Inhibition of aurora b activity. Medical search. Frequent questions

In particular, compound 21 (SNS-314) is a potent and selective Aurora kinase inhibitor that exhibits significant activity in pre-clinical in vivo tumor models. (rcsb.org)
A crystal structure of Aurora kinase A in complex with an initial hit revealed a binding mode of the inhibitor within the ATP binding site and provided insight for structure-guided compound optimization. (rcsb.org)
Subsequent SAR campaign provided a potent and selective pan Aurora inhibitor, which demonstrated potent target modulation and antiproliferative effects in the pancreatic cell line, MIAPaCa-2. (rcsb.org)
Background: The phosphorylation of NF-kappaB inhibitor alpha (IκBα) protein is pivotal to the regulation of NF-κB transcription factor activity in the cell. (researchsquare.com)
MLN8237, an Aurora inhibitor induced G2/M arrest with polyploidy and abrogated Aurora A and histone-H3 phosphorylation. (elsevierpure.com)
In this study, we investigated the effect of AKI603, a novel small molecule inhibitor of Aurora kinase A (AurA) to overcome resistance mediated by BCR-ABL-T315I mutation. (scite.ai)
In this paper we analyzed the participation of Aurora kinase B (AurKB) in the DENV replicative cycle using the specific AurKB inhibitor ZM447439. (mendeley.com)
SNS-314 is an ATP-competitive, selective, and potent nanomolar inhibitor of aurora kinases in vitro. (cogershop.com)
SNS-314 is a potent small-molecule inhibitor of Aurora kinase that is being developed as a novel anti-cancer therapeutic agent. (cogershop.com)
MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. (xcessbio.com)
Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. (xcessbio.com)
We tested this hypothesis by determining the antitumor effects of KW- 2450, a multikinase inhibitor of both Aurora A and B kinases. (elsevierpure.com)
Treating SCCHN cell lines with a pan-Aurora kinase inhibitor resulted in defective cytokinesis, polyploidy and apoptosis, which was effective irrespective of the EGFR status. (oncotarget.com)
These data suggest KYC is certainly a book and particular inhibitor of MPO activity that's non-toxic to 1353859-00-3 supplier endothelial cell civilizations. (technumber.com)
A test kit to evaluate the inhibition of Aurora A kinase (CycLex Aurora Family Kinase Assay / Inhibitor Screening Kit) will be performed. (edu.pl)
The arrangement and the interaction network formed by the inhibitor molecule bound by Aurora A kinase will serve as a benchmark for the results obtained with the test compounds. (edu.pl)

The Aurora kinases associate with microtubules during chromosome movement and segregation. (wikipedia.org)
In 1998, Aurora kinase B was identified in humans by a polymerase chain reaction screen for kinases that are overexpressed in cancers. (wikipedia.org)
In the same year, rat Aurora kinase B was identified in a screen designed to find kinases that altered S. cerevisiae proliferation when overexpressed. (wikipedia.org)
Numerous kinetochore targets of Aurora kinases have been determined in organisms ranging from yeast to man. (wikipedia.org)
Auroras (A and B) are oncogenic serine/threonine kinases that play key roles in the mitotic phase of the eukaryotic cell cycle. (elsevierpure.com)
Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
Aurora kinases are found in all organisms in which their function has been conserved throughout evolution, namely the control of chromosome segregation. (lookformedical.com)
Aurora kinases constitute a family of serine-threonine kinases that are strongly associated with cancer. (cogershop.com)
Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers. (xcessbio.com)
TNBC has high mitotic activity, and, because Aurora A and B mitotic kinases drive cell division and are overexpressed in tumors with a high mitotic index, we hypothesized that inhibiting Aurora A and B produces a significant antitumor effect in TNBC. (elsevierpure.com)
Our results demonstrate that combined targeting of EGFR and Aurora kinases represents a therapeutic means to activate cell cycle checkpoints and apoptosis in SCCHN. (oncotarget.com)
The three Aurora mitotic kinases localize to the centrosome during different phases of mitosis. (aurorapathway.com)
Aurora A kinase is one of the serine-threonine kinases that control mitotic and meiosis processes in cells. (edu.pl)
It will also include compounds known to be active on Aurora kinases, e.g. barasertib, alisertib, danusertib [7-8]. (edu.pl)
That SP600125 induces endoreduplication signals, promotes tubulin polymerization, a critical process in cell division, and induces delayed apoptosis in leukemia Aurora kinases cells. (hsp90-inhibitors.com)
We observed that dexamethasone exposure caused upregulation of Aurora kinase and its various downstream effector kinases such as JAK, p38, mTOR, and S6K. (lu.se)

