Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. It is found primarily in GERM CELLS in the TESTIS, and may mediate CHROMOSOME SEGREGATION during SPERMATOGENESIS.
A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. They are involved in many aspects of cell division, including centrosome duplication, SPINDLE APPARATUS formation, chromosome alignment, attachment to the spindle, checkpoint activation, and CYTOKINESIS.
An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. Aurora A overexpression in many malignant tumor types suggests that it may be directly involved in NEOPLASTIC CELL TRANSFORMATION.
An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. It mediates proper CHROMOSOME SEGREGATION and contractile ring function during CYTOKINESIS.
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. 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.
A group of enzymes that catalyzes the phosphorylation of serine or threonine residues in proteins, with ATP or other nucleotides as phosphate donors.
A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.
Databases containing information about PROTEINS such as AMINO ACID SEQUENCE; PROTEIN CONFORMATION; and other properties.
The portion of an interactive computer program that issues messages to and receives commands from a user.
5'-Adenylic acid, monoanhydride with imidodiphosphoric acid. An analog of ATP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It is a potent competitive inhibitor of soluble and membrane-bound mitochondrial ATPase and also inhibits ATP-dependent reactions of oxidative phosphorylation.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Large multiprotein complexes that bind the centromeres of the chromosomes to the microtubules of the mitotic spindle during metaphase in the cell cycle.
Agents which affect CELL DIVISION and the MITOTIC SPINDLE APPARATUS resulting in the loss or gain of whole CHROMOSOMES, thereby inducing an ANEUPLOIDY.
Agents that inhibit PROTEIN KINASES.
A province of eastern Canada. Its capital is Quebec. The region belonged to France from 1627 to 1763 when it was lost to the British. The name is from the Algonquian quilibek meaning the place where waters narrow, referring to the gradually narrowing channel of the St. Lawrence or to the narrows of the river at Cape Diamond. (From Webster's New Geographical Dictionary, 1988, p993 & Room, Brewer's Dictionary of Names, 1992, p440)
Large collections of small molecules (molecular weight about 600 or less), of similar or diverse nature which are used for high-throughput screening analysis of the gene function, protein interaction, cellular processing, biochemical pathways, or other chemical interactions.
The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.
Circadian rhythm signaling proteins that influence circadian clock by interacting with other circadian regulatory proteins and transporting them into the CELL NUCLEUS.
A subspecialty of internal medicine concerned with the study of neoplasms.
A gene silencing phenomenon whereby specific dsRNAs (RNA, DOUBLE-STRANDED) trigger the degradation of homologous mRNA (RNA, MESSENGER). The specific dsRNAs are processed into SMALL INTERFERING RNA (siRNA) which serves as a guide for cleavage of the homologous mRNA in the RNA-INDUCED SILENCING COMPLEX. DNA METHYLATION may also be triggered during this process.
A cluster of metabolic risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome X include excess ABDOMINAL FAT; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state. (from AHA/NHLBI/ADA Conference Proceedings, Circulation 2004; 109:551-556)
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Body of knowledge related to the use of organisms, cells or cell-derived constituents for the purpose of developing products which are technically, scientifically and clinically useful. Alteration of biologic function at the molecular level (i.e., GENETIC ENGINEERING) is a central focus; laboratory methods used include TRANSFECTION and CLONING technologies, sequence and structure analysis algorithms, computer databases, and gene and protein structure function analysis and prediction.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The combining of administrative and organizational resources of two or more health care facilities.

The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (1/30)

Our previous studies showed that Aie1 (aurora-C), is a novel testis kinase belonging to the aurora kinase family (). In this report, we describe a testis zinc finger protein (Tzfp) that binds to the upstream flanking sequence of the Aie1 gene. The mouse Tzfp gene, mapped to chromosome 7 B2-B3, encodes a 465-amino acid transcription factor containing a conserved N-terminal BTB/POZ domain and three C-terminal PLZF-like C(2)H(2) zinc fingers. The zinc finger domain of Tzfp binds to the TGTACAGTGT motif (Tzfp binding site, termed tbs) located at the upstream flanking sequence of the Aie1 gene by gel mobility shift, DNase I footprinting, and competition analyses. When the C-terminal zinc fingers of Tzfp were fused to the transactivation domain of VP16, the chimera activated transcription of a reporter construct containing multiple copies of the tbs. In contrast, the same chimera did not activate the reporter gene when an essential nucleotide fifth C was mutated to A at the tbs. Furthermore, we showed that the N-terminal BTB/POZ domain of TZFP has a repressor activity. Taken together, our results indicate that Tzfp recognizes a sequence-specific motif (tbs) and may play a role in the regulation of the genes carrying the tbs.  (+info)

On the role of aurora-A in centrosome function. (2/30)

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. 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. Aurora kinases are found in all organisms in which their function has been conserved throughout evolution, namely the control of chromosome segregation. 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. Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. However, overexpression of aurora-A in particular cell lines such as NIH3T3 is sufficient to induce growth on soft agar. Those transformed cells form tumours when implanted in immunodeficient mice, indicating that the kinase is an oncogene.  (+info)

