Targets aurora kinase b. Medical search. Frequent questions

Several potent Aurora kinase inhibitors derived from 5H-benzo[c][1,8]naphthyridin-6-one scaffold were identified. (rcsb.org)
Pharmacological response data for targeted inhibitors of SRC, WNT, GSK3b, aurora kinase, PI3 kinase, and mTOR, showed significant differences in sensitivity across cell lines assigned to different subtypes. (tudelft.nl)
Anderson, B.D. Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties. (eurekaselect.com)
Mount Sinai researchers have developed a novel method to identify aggressive early-stage lung cancers and target drugs known as aurora kinase inhibitors to tumors that are especially likely to respond. (bio-itworld.com)
The Mount Sinai team used a genomics network model to measure tumor invasiveness-distinguishing aggressive tumors from so-called "indolent" ones, which often cannot be told apart via chest CT scan-and identify those that will respond to aurora kinase inhibitors, molecules that can inhibit gene signature regulators. (bio-itworld.com)
They identified and tested aurora kinase inhibitors, including AMG900, as an effective treatment to intercept lung cancer progression in the models. (bio-itworld.com)
MicroRNA-106a targets autophagy and enhances sensitivity of lung cancer cells to Src inhibitors. (unibe.ch)
Work done from the Boston group had talked about the aurora kinase amplifications, and we've seen aurora kinase inhibitors such as alisertib that were studied in patients who progressed on CDK4/6 inhibitors. (onclive.com)
Applying "drug target constellation" (DTECT) mapping, we further show that protein levels of TTF1 and cMYC predict response to targeted therapies including aurora kinase, Bcl2, and HSP90 inhibitors. (oncotarget.com)
Kinase inhibitors are now one of the major categories of chemotherapy medicine. (callaix.com)
Over 50 kinase inhibitors are approved in the US for cancer treatment with more under development. (callaix.com)
Of the 69 new drugs approved by the FDA for cancer from 2015 to 2020, 26 were kinase inhibitors. (callaix.com)
Most kinase inhibitors work on tyrosine kinases . (callaix.com)
As oncology drugs, kinase inhibitors were created out of modern genetics- the understanding of DNA, the cell cycle, and molecular signaling pathways- and thus represent a change from general to molecular methods of cancer treatment. (callaix.com)
An article published in the journal Molecular Cancer in 2018 claimed that over 10,000 patents had been filed in the US for kinase inhibitors since 2001. (callaix.com)
Tyrosine kinase inhibitors (TKIs) are a class of chemotherapy medications that inhibit, or block, one or more of the enzyme tyrosine kinases. (callaix.com)
Tyrosine kinase inhibitors treat cancer by correcting this deregulation. (callaix.com)

The mammalian Aurora kinase family contains three serine/threonine kinase members that participate in cell division. (rndsystems.com)
Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. (nih.gov)
The protein encoded by this gene is a putative serine/threonine kinase that localizes to the mitotic apparatus and complexes with cell cycle controller CDC2 kinase in early mitosis. (cancerindex.org)
A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. (lookformedical.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)
A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)
Aurora kinases are serine/threonine kinases that are essential for cell proliferation. (targetmol.com)
Other kinases work on serine or threonine residues. (callaix.com)
These proteins, including Aurora A and B, are serine/threonine kinases that are essential for cell division activities such as spindle construction, chromosome segregation, and cytokinesis. (smadpathway.com)

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)
We herein demonstrated that CADM1 interacts with Hippo pathway core kinases and enhances the phosphorylation of YAP1, and also that the membranous co-expression of CADM1 and LATS2 predicts a favorable prognosis in lung adenocarcinoma. (cancerindex.org)
GR phosphorylation by an Aurora kinase-dependent pathway provides the mechanism explaining the tight coupling GSK1904529A of ligand-independent GR phosphorylation to cell cycle phase because the maximal activity of these kinases occurs in mitosis. (ap26113.com)
Kinases are a class of enzyme that promote phosphorylation. (callaix.com)
Imatinib, for example, blocks a kinase receptor from binding to ATP, preventing the phosphorylation that would benefit the cancerous cell and promote cell division. (callaix.com)
Importantly, one other individual meats directly influence Aurora T localization, and phosphorylation of conserved residues in the C terminus of INCENP greatly raises Aurora B kinase activity. (smadpathway.com)

