UniProtKB O14965 (Hs), P97477 (Mm), P59241 (Rn)
Wikipedia AURKA (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of AuroraA with pyridyl-pyrimidine urea inhibitor
PDB Id:  3EFW
Resolution:  2.29Å
Species:  Human
References:  9
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Aurora-A Protein Kinase
PDB Id:  1MQ4
Resolution:  1.9Å
Species:  Human
References:  27
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
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 8.4 pKd 10
⤷ pKd 8.4 (Kd 3.9x10-9 M) [10]
MLN-8054 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pKd 10
⤷ pKd 8.2 (Kd 6.5x10-9 M) [10]
RG-1530 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pKd 39
⤷ pKd 7.0 (Kd 9.6x10-8 M) [39]
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 9.2 pKi 17
⤷ pKi 9.2 (Ki 6x10-10 M) [17]
GSK-3 inhibitor XIII Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pKi 6
⤷ pKi 7.2 (Ki 5.8x10-8 M) [6]
GSK1070916 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pKi 1
⤷ pKi 6.3 (Ki 4.9x10-7 M) [1]
VTX-11e Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pKi 4
⤷ pKi 6.3 (Ki 5.4x10-7 M) [4]
MK-5108 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 10.2 pIC50 33
⤷ pIC50 10.2 (IC50 6.4x10-11 M) [33]
VIC 1911 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.4 pIC50 36
⤷ pIC50 9.4 (IC50 4x10-10 M) [36]
alisertib Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.0 pIC50 30
⤷ pIC50 9.0 (IC50 1x10-9 M) [30]
compound 46 [PMID: 16451062] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >9.0 pIC50 20
⤷ pIC50 >9.0 (IC50 <1x10-9 M) [20]
tinengotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.9 pIC50 41
⤷ pIC50 8.9 (IC50 1.2x10-9 M) [41]
MLN-8054 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 – 9.0 pIC50 2,24
⤷ pIC50 8.4 – 9.0 (IC50 4x10-9 – 1x10-9 M) [2,24]
AT-9283 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition ~8.5 pIC50 18
⤷ pIC50 ~8.5 (IC50 ~3x10-9 M) [18]
dubermatinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 26
⤷ pIC50 8.5 (IC50 3x10-9 M) [26]
compound 10 [PMID: 19402633] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 2
⤷ pIC50 8.5 (IC50 3.4x10-9 M) [2]
compound 25 [PMID: 20855207] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >8.4 pIC50 7
⤷ pIC50 >8.4 (IC50 <4x10-9 M) [7]
GSK143 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 22
⤷ pIC50 8.3 (IC50 4.8x10-9 M) [22]
Description: Enzyme inhibition assay using recombinant human protein
AMG-900 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 29
⤷ pIC50 8.3 (IC50 5x10-9 M) [29]
XMD-12 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 21
⤷ pIC50 8.3 (IC50 5.6x10-9 M) [21]
SNS-314 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 28
⤷ pIC50 8.1 (IC50 9x10-9 M) [28]
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 7.9 pIC50 12
⤷ pIC50 7.9 (IC50 1.3x10-8 M) [12]
ENMD-2076 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 30
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [30]
JNJ-7706621 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 19
⤷ pIC50 7.7 (IC50 1.8x10-8 M) [19]
compound 38 [PMID: 20817473] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 8
⤷ pIC50 7.7 (IC50 1.8x10-8 M) [8]
BI-847325 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 35
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [35]
aurora kinase inhibitor III Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.4 pIC50 38
⤷ pIC50 7.4 (IC50 4.2x10-8 M) [38]
KW-2449 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 34
⤷ pIC50 7.3 (IC50 4.8x10-8 M) [34]
Cdk2 inhibitor IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 19
⤷ pIC50 7.2 (IC50 6.7x10-8 M) [19]
compound 16 [PMID: 18945615] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 32
⤷ pIC50 7.0 (IC50 9.3x10-8 M) [32]
ZM447439 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 11
⤷ pIC50 7.0 (IC50 1x10-7 M) [11]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.9 pIC50 16
⤷ pIC50 6.9 (IC50 1.2x10-7 M) [16]
Description: Measuring inhibition of kinase activity in a biochemical assay.
PF-562271 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pIC50 31
⤷ pIC50 6.8 (IC50 1.45x10-7 M) [31]
aurora kinase inhibitor II Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.5 pIC50 13
⤷ pIC50 6.5 (IC50 3.1x10-7 M) [13]
barasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.9 pIC50 42
⤷ pIC50 5.9 (IC50 1.368x10-6 M) [42]
Rho kinase inhibitor IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.6 pIC50 37
⤷ pIC50 5.6 (IC50 2.35x10-6 M) [37]
GSK2334470 Small molecule or natural product Click here for species-specific activity table Hs Inhibition <5.0 pIC50 25
⤷ pIC50 <5.0 (IC50 >1x10-5 M) [25]
GSK2646264 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition <4.3 pIC50 5
⤷ pIC50 <4.3 (IC50 >5.012x10-5 M) [5]
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: 10,40
Key to terms and symbols Click column headers to sort
Target used in screen: AURKA
Ligand Sp. Type Action Value Parameter
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
MLN-8054 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 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: 3,15
Key to terms and symbols Click column headers to sort
Target used in screen: Aurora-A/Aurora A
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.4 1.0 10.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.4 -5.5 -2.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.0 1.0 5.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 4.5 -3.0 -2.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 4.6 2.0 -1.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.2
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 9.8 7.0 3.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.0 0.0 -2.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.1 36.0 13.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 17.1 31.0 25.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Tissue Distribution Click here for help
Aurora kinase A localises to the centrosomes during DNA duplication in the S phase and migrates to spindle poles during mitosis.
Species:  Human
Technique:  Transfected HeLa cells.
References:  14
Physiological Functions Click here for help
Aurora kinase A plays a central role in centrosome regulation and mitotic spindle formation.
Species:  Human
Tissue:  Transfected HeLa cells.
References:  14
Physiological Consequences of Altering Gene Expression Click here for help
Aurora kinase A knock-out mice are not viable. Aurka−/− embryos die before the 16-cell stage.
Species:  Mouse
Tissue: 
Technique:  Gene knock-out.
References:  23
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Colorectal cancer
Disease Ontology: DOID:9256
OMIM: 114500