They significantly increase chromosome instability and aneuploidy in a subset of hepatocellular carcinoma, resulting in growth inhibition. (carislifesciences.com)
However, MLN8237 plus docetaxel demonstrated a statistically significant tumor growth inhibition and enhanced survival compared to single agent therapy. (elsevierpure.com)
40-fold more selective inhibitory activity for Aurora A compared with Aurora B. In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. (xcessbio.com)
In the HCT-116 tumor-bearing mice, MLN8054, administered orally at 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, leads to dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg). (xcessbio.com)

Also, cells deficient in topoisomerase II show significantly reduced Aurora B kinase activity. (wikipedia.org)

Localization of Aurora B to the centromere during prometaphase and metaphase requires phosphorylation of the mammalian kinetochore-specific histone-H3 variant centromere protein A (CENP-A). CENP-A associates with the centromere and is necessary for assembly of the kinetochore. (wikipedia.org)
Phosphorylation of CENP-A at serine 7 by Aurora A kinase recruits Aurora B to the centromere. (wikipedia.org)
Furthermore, this compound inhibited phosphorylation of histone H3 (pHH3) in mouse bone morrow upon oral administration, which is consistent with inhibition of Aurora kinase B activity. (rcsb.org)
Phosphorylation of Histone H3 on serine 10, a known Aurora B cellular target, is inhibited with an EC50 of ~9nM following treatment of cells with SNS-314. (cogershop.com)

We observed significant inhibitory activities of KW-2450 on cell viability, apoptosis, colony formation in agar, and mammosphere formation in TNBC cells. (elsevierpure.com)
Inhibition of TTK results in chromosome missegregation and apoptosis of tumour cells. (oncolines.com)

This communication describes the discovery of a novel series of Aurora kinase inhibitors. (rcsb.org)
Several potent Aurora kinase inhibitors derived from 5H-benzo[c][1,8]naphthyridin-6-one scaffold were identified. (rcsb.org)
Tyrosine kinase inhibitors like vandetanib and lenvatinib have shown promising clinical activity in RET -positive tumours, and convincing results were obtained with the next-generation ALK inhibitors ceritinib, alectinib and brigatinib. (memoinoncology.com)
NTRC has developed a series of highly selective inhibitors of TTK enzyme activity that potently inhibit proliferation of human cancer cells and tumour growth in mouse models. (oncolines.com)
Increased target residence time correlated with increased activity of TTK inhibitors in cancer cell line proliferation assays. (oncolines.com)
Different subclasses of PI3K/mTOR, Aurora and EZH2 inhibitors were identified that relate to different mechanisms of activity or different genetic targeting. (oncolines.com)
In the first stage of the project, using molecular docking to find potential Aurora A kinase inhibitors, a group of compounds (mainly of natural origin), showing structural similarities with capsaicin, will be tested. (edu.pl)
Such tests are commonly used in the evaluation of Aurora A inhibitors [9]. (edu.pl)
Although Aurora A kinase is a known protein and numerous experiments have been carried out on it for years, so far no combination of numerical and experimental methods has been used in the study of its inhibitors. (edu.pl)

Chiauranib's [1] highly selective inhibition of Aurora B/VEGFR/PDGFR/c-Kit/CSF1R targets can exert a comprehensive anti-tumor effect by simultaneously inhibiting tumor angiogenesis, inhibiting tumor cell mitosis and regulating tumor microenvironment, it has better animal pharmacodynamic activity and good safety than similar drugs with similar mechanisms. (bla-regulatory.com)

A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)
Enables cyclin-dependent protein serine/threonine kinase regulator activity. (nih.gov)

Specifically, Aurora B localizes to the chromosomes in prophase, the centromere in prometaphase and metaphase, and the central mitotic spindle in anaphase. (wikipedia.org)
Inhibition of Aurora B function by RNA interference or microinjection of blocking antibodies impairs the alignment of chromosomes at the equator of the mitotic spindle. (wikipedia.org)
As ATR is activated at centromeres, it stimulates Aurora B through Chk1, preventing formation of lagging chromosomes. (umn.edu)
Perturbation of their activity leads to multiple defects in mitosis including aberrant centrosome duplication, misalignment of chromosomes, inhibition of cytokinesis, and disruption of the spindle checkpoint. (cogershop.com)