The identified potential therapeutic targets of HNK (PTTH) included CCND1 , SIRT2 , AURKB , VEGFA , HDAC1 , CASP9 , HSP90AA1 , and HSP90AB1 , which can potentially inhibit the cell cycle of mBCSCs. (hindawi.com)

The Myc protein and proteins that participate in mitosis represent attractive targets for cancer therapy. (nih.gov)
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)
Mitosis is usually a dynamic process controlled by the activity of multiple kinases with attendant modification of proteins facilitating rigid checkpoint control. (ap26113.com)
GSK1904529A Aurora A is found at centrosomes in early mitosis and controls centrosome maturation centriole separation and chromosome alignment (33) whereas accurate targeting of Aurora B to the chromosomes and then to the spindle midzone and midbody is essential for maintaining microtubule/kinetochore attachments and therefore faithful chromosomal segregation (34). (ap26113.com)
Along with Cdk1/cyclin N, members of the Aurora/Ipl1 kinase family are also crucial regulators of mitosis. (smadpathway.com)
Aurora B levels peak in early mitosis and then dramatically decline at mitotic exit. (smadpathway.com)
Remarkably, a current study contradicts these findings, indicating that p97 is needed for the disassociation of Aurora B from chromosomes, which will be in turn a requisite for nuclear envelope reformation at the end of mitosis. (smadpathway.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)

Conversely, during starvation mTORC1 is inhibited and autophagy is induced by AMP-activated protein kinase (AMPK), leading to generation of intracellular nutrients and energy during degradation of non-functional or non-essential organelles or protein aggregates [ 4 , 6 ], in turn contributing to cell survival. (springer.com)

The intersection between the differentially expressed genes (DEGs) and the HNK-targets was determined using a Venn diagram, and the results were analyzed using a protein-protein interaction network, hub gene selection, gene ontology and Kyoto Encyclopedia of Genes and Genomes pathway enrichment analyses, genetic alteration analysis, survival rate, and immune cell infiltration levels. (hindawi.com)
A database to provide information about the known and explored therapeutic protein and nucleic acid targets, the targeted disease, pathway information and the corresponding drugs directed at each of these targets. (idrblab.net)

Aurora A influences centrosome maturation and spindle assembly, while Auroras B and C direct chromosome alignment and segregation. (rndsystems.com)
Works in various organisms have revealed that the kinase is involved in centrosome separation, duplication and maturation as well as in bipolar spindle assembly and stability. (lookformedical.com)

A genomic network model is used to identify aurora kinase inhibitor-sensitive lung tumors, new Illumina Accelerator start-ups are announced, AI algorithms are being used to improve prostate cancer identification and treatment, and a blood-based DNA methylation test can detect liver cancer. (bio-itworld.com)

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)

HNK controls various intracellular signaling pathways involved in cancer, including those related to nuclear factor kappa B (NF- B), signal transducers and activators of transcription 3 (STAT3), epidermal growth factor receptor (EGFR), and mammalian targets of rapamycin (mTOR) [ 12 ]. (hindawi.com)

The mix of induced pluripotent stem (iPS) cell technology and targeted gene adjustment by homologous recombination (HR) represents a promising new method of generate genetically corrected patient-derived cells that might be useful for autologous transplantation therapies. (biomasswars.com)
Gene symbols, accession ids and various other target identifiers. (nih.gov)
Total count of NCBI Gene Reference Into Function hits for target listed in parenthesis, and summary table with links to publications per PMID with the specific text in article that includes the reported target. (nih.gov)
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)
Using a mouse model of TSC in which the gene was conditionally targeted in most developing neurons and glial cells of the CNS (brains (9), with no switch in the downstream polyamine metabolites spermidine or spermine. (ubatubasat.com)

Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. (lookformedical.com)

Receptor Tyrosine Kinases (RTKs) are a family of tyrosine protein kinases. (callaix.com)
There are three primary growth factors that relate to tyrosine kinase. (callaix.com)
Crystallization and Structural Determination of ABLT315I:AP24534 The kinase domain of murine ABLT315I was coexpressed with YopH protein tyrosine phosphatase in E. coli as described previously and purified in the clear presence of AP24534 to near homogeneity using metal affinity, Mono Q, and measurement exclusion chroma tography. (smadpathway.com)
Alert FDA Approves Bosutinib for Children With CML The agency approved the tyrosine kinase inhibitor for pediatric patients with chronic phase Ph+ chronic myelogenous leukemia that is newly diagnosed or resistant or intolerant to prior therapy. (medscape.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)

TC-A 2317 hydrochloride is an inhibitor of Aurora kinase A with a Ki of 1.2 nM compared to Aurora kinase B with a Ki of 101 nM. (targetmol.com)

We analyzed the clinical data and performed immunohistochemistry for Epidermal growth factor receptor (EGFR) and Aurora kinase A (Aurora-A) expression in 180 SCCHN patients. (oncotarget.com)
Importance Aurora A kinase (AURKA) activation, related in part to AURKA amplification and variants, is associated with downregulation of estrogen receptor (ER) α expression, endocrine resistance, and implicated in cyclin-dependent kinase 4/6 inhibitor (CDK 4/6i) resistance. (kanker-actueel.nl)
The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (lookformedical.com)
The spike (S) protein of SARS-CoV-2, which mediates receptor binding and subsequent membrane fusion to promote viral entry, is a major target for current drug development and vaccine design. (bvsalud.org)

But if we could stratify patients and include people with all levels of frailty, we could broaden inclusion and hopefully develop a greater number of targeted therapies, he added. (genomeweb.com)
To tailor CRC treatment, it is essential to first model this heterogeneity by defining subtypes of patients with homogeneous biological and clinical characteristics and second match these subtypes to cell lines for which extensive pharmacological data is available, thus linking targeted therapies to patients most likely to respond to treatment. (tudelft.nl)
By matching the identified subtypes to cell line panels that have been pharmacologically characterized, it opens up new possibilities for the development and application of targeted therapies for defined CRC patient sub-populations. (tudelft.nl)

While Aurora A localizes to mitotic centrosomes and is required for centrosome growth and the development of a functional bipolar mitotic spindle, Aurora W is the catalytic core of the highly conserved genetic individual complex. (smadpathway.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)
We're working on all these mechanisms, and we're trying to understand how we can use the acquired mechanisms of resistance as a way of a target for newer targeted therapy. (onclive.com)
Since molecular mechanisms of AI resistance are largely undisclosed, the development of cell lines resistant to the non-steroidal AI anastrozole allows the study of the molecular basis for resistance to AIs to unravel new targets for treatment. (ximbio.com)
Tubulin isotypes are known to regulate microtubule stability and dynamics, as well as to play a role in the development of resistance to microtubule-targeted cancer drugs. (bvsalud.org)

Molecular docking and molecular dynamics simulations further confirmed the relationship between compounds and target proteins. (bvsalud.org)
Preeminent among these proteins are the cyclin dependent kinases, which upon binding to cyclins, phosphorylate numerous targets to trigger cell cycle progression. (smadpathway.com)

Conversely, the deubiquitinating enzyme hFAM was required for the disassociation of Survivin and Aurora B from anaphase chromosomes. (smadpathway.com)

HSP90AA1 Aurora kinases are grasp regulators of both centrosome and checkpoint control function. (ap26113.com)

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. (idrblab.net)
LY3295668 is a selective inhibitor of Aurora A with Kis of 0.8 nM and 1038 nM for Aurora A and B, respectively. (targetmol.com)

Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1. (targetmol.com)

The BRAF V600E mutation may be a potential prognostic factor and therapeutic target for breast cancer. (karger.com)
The term "oncotarget" encompasses all molecules, pathways, cellular functions, cell types, and even tissues that can be viewed as targets relevant to cancer as well as other diseases. (oncotarget.com)
Findings In this phase 2 randomized clinical trial of 91 patients with endocrine-resistant, metastatic breast cancer who were previously treated with a cyclin-dependent kinase 4/6 inhibitor, participants were randomized to receive treatment with alisertib alone or combined with fulvestrant. (kanker-actueel.nl)
Meaning The trial results found that while alisertib did not restore fulvestrant sensitivity and increase ORRs, promising clinical activity was observed with alisertib monotherapy among patients with endocrine-resistant and cyclin-dependent kinase 4/6 inhibitor-resistant metastatic breast cancer. (kanker-actueel.nl)
Chemotherapeutic drugs target a physiological differentiating feature of cancer cells because they have a tendency to actively proliferate a lot more than regular cells. (biomasswars.com)
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)
To identify and validate signal transduction pathways and molecular targets that are disregulated in cancer cells. (moffitt.org)
The observations that (1) is usually a transcriptional target of proto-oncogene (14), (2) polyamines are involved in cell growth and proliferation and (3) polyamines are upregulated in malignancies have made them a focus of cancer research (15). (ubatubasat.com)
Aurora kinase A and B as new treatment targets in aromatase inhibitor-resistant breast cancer cells. (ximbio.com)
Kinase deregulation can contribute to the growth of cancer. (callaix.com)
The first kinase inhibitor introduced for cancer was imatinib, which the FDA approved in 2001. (callaix.com)
Scientists are looking the possibility of kinase inhibition for other diseases including hypertension and Parkinson's disease but here we focus on cancer medicines. (callaix.com)
The CPC includes, as well as Aurora B, three regulatory subunits: the inner centromeric protein, Survivin, and Borealin/Dasra W. Beginning in prophase, the CPC localizes to condensing chromosomes and steadily concentrates at the internal centromere where one function would be to correct poor Infectious causes of cancer spindle kinetochore devices. (smadpathway.com)

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)
Combined Aurora kinase and EGFR targeting using a monoclonal anti-EGFR antibody was more effective compared to single EGFR and Aurora kinase inhibition. (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)

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

The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (idrblab.net)

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)

AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I). (targetmol.com)
Fragment-Based Discovery of the Pyrazol-4-yl urea (AT9283), a Multi-targeted Kinase Inhibitor with Potent Aurora Kinase Activity. (astx.com)

De aurora A-kinaseremmer alisertib in combinatie met fulvestrant geeft geen extra voordeel in vergelijking met Alisertib alleen bij patiënten met hormoonresistente gevorderde borstkanker . (kanker-actueel.nl)
Uit de onderzoeksresultaten bleek wel dat in de groep die alleen alisertib als medicijn kreeg veelbelovende klinische activiteit werd waargenomen bij patiënten met hormoonresistente en cycline-afhankelijke kinase 4/6-remmer-resistente gemetastaseerde borstkanker. (kanker-actueel.nl)
Vraag: Herstelt behandeling met alisertib de gevoeligheid voor fulvestrant en verbetert het de tumor objectieve response rates (ORR's) in vergelijking met alisertib monotherapie bij patiënten met hormoonresistente gemetastaseerde borstkanker? (kanker-actueel.nl)
In deze gerandomiseerde klinische fase 2-studie met 91 patiënten met hormoonresistente, gemetastaseerde borstkanker die eerder waren behandeld met een cycline-afhankelijke kinase 4/6-remmer, werden de deelnemers gerandomiseerd ingedeeld om een behandeling met alleen alisertib of gecombineerd met fulvestrant te krijgen. (kanker-actueel.nl)
Uit de onderzoeksresultaten bleek dat hoewel alisertib de fulvestrantgevoeligheid niet herstelde en de ORR's niet verhoogde, veelbelovende klinische activiteit werd waargenomen met alisertib-monotherapie bij patiënten met hormoonresistente en cycline-afhankelijke kinase 4/6-remmer-resistente gemetastaseerde borstkanker. (kanker-actueel.nl)