Direct association with inner centromere protein (INCENP) activates the novel chromosomal passenger protein, Aurora-C. (3/30)

A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. The human Aurora paralogues Aurora-A, Aurora-B, and Aurora-C have a highly conserved catalytic domain. Extensive studies on the role of Aurora-A and Aurora-B have revealed distinct localizations and functions in regulating mitotic processes, whereas little is known about Aurora-C. The present study shows that human Aurora-C is a chromosomal passenger protein that forms complexes with Aurora-B and inner centromere protein (INCENP), which are known passenger proteins. We show that INCENP binds and activates Aurora-C in vivo and in vitro. Furthermore, Aurora-C co-expressed with INCENP elicits the phosphorylation of endogenous histone H3 in mammalian cells, even though this phosphorylation is not sufficient to establish chromosome condensation in interphase cells. We therefore suggest that Aurora-C is a novel chromosomal passenger protein that cooperates with Aurora-B to regulate mitotic chromosome dynamics in mammalian cells.  (+info)

Evolutionary relationships of Aurora kinases: implications for model organism studies and the development of anti-cancer drugs. (4/30)

BACKGROUND: As key regulators of mitotic chromosome segregation, the Aurora family of serine/threonine kinases play an important role in cell division. Abnormalities in Aurora kinases have been strongly linked with cancer, which has lead to the recent development of new classes of anti-cancer drugs that specifically target the ATP-binding domain of these kinases. From an evolutionary perspective, the species distribution of the Aurora kinase family is complex. Mammals uniquely have three Aurora kinases, Aurora-A, Aurora-B, and Aurora-C, while for other metazoans, including the frog, fruitfly and nematode, only Aurora-A and Aurora-B kinases are known. The fungi have a single Aurora-like homolog. Based on the tacit assumption of orthology to human counterparts, model organism studies have been central to the functional characterization of Aurora kinases. However, the ortholog and paralog relationships of these kinases across various species have not been rigorously examined. Here, we present comprehensive evolutionary analyses of the Aurora kinase family. RESULTS: Phylogenetic trees suggest that all three vertebrate Auroras evolved from a single urochordate ancestor. Specifically, Aurora-A is an orthologous lineage in cold-blooded vertebrates and mammals, while structurally similar Aurora-B and Aurora-C evolved more recently in mammals from a duplication of an ancestral Aurora-B/C gene found in cold-blooded vertebrates. All so-called Aurora-A and Aurora-B kinases of non-chordates are ancestral to the clade of chordate Auroras and, therefore, are not strictly orthologous to vertebrate counterparts. Comparisons of human Aurora-B and Aurora-C sequences to the resolved 3D structure of human Aurora-A lends further support to the evolutionary scenario that vertebrate Aurora-B and Aurora-C are closely related paralogs. Of the 26 residues lining the ATP-binding active site, only three were variant and all were specific to Aurora-A. CONCLUSIONS: In this study, we found that invertebrate Aurora-A and Aurora-B kinases are highly divergent protein families from their chordate counterparts. Furthermore, while the Aurora-A family is ubiquitous among all vertebrates, the Aurora-B and Aurora-C families in humans arose from a gene duplication event in mammals. These findings show the importance of understanding evolutionary relationships in the interpretation and transference of knowledge from studies of model organism systems to human cellular biology. In addition, given the important role of Aurora kinases in cancer, evolutionary analysis and comparisons of ATP-binding domains suggest a rationale for designing dual action anti-tumor drugs that inhibit both Aurora-B and Aurora-C kinases.  (+info)

Identification of V23RalA-Ser194 as a critical mediator for Aurora-A-induced cellular motility and transformation by small pool expression screening. (5/30)

Human Aurora kinases have three gene family members: Aurora-A, Aurora-B, and Aurora-C. It is not yet established what the specificity of these kinases are and what signals relayed by their reactions. Therefore, we employed small pool expression screening to search for downstream substrates of Aurora-A. Interestingly, all of the identified Aurora-A substrates were resistant to serve as substrates for Aurora-B or Aurora-C, suggesting that these Aurora family members may have distinct substrate specificity for propagation of diverse signaling pathways, even though they share a conserved catalytic kinase domain. Of the candidate substrates, Aurora-A could increase the functional activity of RalA. Mutational analysis revealed that RalA-Ser194 was the phosphorylation site for Aurora-A. Ectopic expression of V23RalA-WT could enhance collagen I-induced cell migration and anchorage-independent growth in Madin-Darby canine kidney (MDCK) Aurora-A stable cell lines. In contrast, overexpression of V23RalA-S194A in MDCK Aurora-A-stable cell lines abolished the intrinsic migration and transformation abilities of Aurora-A. To our knowledge, this is the first systematic search for the downstream substrates of Aurora-A kinase. Moreover, these results support the notion that Aurora-A may act in concert with V23RalA through protein phosphorylation on Ser194 to promote collagen I-induced cell motility and anchorage-independent growth in MDCK epithelial cells.  (+info)

