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aurora kinase B

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Target id: 1937

Nomenclature: aurora kinase B

Abbreviated Name: AurB

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 - 344 17p13.1 AURKB aurora kinase B
Mouse - 345 11 42.32 cM Aurkb aurora kinase B
Rat - 343 10q24 Aurkb aurora kinase B
Previous and Unofficial Names Click here for help
Aik2 | Aim1 | AIRK2 | ARK2 | serine/threonine-protein kinase 12 | serine/threonine-protein kinase 5 | STK-1 | STK12 | STK5
Database Links Click here for help
Alphafold Q96GD4 (Hs), O70126 (Mm), O55099 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2185 (Hs), CHEMBL1075275 (Mm)
Ensembl Gene ENSG00000178999 (Hs), ENSMUSG00000020897 (Mm), ENSRNOG00000005659 (Rn)
Entrez Gene 9212 (Hs), 20877 (Mm), 114592 (Rn)
Human Protein Atlas ENSG00000178999 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9212 (Hs), mmu:20877 (Mm), rno:114592 (Rn)
OMIM 604970 (Hs)
Pharos Q96GD4 (Hs)
RefSeq Nucleotide NM_001256834 (Hs), NM_011496 (Mm), NM_053749 (Rn)
RefSeq Protein NP_004208 (Hs), NP_035626 (Mm), NP_446201 (Rn)
SynPHARM 81213 (in complex with tozasertib)
UniProtKB Q96GD4 (Hs), O70126 (Mm), O55099 (Rn)
Wikipedia AURKB (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Human Aurora B Kinase in complex with INCENP and VX-680 (tozasertib)
PDB Id:  4AF3
Ligand:  tozasertib
Resolution:  2.75Å
Species:  Human
References:  12
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
barasertib-hQPA Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.3 pKd 10
⤷ pKd 8.3 (Kd 4.6x10-9 M) [10]
GSK1070916 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.4 pKi 1
⤷ pKi 9.4 (Ki 3.8x10-10 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 7.7 pKi 18
⤷ pKi 7.7 (Ki 1.8x10-8 M) [18]
barasertib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.4 pIC50 37
⤷ pIC50 9.4 (IC50 3.7x10-10 M) [37]
barasertib-hQPA 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) This data refers to Compound 7 in Table 7 of the listed reference. [30]
compound 1 [PMID: 21742770] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 34
⤷ pIC50 8.6 (IC50 2.8x10-9 M) [34]
AT-9283 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition ~8.5 pIC50 20
⤷ pIC50 ~8.5 (IC50 ~3x10-9 M) [20]
tinengotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 36
⤷ pIC50 8.5 (IC50 3.3x10-9 M) [36]
AMG-900 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 29
⤷ pIC50 8.4 (IC50 4x10-9 M) [29]
compound 46 [PMID: 16451062] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >8.1 pIC50 22
⤷ pIC50 >8.1 (IC50 <7x10-9 M) [22]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 17
⤷ pIC50 8.1 (IC50 7x10-9 M) [17]
Description: Measuring inhibition of kinase activity in a biochemical assay.
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 38
⤷ pIC50 8.1 (IC50 9x10-9 M) [38]
Description: Inhibition in a biochemical assay.
MLN-8054 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 2
⤷ pIC50 8.0 (IC50 9.3x10-9 M) [2]
dubermatinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.9 pIC50 26
⤷ pIC50 7.9 (IC50 1.24x10-8 M) [26]
JNJ-7706621 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 21
⤷ pIC50 7.9 (IC50 1.3x10-8 M) [21]
compound 25 [PMID: 20855207] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >7.9 pIC50 6
⤷ pIC50 >7.9 (IC50 <1.3x10-8 M) [6]
MK-5108 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 31
⤷ pIC50 7.8 (IC50 1.41x10-8 M) [31]
XMD-12 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 23
⤷ pIC50 7.7 (IC50 1.84x10-8 M) [23]
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 7.7 pIC50 4
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [4]
cenisertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 – 8.1 pIC50 9,24
⤷ pIC50 8.1 (IC50 7x10-9 M) [24]
Description: Measuring phosphorylation of AurB substrate histone H3 in A549 cells.
pIC50 7.3 (IC50 5.4x10-8 M) [9]
Description: In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM.
BX-795 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.5 pIC50 8
⤷ pIC50 7.5 (IC50 3.1x10-8 M) [8]
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 7.5 pIC50 28
⤷ pIC50 7.5 (IC50 3.1x10-8 M) [28]
Cdk2 inhibitor IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 21
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [21]
NIK inhibitor 12f Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.4 pIC50 39
⤷ pIC50 7.4 (IC50 4.32x10-8 M) [39]
Description: Inhibitory concentration determined in a Reaction Biology kinase sreening assay.
compound 38 [PMID: 20817473] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 7
⤷ pIC50 7.3 (IC50 4.5x10-8 M) [7]
KW-2449 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 32
⤷ pIC50 7.3 (IC50 4.8x10-8 M) [32]
TAK-632 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.2 pIC50 27
⤷ pIC50 7.2 (IC50 6.6x10-8 M) [27]
Description: Biochemical enzyme inhibition assay.
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 7.1 pIC50 13
⤷ pIC50 7.1 (IC50 7.9x10-8 M) [13]
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]
VIC 1911 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 33
⤷ pIC50 6.8 (IC50 1.4x10-7 M) [33]
hesperadin Small molecule or natural product Ligand has a PDB structure Hs Inhibition 6.6 pIC50 19
⤷ pIC50 6.6 (IC50 2.5x10-7 M) [19]
aurora kinase inhibitor II Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.9 pIC50 14
⤷ pIC50 5.9 (IC50 1.25x10-6 M) [14]
GSK2334470 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 25
⤷ pIC50 5.5 (IC50 3.16x10-6 M) [25]
compound 10 [PMID: 19402633] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 2
⤷ pIC50 5.5 (IC50 3.4x10-6 M) [2]
GSK2646264 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition <4.6 pIC50 5
⤷ pIC50 <4.6 (IC50 >2.512x10-5 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: 10,35
Key to terms and symbols Click column headers to sort
Target used in screen: AURKB
Ligand Sp. Type Action Value Parameter
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 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 7.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
MLN-8054 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.1 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: 3,16
Key to terms and symbols Click column headers to sort
Target used in screen: Aurora-B/Aurora B
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 3.0 1.0 3.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 3.5 0.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.3 0.5 -0.5
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 4.3 2.0 -1.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.9
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 8.5 4.0 4.0
PKR inhibitor, negative control Small molecule or natural product Hs Inhibitor Inhibition 9.2 51.0 2.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 9.5 2.0 4.0
semaxanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.6 6.0 0.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 10.5 3.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  B cell (activation)
Tissue Distribution Click here for help
Aurora kinase B (as part of the passenger complex) localise to centromeres from prometaphase to metaphase. Following chromatid separation, Aurora kinase B redistributes to midzone and persists at the midbody until cytokinesis is completed.
Species:  Human
Technique:  Transfected HeLa cells.
References:  15
Physiological Functions Click here for help
Aurora kinase B is a component of the chromosomal passenger complex which functions to ensure accurate chromosome segregation and cell body division during mitosis.
Species:  Human
Tissue:  Transfected HeLA cells
References:  15

