Aurora B
Aurora B (AURKB) is a mitotic serine/threonine kinase and the enzymatic core of the chromosomal passenger complex (CPC), which includes INCENP, Survivin, and Borealin[1]. Mechanistically, the CPC guides Aurora B through mitosis to control chromosome alignment, histone modification, kinetochore-microtubule error correction, spindle checkpoint signaling, and cytokinesis[1][2]. Therefore, Aurora B activity supports faithful chromosome segregation by releasing incorrect kinetochore-microtubule attachments, while reduced activity increases chromosome missegregation and aneuploid-cell generation[2]. In disease models, Aurora B deregulation or overexpression appears in several tumors, and studies in hepatocellular carcinoma, oral squamous cell carcinoma, prostate carcinoma, and glioblastoma connect Aurora B activity with recurrence, prognosis, tumor growth, or mitotic disruption[3][4][5][6]. Compared with related isoforms, Aurora A localizes to spindle poles and regulates mitotic entry, centrosome maturation, and spindle assembly, whereas Aurora B localizes with the CPC from inner centromeres to the spindle midzone and midbody[7]. Aurora C can act as a chromosomal passenger protein and complement Aurora B in mitotic cells, but Aurora B shows preferential INCENP binding and earlier M-phase expression[8]. For experimental applications, Aurora B or pan-Aurora inhibitors such as VX-680, AMG900, and danusertib help dissect metaphase-anaphase transition, cytokinetic initiation, mitotic progression, and cancer-cell proliferation[6][9][10].
Références:
- [1]. Vader G, et al. The chromosomal passenger complex: guiding Aurora-B through mitosis. J Cell Biol. 2006 Jun 19;173(6):833-7. [Content Brief]
- [2]. Abe Y, et al. System-level deficiencies in Aurora B control in cancers. Cell Cycle. 2016 Aug 17;15(16):2091-2092. [Content Brief]
- [3]. Tanaka S, et al. Aurora kinase B is a predictive factor for the aggressive recurrence of hepatocellular carcinoma after curative hepatectomy. Br J Surg. 2008 May;95(5):611-9. [Content Brief]
- [4]. Pannone G, et al. Aurora B expression as a prognostic indicator and possible therapeutic target in oral squamous cell carcinoma. Int J Immunopathol Pharmacol. 2011 Jan-Mar;24(1):79-88. [Content Brief]
- [5]. Cao M, et al. A Vector-Based Short Hairpin RNA Targeting Aurora B Suppresses Human Prostatic Carcinoma Growth. Technol Cancer Res Treat. 2017 Feb;16(1):112-119. [Content Brief]
- [6]. Ryu J, et al. An Aurora kinase inhibitor, AMG900, inhibits glioblastoma cell proliferation by disrupting mitotic progression. Cancer Med. 2018 Nov;7(11):5589-5603. [Content Brief]
- [7]. Carmena M, et al. Making the Auroras glow: regulation of Aurora A and B kinase function by interacting proteins. Curr Opin Cell Biol. 2009 Dec;21(6):796-805. [Content Brief]
- [8]. Sasai K, et al. Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells. Cell Motil Cytoskeleton. 2004 Dec;59(4):249-63. [Content Brief]
- [9]. Li Z, et al. The Aurora Kinase in Trypanosoma brucei plays distinctive roles in metaphase-anaphase transition and cytokinetic initiation. PLoS Pathog. 2009 Sep;5(9):e1000575. [Content Brief]
- [10]. Meulenbeld HJ, et al. Danusertib, an aurora kinase inhibitor. Expert Opin Investig Drugs. 2012 Mar;21(3):383-93. [Content Brief]
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Aurora B Produits associés (79)
Produits associés (79)
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Anticorps (1)
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Alisertib
0 ImagesSynonyms: MLN 8237Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
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Reversine
0 ImagesReversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
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Tozasertib
0 ImagesSynonyms: VX 680; MK-0457Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
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CCT400028
0 ImagesCat. No.: HY-181311Pureté: 98.03%CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.
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Aurora kinase-IN-10
0 ImagesCat. No.: HY-181082CAS No.: 3053885-69-8Aurora kinase-IN-10 is an Aurora kinase inhibitor. Aurora kinase-IN-10 exhibits IC50 values of 5.94 nM and 86.06 nM against Aurora A and Aurora B, respectively. Aurora kinase-IN-10 has anti-tumor activity and can be used in the research of tumors such as triple-negative breast cancer.
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CG-1521
0 ImagesCat. No.: HY-108919CAS No.: 674767-29-4CG-1521 is a histone deacetylase (HDAC) inhibitor that stabilizes Ac-Lys373 P53, increases P21 levels and HDAC2 degradation. CG-1521 can inhibit proliferation, induce cell cycle arrest and apoptosis. CG-1521 promotes Bax translocation to the mitochondria and cleavage. CG-1521 downregulates KIF4, Aurora B and Nek2 protein expression and DNA synthesis. CG-1521 can be used for the research of prostate cancer and inflammatory breast cancer.
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Hesperadin
0 ImagesHesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
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Danusertib
0 ImagesSynonyms: PHA-739358Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
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LY3295668
0 ImagesSynonyms: AK-01LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer.
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TAK-632
0 ImagesTAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.
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Tinengotinib
0 ImagesSynonyms: TT 00420Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment.