The absence of p53 aggravates polyploidy and centrosome number abnormality induced by Aurora-C overexpression. (6/30)

Aurora-C is the third member of the aurora serine/threonine kinase family and was found only in mammals. Because Aurora-C is overexpressed in many different types of cancer cells we decided to analyze the consequences of Aurora-C overexpression in human cells. We first investigated the subcellular localization of overexpressed GFP-Aurora-C in mitosis and interphase in HeLa cells. As expected, during mitosis, we found that Aurora-C mimics Aurora-B. Surprisingly, in few interphase cells, we found that Aurora-C localized to the centrosome, like Aurora-A. We then examined the phenotype generated by Aurora-C overexpression. Basically it looked similar to the phenotypes observed after overexpression of the other Aurora kinases. We observed an augmentation of polyploid cells containing more than two centrosomes. More interestingly this phenotype was aggravated in the absence of a functional p53. Although the physiological function of Aurora-C in somatic cells remains to be clarified, our results, just like for the two other Aurora kinases, raised the question of a role of Aurora-C in the development and progression of cancer especially in the presence of mutated p53.  (+info)

Dynamic localization and functional implications of Aurora-C kinase during male mouse meiosis. (7/30)

Aurora-C was first identified during screening for kinases expressed in mouse sperm and eggs. Herein, we report for the first time the precise subcellular localization of endogenous Aurora-C during male meiotic division. The localization of Aurora-C was analyzed by immunofluorescence staining on chromosome spreads of mouse spermatocytes or in squashed seminiferous tubules. Aurora-C was first detected at clusters of chromocenters in diplotene spermatocytes and was concentrated at centromeres in metaphase I and II. Interestingly, Aurora-C was also found along the chromosome axes, including both the regions of centromeres and the chromosome arms in diakinesis. During the anaphase I/telophase I and anaphase II/telophase II transitions, Aurora-C was relocalized to the spindle midzone and midbody. A similar distribution pattern was also observed for Aurora-B during male meiotic divisions. Surprisingly, we detected no Aurora-C in mitotic spermatogonia. Furthermore, immunoprecipitation analyses revealed that INCENP associated with Aurora-C in the male testis. We propose that INCENP recruits Aurora-C (or some other factor(s) recruit INCENP and Aurora-C) to meiotic chromosomes, while Aurora-C may either work alone or cooperate with Aurora-B to regulate chromosome segregation during male meiosis.  (+info)

The human cumulus--oocyte complex gene-expression profile. (8/30)

BACKGROUND: The understanding of the mechanisms regulating human oocyte maturation is still rudimentary. We have identified transcripts differentially expressed between immature and mature oocytes and cumulus cells. METHODS: Using oligonucleotide microarrays, genome-wide gene expression was studied in pooled immature and mature oocytes or cumulus cells from patients who underwent IVF. RESULTS: In addition to known genes, such as DAZL, BMP15 or GDF9, oocytes up-regulated 1514 genes. We show that PTTG3 and AURKC are respectively the securin and the Aurora kinase preferentially expressed during oocyte meiosis. Strikingly, oocytes overexpressed previously unreported growth factors such as TNFSF13/APRIL, FGF9, FGF14 and IL4 and transcription factors including OTX2, SOX15 and SOX30. Conversely, cumulus cells, in addition to known genes such as LHCGR or BMPR2, overexpressed cell-to-cell signalling genes including TNFSF11/RANKL, numerous complement components, semaphorins (SEMA3A, SEMA6A and SEMA6D) and CD genes such as CD200. We also identified 52 genes progressively increasing during oocyte maturation, including CDC25A and SOCS7. CONCLUSION: The identification of genes that were up- and down-regulated during oocyte maturation greatly improves our understanding of oocyte biology and will provide new markers that signal viable and competent oocytes. Furthermore, genes found expressed in cumulus cells are potential markers of granulosa cell tumours.  (+info)