Expression of Aurora B reaches a maximum at the G2-M transition, whereas Aurora B protein is most active during mitosis. (wikipedia.org)
This analysis showed that the association of Aurora B with centromeres is dynamic (Aurora B at the centromere is constantly exchanging with a pool of cytoplasmic Aurora B). The analysis of tagged Aurora B also suggested that it associates with spindle microtubules during anaphase of mitosis and this association significantly limits its mobility. (wikipedia.org)
In topoisomerase II-depleted cells, Aurora B and INCENP do not transfer to the central spindle in late mitosis. (wikipedia.org)
Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. (lookformedical.com)
An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. (lookformedical.com)
Acute inhibition or degradation of ATR in mitosis induces whole-chromosome missegregation. (umn.edu)
In mitosis, ATR localizes to centromeres through Aurora A-regulated association with centromere protein F (CENP-F), allowing ATR to engage replication protein A (RPA)-coated centromeric R loops. (umn.edu)
Aurora A and B are essential in mitosis. (cogershop.com)
however, Aurora C can complement Aurora B kinase activity in mitosis. (cogershop.com)
Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. (xcessbio.com)
Recently, certain cancer chemotherapy agents have been found to exert their anticancer activities by disrupting the dynamics of microtubule assembly, thus perturbing the formation and function of the mitotic spindle apparatus and arresting cells in mitosis. (hsp90-inhibitors.com)

A small molecule with anticancer and antimetastatic activities induces rapid mitochondrial-associated necrosis in breast cancer. (omrf.org)

Analysis of DNA content and indirect immunofluoresence demonstrates that SNS-314 induces defects in cytokinesis and spindle checkpoint that are consistent with Aurora kinase inhibition. (cogershop.com)
In the HCT-116 xenograft-bearing animals, MLN8054 induces DNA and tubulin staining of tumor tissue in nuclear and cell body area, consistent with a senescent phenotype by increasing senescence-associated beta-galactosidase activity. (xcessbio.com)

Alanine transition of S63 and S262 (S63A and S262A) of IκBα induced inhibition of cell proliferation and suppression of p65 transcription activity. (researchsquare.com)
In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. (xcessbio.com)
These results indicate that JNK activity may regulate cell proliferation through the regulation of cell cycles. (hsp90-inhibitors.com)

Intriguingly, EB1 overexpression enhances Aurora B kinase activity, at least in part because EB1 blocks the dephosphorylation/inactivation of Aurora B by protein phosphatase 2A. (wikipedia.org)
Aurora A overexpression in many malignant tumor types suggests that it may be directly involved in NEOPLASTIC CELL TRANSFORMATION. (lookformedical.com)
In human, aurora-A has focused a lot of attention, since its overexpression has been found to be correlated with the grade of various solid tumours. (lookformedical.com)
However, overexpression of aurora-A in particular cell lines such as NIH3T3 is sufficient to induce growth on soft agar. (lookformedical.com)
A luciferase activity assay revealed that the transcriptional activity of the beta-catenin/TCF complex was elevated by AURKA, but decreased by SMAD4 overexpression. (adanabtu.edu.tr)
Capsaicin as a compound with a potential to inhibit Aurora A kinase was selected because capsaicin supplementation had previously been shown to abolish resistance to cisplatin treatment induced by overexpression of Aurora A kinase [4]. (edu.pl)

Demand for the induction of PI3K activity t RAE SST 1 show that MCMV infection activates the PI3K pathway. (microrna1.com)

These phenotypes resembled those of Aurora B knockdown and complete pharmaceutical inhibition of Aurora A. We demonstrated that 8N cells resulting from KW-2450 treatment depended on the activation of mitogen-activated protein kinase kinase (MEK) for their survival. (elsevierpure.com)

Aurora B is a chromosomal passenger protein. (wikipedia.org)

A mouse xenograft model of MCL demonstrated that MLN8237 (10 or 30 mg/kg) or docetaxel (10 mg/kg) alone had modest anti-tumor activity. (elsevierpure.com)
Analysis of SNS-314 treated tumors confirms that the anti-tumor activity is consistent with Aurora kinase inhibition. (cogershop.com)