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. Aliagas-Martin I, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Huang OW, Hunsaker T, Kleinheinz T, Krueger E et al.. (2009) A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J Med Chem, 52 (10): 3300-7. [PMID:19402633]

3. 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]

4. Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J et al.. (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. J Med Chem, 52 (20): 6362-8. [PMID:19827834]

5. Barker MD, Liddle J, Atkinson FL, Wilson DM, Dickson MC, Ramirez-Molina C, Lewis H, Davis RP, Somers DO, Neu M et al.. (2018) Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. Bioorg Med Chem Lett, 28 (21): 3458-3462. [PMID:30249354]

6. Bebbington D, Binch H, Charrier JD, Everitt S, Fraysse D, Golec J, Kay D, Knegtel R, Mak C, Mazzei F et al.. (2009) The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett, 19 (13): 3586-92. [PMID:19447622]

7. Belanger DB, Williams MJ, Curran PJ, Mandal AK, Meng Z, Rainka MP, Yu T, Shih NY, Siddiqui MA, Liu M et al.. (2010) Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Bioorg Med Chem Lett, 20 (22): 6739-43. [PMID:20855207]

8. 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]

9. Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A et al.. (2009) Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase. Bioorg Med Chem Lett, 19 (2): 424-7. [PMID:19062275]

10. 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]

11. Ditchfield C, Johnson VL, Tighe A, Ellston R, Haworth C, Johnson T, Mortlock A, Keen N, Taylor SS. (2003) Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol, 161 (2): 267-80. [PMID:12719470]

12. 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]

13. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci USA, 104 (51): 20523-8. [PMID:18077363]

14. Fu J, Bian M, Jiang Q, Zhang C. (2007) Roles of Aurora kinases in mitosis and tumorigenesis. Mol Cancer Res, 5 (1): 1-10. [PMID:17259342]

15. 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]

16. 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]

17. 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]

18. Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL et al.. (2009) Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J Med Chem, 52 (2): 379-88. [PMID:19143567]

19. Jorda R, Hendrychová D, Voller J, Řezníčková E, Gucký T, Kryštof V. (2018) How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem, 61 (20): 9105-9120. [PMID:30234987]

20. Jung FH, Pasquet G, Lambert-van der Brempt C, Lohmann JJ, Warin N, Renaud F, Germain H, De Savi C, Roberts N, Johnson T et al.. (2006) Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. J Med Chem, 49 (3): 955-70. [PMID:16451062]

21. Kwiatkowski N, Deng X, Wang J, Tan L, Villa F, Santaguida S, Huang HC, Mitchison T, Musacchio A, Gray N. (2012) Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. ACS Chem Biol, 7 (1): 185-96. [PMID:21992004]

22. Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS et al.. (2011) Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg Med Chem Lett, 21 (20): 6188-94. [PMID:21903390]

23. Lu LY, Wood JL, Ye L, Minter-Dykhouse K, Saunders TL, Yu X, Chen J. (2008) Aurora A is essential for early embryonic development and tumor suppression. J Biol Chem, 283 (46): 31785-90. [PMID:18801727]

24. Manfredi MG, Ecsedy JA, Meetze KA, Balani SK, Burenkova O, Chen W, Galvin KM, Hoar KM, Huck JJ, LeRoy PJ et al.. (2007) Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci USA, 104 (10): 4106-11. [PMID:17360485]

25. Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP et al.. (2011) Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. J Med Chem, 54 (6): 1871-95. [PMID:21341675]

26. Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. (2011) Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett, 2 (12): 907-912. [PMID:22247788]

27. Nowakowski J, Cronin CN, McRee DE, Knuth MW, Nelson CG, Pavletich NP, Rogers J, Sang BC, Scheibe DN, Swanson RV et al.. (2002) Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography. Structure, 10 (12): 1659-67. [PMID:12467573]

28. Oslob JD, Romanowski MJ, Allen DA, Baskaran S, Bui M, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris S et al.. (2008) Discovery of a potent and selective aurora kinase inhibitor. Bioorg Med Chem Lett, 18 (17): 4880-4. [PMID:18678489]

29. 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]

30. Pollard JR, Mortimore M. (2009) Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem, 52 (9): 2629-51. [PMID:19320489]

31. Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J et al.. (2008) Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 68 (6): 1935-44. [PMID:18339875]

32. Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R et al.. (2008) Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity. Bioorg Med Chem Lett, 18 (23): 6142-6. [PMID:18945615]

33. 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]

34. Shiotsu Y, Kiyoi H, Ishikawa Y, Tanizaki R, Shimizu M, Umehara H, Ishii K, Mori Y, Ozeki K, Minami Y et al.. (2009) KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood, 114 (8): 1607-17. [PMID:19541823]

35. 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]

36. Sugimoto T, Takahashi H, Mitsuya M, Masuko N, Sootome H. (2018) Piperidine compound or salt thereof. Patent number: US10092556B2. Assignee: Taiho Pharmaceutical Co Ltd. Priority date: 29/02/2012. Publication date: 19/10/2018.

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How to cite this page

Aurora kinase (Aur) family: aurora kinase A. Last modified on 08/05/2023. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1936.