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Aurora C kinase is an essential regulator of cytokinesis seeing that it stabilizes the intercellular channel within the midbody to ensure proper chromosomal segregation during cell department. tetraploidy, mitotic criminal arrest, and apoptosis of tumorigenic cells and inhibiting tumor formation in athymic naked rodents profoundly. These findings suggest molecular interaction between Aurora C and calmodulin in telophase and recommend that calmodulin serves as a gate sensor for chromosomal segregation PF-03814735 mistakes during mitosis. rodents/group with medication focus at 2 Meters (low), 10 Meters (moderate) and 40 Meters (high) in the consuming … Debate Lately, Steigemann et al. suggested an elegant model by which Aurora C is normally the essential regulator of abscission time, which responds to chromosome connection development by slowing down abscission to stabilize the intercellular channel until the chromosome connection is normally solved.12 In quality, a indication is provided by ...
Supplementary MaterialsSupplementary material 1 (AVI 412 kb) 13238_2017_407_MOESM1_ESM. regulators of mitosis. Aurora kinase B (AurkB) is usually ubiquitously expressed while Aurora kinase C (AurkC) is usually specifically expressed in gametes and preimplantation embryos. Decitabine price We found that increasing AurkC level in one blastomere of the 2-cell embryo accelerated cell division and decreasing AurkC level slowed down mitosis. Changing AurkB level experienced the opposite effect. The kinase domains of AurkB and AurkC were responsible for their different ability to phosphorylate Histone H3 Serine 10 (H3S10P) and regulate metaphase timing. Using an Oct4-photoactivatable GFP fusion protein (Oct4-paGFP) and fluorescence decay after photoactivation assay, we found that AurkB overexpression reduced Oct4 retention in the nucleus. Finally, we show that blastomeres with higher AurkC level elevated pluripotency gene expression, which were inclined to enter the inner cell mass lineage and ...
Supplementary MaterialsSupplementary material 1 (AVI 412 kb) 13238_2017_407_MOESM1_ESM. regulators of mitosis. Aurora kinase B (AurkB) is usually ubiquitously expressed while Aurora kinase C (AurkC) is usually specifically expressed in gametes and preimplantation embryos. Decitabine price We found that increasing AurkC level in one blastomere of the 2-cell embryo accelerated cell division and decreasing AurkC level slowed down mitosis. Changing AurkB level experienced the opposite effect. The kinase domains of AurkB and AurkC were responsible for their different ability to phosphorylate Histone H3 Serine 10 (H3S10P) and regulate metaphase timing. Using an Oct4-photoactivatable GFP fusion protein (Oct4-paGFP) and fluorescence decay after photoactivation assay, we found that AurkB overexpression reduced Oct4 retention in the nucleus. Finally, we show that blastomeres with higher AurkC level elevated pluripotency gene expression, which were inclined to enter the inner cell mass lineage and ...
Human AURKC (NP_002392.2, 1 a.a. - 275 a.a.) full-length recombinant protein with GST tag expressed in Baculovirus infected Sf21 cells. (P5686) - Products - Abnova
Novel inhibitor of Ark1, the fission yeast member of the conserved Aurora kinase family; High Quality Biochemicals for Research Uses
Plasmid AURKB A4.1 gRNA from Dr. Iain Cheesemans lab contains the insert AURKB (Guide Designation A4.1) and is published in Dev Cell. 2017 Feb 27;40(4):405-420.e2. doi: 10.1016/j.devcel.2017.01.012. Epub 2017 Feb 16. This plasmid is available through Addgene.
5648 The Aurora family of serine/threonine kinases (Aurora A, Aurora B, and Aurora C) plays a key role in cells orderly progression through mitosis. Elevated expression levels of Aurora kinases have been detected in a high percentage of melanoma, colon, breast, ovarian, gastric, and pancreatic tumors, and in a subset of these tumors the AURKA locus (20q13) is amplified. SNS-314, a novel aminothiazole-derived urea, is a selective inhibitor of Aurora kinases A, B, and C with IC50 values in the low nanomolar range. SNS-314 potently inhibits cell proliferation and induces polyploidy (, 4N DNA) in a diverse panel of human cancer cell lines. In the present study we investigated the pharmacodynamic effects and in vivo activity of SNS-314 in human tumor xenograft models. SNS-314 displayed potent anti-tumor activity in HCT-116 (colon), PC-3 (prostate), CALU-6 (NSCLC) and MDA-MB-231 (breast) models. Tumor growth inhibition in these xenograft models ranged from 67.5 to 96.6% on a bi-weekly administration ...
SPGF5 (AURKC) Test Cost INR 30000.00 Surat Pune Jaipur Lucknow Kanpur Nagpur Visakhapatnam Indore Thane Bhopal Patna Vadodara Ghaziabad Ludhiana Coimbatore Madurai Meerut Ranchi Allahabad Trivandrum Pondicherry Mysore Aligarh best offer discount price
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Recombinant full-length human Aurora B was expressed by baculovirus in Sf9 cells using an N-terminal GST tag. Aurora B is a member of the Aurora kinase family that associates with microtubules during chromosome movement and segregation.
Cell division is regulated by protein kinases of the Cdk, Polo, and Aurora families. Although it has long been established that temporal control is central to the coordinated action of these kinases, the importance of spatial regulation has only recently been appreciated and is still poorly understo …
Rabbit ,200 µg/ml of Ab Purified from Bioreactor Concentrate by Protein A/G. Prepared in 10mM PBS with 0.05% BSA & 0.05% azide. Also available WITHOUT BSA & azide at 1.0mg/ml.AB2, 36-3502