On the role of aurora-A in centrosome function. (lookformedical.com)

Aurora kinase B is a protein that functions in the attachment of the mitotic spindle to the centromere. (wikipedia.org)
A more detailed analysis of Aurora B localization has been carried out in mammalian cells by tagging Aurora B with green fluorescent protein. (wikipedia.org)
Aurora B has been shown to bind to end-binding protein 1 (EB1), a protein that regulates microtubule dynamics. (wikipedia.org)
Intriguingly, expression of a dominant-negative and catalytically inactive form of Aurora B disrupted microtubule attachment to the kinetochore and prevented the association of dynein and centromere protein E (CENP-E) with kinetochores. (wikipedia.org)
By using a direct in vivo shRNA screen, we show that liver cancer cells that have mutations in the gene encoding the tumor suppressor protein p53 (Trp53 in mice and TP53 in humans) and that are driven by the oncoprotein NRAS become addicted to MYC stabilization via a mechanism mediated by aurora kinase A (AURKA). (scite.ai)
Since Myc is the common downstream protein of both BCR-ABL and AurA, we proposed the combinational effect of AKI603 and imatinib could be caused by inhibition of Myc. (scite.ai)
The kinase inhibition does not alter the viral protein production/secretion or genome replication but impaired the viral yield without altering the percentage of infected cells. (mendeley.com)
The N-terminal region of the protein binds CDC2 to form a complex showing reduced H1 histone kinase activity, indicating a role as a negative regulator of CDC2/cyclin A. In addition, the C-terminal kinase domain binds to its own N-terminal region, suggesting potential negative regulation through interference with complex formation via intramolecular binding. (cancerindex.org)
Patients characterized by elevated EGFR and elevated Aurora-A protein expression in tumor tissue represent a risk group with poor disease-free and overall survival (EGFR low Aurora-A low versus EGFR high Aurora-A high , p=0.024). (oncotarget.com)
Comparing pan-Aurora kinase and Aurora-A targeting hints towards a strong and clinically relevant biological effect mediated via Aurora kinase B. Taken together, our findings characterize a new poor risk group in SCCHN patients defined by elevated EGFR and Aurora-A protein expression. (oncotarget.com)
A substance that inhibits that activity of the Hsp90 heat shock protein. (hsp90-inhibitors.com)

Indirect immunofluorescence showed that Aurora B and EB1 colocalize during anaphase on the central spindle and in the midbody during cytokinesis. (wikipedia.org)

SMAD4 has been suggested to inhibit the activity of the WNT/beta-catenin signaling pathway in cancer. (adanabtu.edu.tr)
Around 40% of AML patients display elevated nuclear NF-κB activity, providing a compelling rationale for targeting the NF-κB pathway in AML. (mdpi.com)

Aurora A kinase (AURKA), which is frequently overexpressed in cancer, increases the transcriptional activity of beta-catenin/T-cell factor (TCF) complex by stabilizing beta-catenin through the inhibition of GSK-3 beta. (adanabtu.edu.tr)
These results indicate that the tumor-suppressive function of SMAD4 is mediated by down regulation of b-catenin transcriptional activity via AURKA degradation in a TGF beta-independent manner. (adanabtu.edu.tr)
We observed that BCL2L13 and PMAIP1 genes get upregulated upon PLK1 inhibition, probably through transcriptional regulation by FOXOs in interaction with β-catenin. (lu.se)

On the other hand, although SP600125 exhibited mineralization inhibition activity, the influence was much weaker as compared to SB202190: SP600125 (20? (mslideas.com)
Some studies have reported that the G2 M arrest induced by SP600125 may be due to inhibition of cyclin B Cdk1 kinase activity through an increase in p21 levels. (hsp90-inhibitors.com)

KYC particularly inhibits the experience of MPO that's released from PMA-activated HL-60 cells however, not NOX activity that's needed for HL-60 cells to create O2? (technumber.com)

The effect of ATR ablation is not due to altered cyclin-dependent kinase 1 (CDK1) activity, DNA damage responses, or unscheduled DNA synthesis but to loss of an ATR function at centromeres. (umn.edu)
Thus, inhibition of JNK activity prevents dissociation between p21 and JNK, and then prevents inhibition of cyclin B Cdk1 activity, leading to induction of G2 M arrest. (hsp90-inhibitors.com)