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. 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. 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]

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. 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]

7. 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]

8. Clark K, Plater L, Peggie M, Cohen P. (2009) Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem, 284 (21): 14136-46. [PMID:19307177]

9. Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR et al.. (2012) Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. Bioorg Med Chem Lett, 22 (14): 4750-5. [PMID:22695126]

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. Elkins JM, Santaguida S, Musacchio A, Knapp S. (2012) Crystal structure of human aurora B in complex with INCENP and VX-680. J Med Chem, 55 (17): 7841-8. [PMID:22920039]

13. 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]

14. 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]

15. 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]

16. 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]

17. 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]

18. 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]

19. Hauf S, Cole RW, LaTerra S, Zimmer C, Schnapp G, Walter R, Heckel A, van Meel J, Rieder CL, Peters JM. (2003) The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. J Cell Biol, 161 (2): 281-94. [PMID:12707311]

20. 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]

21. 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]

22. 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]

23. 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]

24. Li H, Argade A, Singh R, Thota S, Carroll D, Tso K, Taylor V, Mclaughlin J, Markovstov VMV. (2005) Cycloalkyl substituted pyrimidinediamine compounds and their uses. Patent number: WO2005118544A2. Assignee: Rigel Pharmaceuticals, Inc.. Priority date: 18/05/2004. Publication date: 15/12/2005.

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. Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S et al.. (2013) Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J Med Chem, 56 (16): 6478-94. [PMID:23906342]

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. 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]

32. 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]

33. 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.

34. Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA et al.. (2012) A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett, 3 (12): 1034-1038. [PMID:23256033]

35. 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]

36. Wu F. (2021) Multi-kinase inhibitor compound, and crystal form and use thereof. Patent number: US10889586B2. Assignee: Nanjing Transthera Biosciences Co Ltd. Priority date: 13/12/2016. Publication date: 12/01/2021.

37. Yang J, Ikezoe T, Nishioka C, Tasaka T, Taniguchi A, Kuwayama Y, Komatsu N, Bandobashi K, Togitani K, Koeffler HP et al.. (2007) AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood, 110 (6): 2034-40. [PMID:17495131]

38. Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao JZ et al.. (2017) CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci, 108 (3): 469-477. [PMID:28004478]

39. Zhu Y, Ma Y, Zu W, Song J, Wang H, Zhong Y, Li H, Zhang Y, Gao Q, Kong B et al.. (2020) Identification of N-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives as Novel, Potent, and Selective NF-κB Inducing Kinase (NIK) Inhibitors for the Treatment of Psoriasis. J Med Chem, 63 (13): 6748-6773. [PMID:32479083]

How to cite this page

Aurora kinase (Aur) family: aurora kinase B. Last modified on 03/11/2022. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1937.