Recently, Aurora kinases (A, B, and C/serine threonine kinases) gained much attention due to their implication in several types of cancers. Aurora kinases are involved in multiple functions in mitosis. Aurora A is involved in mitotic entry, separation of centriole pairs, accurate bipolar spindle assembly, alignment of metaphase chromosomes and completion of cytokinesis. Aurora B is a chromosomal passenger protein involved in the regulation of chromosomal orientation, and regulating the association between kinetochores and microtubules, and cytokinesis. Aurora C exhibits similar functions to those assigned to Aurora B and is required for cytokinesis. The above mentioned functions are directly involved in maintaining genomic stability. The relation between Aurora kinases overexpression and transformation has been reported in many cancers. Aurora A was shown to overexpress in colorectal, renal, melanoma, and breast cancers. Mainly Aurora B was shown to overexpress in colorectal cancer. Aurora B was ...
Aurora kinases are serine/threonine kinases that are essential for cell proliferation. Aurora kinase helps the dividing cell dispense its genetic materials to its daughter cells. Defects in this segregation can cause genetic instability, a condition which is highly associated with tumorigenesis. Three Aurora kinases have been identified in mammalian cells to date, Aurora A, Aurora B, Aurora C. Besides being implicated as mitotic regulators, these three kinases have generated significant interest in the cancer research field due to their elevated expression profiles in many human cancers.
Aurora B kinase is a protein that functions in the attachment of the mitotic spindle to the centromere. Chromosomal segregation during mitosis as well as meiosis is regulated by kinases and phosphatases. The Aurora kinases associate with microtubules during chromosome movement and segregation. 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., 2004).[supplied by OMIM] In cancerous cells, over-expression of these enzymes causes unequal distribution of genetic information, creating aneuploid cells, a hallmark of cancer. In 1998, Aurora kinase B was identified in humans by a polymerase chain reaction screen for kinases that are overexpressed in cancers. In the same year, rat Aurora kinase B was identified in a screen designed to find kinases that altered S. cerevisiae proliferation when overexpressed. The expression and activity of Aurora B are regulated ...
Aurora kinases play distinct roles during mitosis, with Aurora A being essential for centrosome maturation and spindle assembly and Aurora B functioning at kinetochores in chromosome attachment and at the end of mitosis in cytokinesis (reviewed in refs. 3, 4).. Inhibition of Aurora kinases is emerging as a new strategy for anticancer therapy, and several small-molecule inhibitors have entered clinical trials. In this report, we describe the biochemical and pharmacologic activity profile of PHA-739358, a spectrum-selective small-molecule kinase inhibitor, which was identified during a screen for inhibitors of Aurora kinases. In most of the cell lines tested, cells fail to divide, resulting in polyploidy without a strong impact on the timing of mitosis (data not shown) and finally leading to a reduction in viability. In some cell lines, an increased apoptosis was seen. This speaks for a dominant Aurora B kinase-related mechanism of action for inhibition because Aurora A inhibition would rather ...
Aurora kinases play distinct roles during mitosis, with Aurora A being essential for centrosome maturation and spindle assembly and Aurora B functioning at kinetochores in chromosome attachment and at the end of mitosis in cytokinesis (reviewed in refs. 3, 4).. Inhibition of Aurora kinases is emerging as a new strategy for anticancer therapy, and several small-molecule inhibitors have entered clinical trials. In this report, we describe the biochemical and pharmacologic activity profile of PHA-739358, a spectrum-selective small-molecule kinase inhibitor, which was identified during a screen for inhibitors of Aurora kinases. In most of the cell lines tested, cells fail to divide, resulting in polyploidy without a strong impact on the timing of mitosis (data not shown) and finally leading to a reduction in viability. In some cell lines, an increased apoptosis was seen. This speaks for a dominant Aurora B kinase-related mechanism of action for inhibition because Aurora A inhibition would rather ...
Background: Aurora kinases are promising targets for cancer chemotherapy. Many reports have been published that some cancers overexpress Aurora kinases, which correlates with tumor grade and poor prognosis. Hence Aurora kinases were considered key genes for cancerogenesis and progression. Many Aurora kinase inhibitors(AKI,s) are in various phases of pre-clinical and clinical development and promising anticancer effects have been reported. Tumor resistance remains one of the major problems in chemotherapy.. Objectives: Our work is mainly aimed at identification of potential resistance mechanisms towards CYC116 (new small molecule pan Aurora kinase inhibitor) and ZM447439. The main aims include generation and selection of resistant tumor cell clones, characterization of resistance, cross resistance with other AKI,s and multidrug resistance. Further characterization of the resistant clones included cell cycle analysis, expression and DNA sequencing of Aurora kinases, cellular target inhibition, and ...