Additionally, topoisomerase II has been implicated in the regulation of Aurora B localization and enzymatic activity. (wikipedia.org)

C, Berthon A, Drougat L, Kiseljak-Vassiliades K, Wierman ME, Faucz FR, Fa?a VM, Tone LG, Stratakis CA. Inhibition of Aurora kinase A activity enhances the antitumor response of beta-catenin blockade in human adrenocortical cancer cells. (ucdenver.edu)

The researchers found no association between any of the brain activity profiles and other mental health outcomes, such as symptoms of depression, dissociation, or impulsivity. (northdallasgazette.com)
Increased JNK activity is important for the dissociation of p21 and JNK, following which cells enter into the S phases. (hsp90-inhibitors.com)

These results demonstrate a non-redundant function of MLL1 in regulating inner centromere liquid condensates and genome stability via a non-canonical enzymatic activity. (carislifesciences.com)

MLN8054 also shows similar antitumor activity in the PC-3 tumor xenograft in nude mice. (xcessbio.com)

Aurora kinase B localizes to microtubules near kinetochores, specifically to the specialized microtubules called K-fibers, and Aurora kinase A (MIM 603072) localizes to centrosomes (Lampson et al. (wikipedia.org)

Aurora B complexes with three other proteins, Survivin, Borealin and INCENP. (wikipedia.org)

The expression and activity of Aurora B are regulated according to the cell cycle. (wikipedia.org)
Finally, a portion of the tagged Aurora B localized to the equatorial cell cortex, having been transported to this location by astral microtubules. (wikipedia.org)
Methods: Previously we observed that aurora kinase (AURK) binds IκBα in the cell. (researchsquare.com)
Aurora A and B were also found elevated in 13 aggressive B-NHL cell lines. (elsevierpure.com)
Surprisingly, inhibition of AurA by AKI603 induced leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells. (scite.ai)
With this in mind, in paper IV we identified that inhibiting BCL2 by venetoclax synergizes with PLK1 inhibition by volasertib in T-ALL cell lines and PDX models. (lu.se)

Jones D, Noble M, Wedge SR, Robson CN, Gaughan L. Aurora A regulates expression of AR-V7 in models of castrate resistant prostate cancer . (ncl.ac.uk)

INCENP stimulates Aurora B kinase activity. (wikipedia.org)

In contrast, the collagen-binding activity and the ratio of the VWF ristocetin cofactor activity and VWF antigen was significantly decreased when compared with healthy controls. (aurorakinaseb.com)

A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. (xcessbio.com)

4 This glucuronidation is carried out by the UGT enzymes, which leads to inactivation of drug activity, increased water solubility, and elimination of the drug imparted by the conjugation. (haematologica.org)

The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)

Inhibiting MLL1 activity or mutating Borealin K143 to arginine perturbs CPC phase separation, reduces Aurora kinase B activity, and impairs the resolution of erroneous kinetochore-microtubule attachments and sister-chromatid cohesion. (carislifesciences.com)

activity, but not high VWF antigen, was associated with poor outcome in patients with ALI/ALF as evidenced by higher grades of encephalopathy, higher transplantation rates, and lower survival. (aurorakinaseb.com)

Our results showed that AKI603 exhibited strong anti-proliferative activity in leukemic cells. (scite.ai)
We suggest that shared inhibitions between Aurora-B and Cyclin-B regulate the duration of abscission and thus the amount of sister cells in each cyst. (biotech-angels.com)

Anatomy10

Organisms1

Diseases3

Chemicals and Drugs30

Phenomena and Processes21

Information Science2

Inhibitor16

Kinases16

Growth inhibition4

Reduced Aurora B kina1

Phosphorylation4

Apoptosis2

Inhibitors9

Selective1

Serine2

Chromosomes4

Mitosis12

Small molecule1

Induces2

Proliferation3

Overexpression6

PI3K1

Phenotypes1

Chromosomal passenger protein1

Anti-tumor activity2

Centrosome1

Protein11

Cytokinesis1

Pathway2

Transcriptional3

SP6001252

Inhibits1

CDK12

Regulation1

Enhances1

Dissociation2

Enzymatic activity1

Antitumor activity1

Localizes1

Survivin1

Cell6

Regulates1

Stimulates1

Significantly1

Cancer1

Inactivation1

Binds1

Reduces1

Survival1

Cells2