Aurora A overexpression in many malignant tumor types suggests that it may be directly involved in NEOPLASTIC CELL TRANSFORMATION. (lookformedical.com)
Drugs given to stop kinases can slow the proliferation of malignant cells and angiogenesis (growth of blood vessels). (callaix.com)

M any kinase inhibitor compounds have been found. (callaix.com)

This study aimed to explore the potential targets and molecular mechanisms of HNK on metastatic BCSC (mBCSC)-cell cycle arrest and the impact of the TME. (hindawi.com)

Advanced head and neck squamous cell carcinoma (HNSCC) is treated with radiotherapy, chemotherapy, targeted therapy or a combination of these treatments. (researchsquare.com)
Finally, the interaction between HNK and two HNK-targets regulating the cell cycle was analyzed using molecular docking analysis. (hindawi.com)
By applying this stratification to several CRC cell line panels and integrating pharmacological response data, we generated hypotheses regarding the targeted treatment of different subtypes. (tudelft.nl)
However, overexpression of aurora-A in particular cell lines such as NIH3T3 is sufficient to induce growth on soft agar. (lookformedical.com)
Key components supplier CX-4945 of these paths are protein kinases that are critical for the appropriate time of each cell cycle stage. (smadpathway.com)

Using bioinformatics analyses, we predicted HNK protein targets from several databases and retrieved the genes differentially expressed in mBCSCs from the GEO database. (hindawi.com)

This newly formed entity leverages years of industry expertise, scientific excellence, and proprietary technology to discover the best antibody candidate for therapeutic targets of interest. (biotechnology.report)
Twist Biopharma Solutions offers an end-to-end workflow for centralized antibody discovery and optimization, including target validation, hit generation, lead selection, lead optimization, and lead characterization. (biotechnology.report)
Alert FDA Approves New Drug for Generalized Myasthenia Gravis Zilucoplan is the first once-daily, subcutaneous, self-administered, targeted C5 complement inhibitor for adults with gMG who are AChR antibody positive. (medscape.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)

The research team used a genetically engineered mouse model to define the role of aurora kinases in early progression of the disease. (bio-itworld.com)

This "on/off" process can become disrupted, often by a mutated kinase, and actions can become unregulated. (callaix.com)

Classes for this protein according to by Drug Target Ontology (DTO). (nih.gov)

These findings suggest Myc as a potential therapeutic target for HB. (scite.ai)
Findings were categorized by type of treatment (radiotherapy, chemotherapy, targeted therapy, or combination therapy). (researchsquare.com)

Hence, this study concluded that p97/Ufd1/Npl4 is just a positive regulator of the CPC, as it is necessary for the localization of Aurora and Survivin W to metaphase centromeres. (smadpathway.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)

Anatomy7

Diseases2

Chemicals and Drugs49

Analytical, Diagnostic and Therapeutic Techniques and Equipment1

Phenomena and Processes18

Information Science2

Inhibitors17

Serine10

Phosphorylation6

Aurkb1

Mitosis9

Cytokinesis1

Autophagy1

Pathway2

Spindle assembly2

Lung tumors1

Mechanism1

Mammalian1

Gene5

Polyploidy1

Tyrosine4

Apoptosis1

2317 hydrochloride1

Receptor4

Therapies3

Highly conserved1

Resistance4

Proteins2

Enzyme1

Regulators1

Selective inhibitor2

Inhibits1

Cancer13

EGFR3

Centrosome1

20161

Potent and selective1

AT92832

Alisertib5

Malignant2

Compounds1

Metastatic1

Cell5

Protein targets1

Antibody3

Cyclin1

Progression1

Actions1

Ontology1

Findings2

Regulator1

Chromosome segregation1