Whether aurora A or aurora B is the better anticancer drug target is a matter of debate (8). At least two groups have directly addressed this question in the laboratory. Warner et al. (36) compared the effects of aurora A and aurora B antisense oligonucleotides in pancreatic cancer cells and found that aurora A-targeted therapy may be preferable to aurora B targeting, as shown by mitotic arrest and the rapid induction of apoptosis. Girdler et al. (37) compared the effects of RNA interference and small molecules targeting aurora A versus aurora B in colon cancer cells and found that the cells tested were extremely sensitive to aurora B inhibition. Interestingly, dual inhibition of aurora A and B results in phenotypes identical to inactivation of aurora B alone (28). Using RNA interference experiments, Yang et al. (38) showed that inactivation of aurora B indeed bypasses the requirement for aurora A and leads to polyploidy, indicating that aurora B is responsible for mitotic arrest in the absence ...
Whether aurora A or aurora B is the better anticancer drug target is a matter of debate (8). At least two groups have directly addressed this question in the laboratory. Warner et al. (36) compared the effects of aurora A and aurora B antisense oligonucleotides in pancreatic cancer cells and found that aurora A-targeted therapy may be preferable to aurora B targeting, as shown by mitotic arrest and the rapid induction of apoptosis. Girdler et al. (37) compared the effects of RNA interference and small molecules targeting aurora A versus aurora B in colon cancer cells and found that the cells tested were extremely sensitive to aurora B inhibition. Interestingly, dual inhibition of aurora A and B results in phenotypes identical to inactivation of aurora B alone (28). Using RNA interference experiments, Yang et al. (38) showed that inactivation of aurora B indeed bypasses the requirement for aurora A and leads to polyploidy, indicating that aurora B is responsible for mitotic arrest in the absence ...
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B / incenp); 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A/B inhibitors. In vivo efficacy has been demonstrated on relevant tumor models, but unfortunately, SAR156497 displayed a narrow therapeutic window.
T he carcinogenic risk induced by low doses of ionizing radiation is controversial. It cannot be assessed with epidemiologic methods alone because at low. doses the data are imprecise and often conflicting. Since the 1970s, the radiation protection community has estimated the risk of low doses by means of extrapolation from the risk assessed at high doses, generally by using the linear no-threshold (LNT) model.. The LNT relationship implies P5091 molecular weight proportionality between dose and cancer risk. This approach is based on one set of data and two hypotheses: (a) The relationship between. dose and DNA damage in vivo seems linear from 1 mGy to 100 Gy with use of H2AX foci as a marker for DNA double-strand breaks (DSBs)-however, this marker is not specific (1); (b) each DSB is hypothesized to have the same probability of inducing cell transformation, irrespective of the Sapanisertib quantity of DSBs present simultaneously in the cell; and (c) each transformed cell is hypothesized ...
Aurora Kinase A Pipeline Review H2 Market 2019. Aurora Kinase A Pipeline Review H2 Market Size by Types, Applications, Major Regions and Major Manufacturers including the capacity, production, price, revenue, cost, gross margin, sales volume, sales revenue, consumption, growth rate, import, export, supply, future strategies.
Aurora kinases comprise a family group of highly conserved serine-threonine proteins kinases that play a pivotal part in the rules of cell routine. from homozygous mutant moms. The mutants recognized were given titles linked to the polar areas, and included not merely but also the similarly famous gene was initially found out in the past due 1980s within a seek out genes regulating cell routine development (Glover, 1989; Glover et al., 1989, 1995). Since that time, Aurora kinases possess emerged as important players in the rules of cell department (for review observe Carmena et al., 2009). The original steady circulation of publications quickly accelerated as paralogs in various species were found out and new features designated to them. The obtaining of elevated degrees of Auroras in malignancy cells soon activated the introduction of little molecule inhibitors of the kinases (Hauf et al., 2003; Harrington et al., 2004). This as well was to become field where research output offers increased ...
OUTLINE: This is an open-label, dose-escalation, multicenter study.. Patients receive Aurora kinase inhibitor AT9283 (AT9283) IV over 24 hours on days 1 and 8 . Treatment repeats every 3 weeks in the absence of disease progression or unacceptable toxicity.. Cohorts of 3-6 patients receive escalating doses of AT9283 until the maximum tolerated dose (MTD) is determined. The MTD is defined as the dose at which at least 2 of 3 or 2 of 6 patients experience dose-limiting toxicity. The dose preceding the MTD is the recommended phase II dose (RPTD). Up to 8 additional patients are treated at the RPTD.. Patients treated at the RPTD undergo skin and tumor tissue biopsy and blood collection at baseline and on days 2 and/or 3. Samples are examined by pharmacokinetic and pharmacodynamic analysis, including immunohistochemistry, immunocytochemistry, western blotting, immunoenzyme techniques, flow cytometry, and reverse transcriptase-polymerase chain reaction, for biological markers.. After completion of ...
The purpose of this study is to assess the safety and tolerability of MK-0457(VX-680), an Aurora kinase inhibitor, in participants with advanced solid tumors. Bioavailability of the oral formulation will also be assessed. The primary study hypothesis is that administration of MK-0457 is sufficiently safe and tolerated to permit further study ...
Fingerprint Dive into the research topics of The Aurora Kinase A polymorphisms are not associated with recurrencefree survival in prostate cancer patients. Together they form a unique fingerprint. ...
Background Autoantibodies against the second extracellular cycle of the 1-adrenergic receptor (1-AA) not only contribute to increased susceptibility to center failing, but also play a causative function in myocardial remodeling through their sympathomimetic-like results that are induced upon holding to the 1-adrenergic receptor. CCK-8 sets and CFSE assay. Traditional western blotting was utilized to evaluate the movement of phospho-VASP and phospho-p38 MAPK. Outcomes 1-AA improved the growth of Testosterone levels lymphocytes. This impact could end up being obstructed by the picky 1-adrenergic receptor villain metoprolol, PKA inhibitor L89, and g38 MAPK inhibitor SB203580. Furthermore, the expression of the phosphorylated forms of phospho-p38 and phospho-VASP MAPK were markedly increased in the presence of 1-AA. 1-AA also inhibited the release of interferon- (IFN-) while marketing an boost in interleukin-4 (IL-4) amounts. A conclusion These outcomes demonstrate that 1-AA singled out from DCM ...
Weve provided evidence which the stimulatory ramifications of (?)-epicatechin ((?)-EPI) in endothelial cell nitric oxide (Zero) production might involve the involvement of the cell-surface receptor. usage of siRNA the function that GPER is wearing mediating ERK1/2 activation by (?)-EPI. GPER is apparently combined to a non Gi/o or Gs, proteins subtype. To extrapolate our results for an model, we utilized phenylephrine pre-contracted aortic bands evidencing that (?)-EPI may mediate vasodilation through GPER activation. To conclude, we provide proof that suggests the GPER being a potential mediator of (?)-EPI effects and highlights the key role that GPER may possess in heart protection. research. As previously reported by us, weve mixed MD simulations and docking research to explore the ligand binding sites of GPER (21). Weve centered on 14 and 70 ns conformers retrieved from MD simulations for the next docking evaluation as these conformers had been capable to acknowledge G1 and G15 in the ...
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03); **represents significant difference between. group 1%FBS + 10 ng/ml TGF-β1′ and group 1%FBS (P = 0.044). Figure 6 The effects of TGF-β1 on expression levels of PKCα and p38 MAPK. BxPC3 cells were treated with 0.1, 1 and 10 ng/ml TGF-β1 for 10 min, 30 min and 24 h. Total cellular protein was extracted and subjected to western blotting analysis to detect expression of PKCα, phosphorylated-p38/total p38 MAPK and phosphorylated-ERK1/2/total ERK1/2. Bx represents BxPC3 cells and Bx/T represents the stably transfected BxPC3 cells with TGF-β1 plasmid. To determine whether the induced PKCα activity is responsible for the TGF-β1-induced decrease in the sensitivity of BxPC3 cells to cisplatin, we treated the cells with a selective PKCα inhibitor, Gö6976, and assessed TGF-β1-induced drug resistance. We found that inhibition of PKCα. activity could partially reverse TGF-β1-induced drug resistance of BxPC3 cells to cisplatin PLX4032 in vivo (Figure 7). Figure 7 MTT assay. (A) BxPC3 ...
Inhibitors,Activator,Agonist,antagonist,API,Aurora,Metabolic Disease,VEGFR-PDGFR,Other Intermediate,Others,MOF Chemicals,,Active Biopharma Corp
As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
Once the dose levels reached 190 mg/m2, tests on skin biopsies showed that the drug was inhibiting the aurora B protein - in other words it was beginning to do what we expected it to.. The aurora B protein is responsible for phosphorylating histone H3 - a protein involved in the structure of chromatin (the strands of DNA that make up chromosomes) in cells. Inhibition of aurora B results in the inhibition of phosphorylation of histone H3, thereby blocking that step in cell division. This study shows, for the first time, that the aurora kinase inhibitor PHA-739358 inhibits phosphorylation of histone H3 in the skin of patients, and therewith provides a proof for its (or one of its) mechanisms of action.. The researchers are continuing to recruit patients in order to define the safety of the drug and the recommended dose for subsequent studies. However, they believe the results so far are promising.. The clinical trial has proved the concept that inhibition of the aurora protein disrupts an ...
Objective This review sought to expand public welfare knowledge about the legal and policy areas of DUI-child endangerment laws and analyze the extent where jurisdictions offer priority for the protection of youngsters. of child deaths by a new driver with a TRAVERSIER ≥. 08. Conclusions Further work has to be done to boost state regulations on DUI-child endangerment. The 9 jurisdictions that do indirectly address this kind buy 1228960-69-7 of public health injury can sanction laws to achieve this and the 40 jurisdictions that already have regulations can grow their approaches to prioritize the proper protection of children. We all suggest that long R306465 run research add a close study of the impact of DUI-child endangerment laws. end up being interpreted to prosecute a driver underneath these circumstances were not included as there might be buy 1228960-69-7 no frequent identification and analysis of individual prosecutorial decisions around states. In every 9 insurance plan elements had ...
Its important to ask about the experience of your local Aurora lawn care companys employees before you select the company for your job. Experienced lawn care experts know which species and types of grass, shrubs and plants work best in the Aurora climate, and know how to maintain them. CVSHome.com researches local pros and partners with the ones that consistently provide the highest quality of service, and also offer competitive pricing. When you hire someone to perform lawn maintenance in Aurora, make sure that you get multiple bids, and ask for references. Even a small difference in pricing can add up over the long run, especially if you are getting frequent Aurora lawn cutting service.. ...
Encontre endereços e telefones de médicos homeopatas, farmácias e drogarias em Aurora do Pará que podem te ajudar com plantas medicinais.
See what 289 cruisers had to say about their Aurora cruises. Find candid photos and detailed reviews of the P&O Cruises Aurora cruise ship.
Javier Pinilla-Ibarz, MD, PhD, and Naval Daver, MD, describe some of the emerging therapies for chronic myeloid leukemia, such as aurora kinase inhibitors, and how treatment discontinuation is becoming a reality.
Aurora A (phospho Thr288) antibody (aurora kinase A) for ICC/IF, IHC-P, WB. Anti-Aurora A (phospho Thr288) pAb (GTX85609) is tested in Human samples. 100% Ab-Assurance.
Aurora A antibody [1F8] (aurora kinase A) for ELISA, FACS, ICC/IF, WB. Anti-Aurora A mAb (GTX60391) is tested in Human, Monkey, Rat samples. 100% Ab-Assurance.
How can we prevent mass killings like Aurora? - AP News: AURORA, Colo. (AP) - On the morning of the latest .12/12/2017 19:16:42PM EST.
Here is the definitive list of Auroras brazilian bbq catering as rated by the Aurora, IL community. Want to see who made the cut?
Find information on Aurora Technologies, Inc. on IQSdirectory. Request information on Aurora Technologies, Inc. located at ,Pacific,MO.
No matter if youre a new or returning patient, you can find helpful information and resources to make your interaction with Aurora simple and easy.
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Yes, thats little one-eyed Aurora undergoing a CT scan on her neck last week at Peak in Burlington. We have a mystery here. As a result, this post might end up being the length of a mystery novel. Sorry! Several...
Get quick and affordable treatment at Concentra Aurora Des Moines in Urbandale, IA. View todays hours, insurance accepted and patient reviews.
Recent releases in Mobile have including a lot of code changes in the Aurora channel. We plan to start doing less of this in the future and the future is now. The Aurora merge is on June 4 and we need to plan to have as much Fx15 feature work landed as possible. Yes, we still plan to do some work while in Aurora, but we have to start cutting back. Lets try to get some of the larger chunks of new features reviewed and landed this week. Make sure we can disable/backout features that wont make it fully in Aurora ...
Always curious what is a custom wrap converted carrier? Tryout to feel the difference! Specifications Material: Hand-made from Didymos Prima Aurora wrapPanel height: 17.5 or 44.5cm Panel width: 18.5 or 47cmSmallest waist to fit: 27 or 68.6cm Largest waist to fit: 57 or 144.8cmEstimated weight of carrier: 2Ib or 900
helps the cell to divide successfully, even if it takes slightly longer, Gerlich explains.. Aurora B delays cell division until chromosome bridges resolve. The researchers identified the already known enzyme Aurora B as an important player in the process. We noticed that Aurora B ...
Theres a medical process that will happen to each of us: Death. Its not the same for everyone, but there are commonalities. What everyone should know.
This process is associated with Aurora B Protein Kinase. When Aurora B's function is disrupted, MCAK ability to locate ... Andrews PD, Ovechkina Y, Morrice N, Wagenbach M, Duncan K, Wordeman L, Swedlow JR (February 2004). "Aurora B regulates MCAK at ... There are other environments in which MCAK's function is impaired, absent impact on its associated kinase. For example, alpha- ...
"Cyclin Dependent Kinase (CDK) and Aurora Kinase (AK) inhibitors , Cyclacel R&D for anticancer drugs acting on cell cycle". www. ...
... strong interest has shifted towards the aurora kinase proteins. The kinase gene Aurora A when amplified acts as an oncogene ... The localization of MAD2 and BubR1 to the kinetochore may also be dependent on the Aurora B kinase. Cells lacking Aurora B fail ... Aurora-B/Ipl1 kinase of the chromosomal passenger complex functions as the tensions sensor in improper kinetochore attachments ... The Aurora-B/Ipl1 kinase is also critical in correcting merotelic attachments, where one kinetochore is simultaneously attached ...
"NEDD9 depletion destabilizes Aurora A kinase and heightens the efficacy of Aurora A inhibitors: implications for treatment of ... Interaction of NEDD9 with Aurora A kinase may also play a role in tumor invasion. NEDD9 binds to and regulates acetylation of ... NEDD9 binds directly to the Aurora-A mitotic kinase at the centrosome, and promotes its activity, allowing cells to enter ... Other phosphorylation events in this region are imposed by the kinase Aurora-A, which phosphorylates residue S296, for ...
Disassembly of cilia requires the action of the Aurora A kinase. The current scientific understanding of primary cilia views ... Pugacheva EN, Jablonski SA, Hartman TR, Henske EP, Golemis EA (June 2007). "HEF1-dependent Aurora A activation induces ...
Other kinases that have interested Sebti include Rho-associated kinase and Aurora kinase. STAT3. In 2003 the Sebti lab ... May 30, 2014). "Dual Aurora A and JAK2 kinase blockade effectively suppresses malignant transformation". Oncotarget. 5 (10): ... Kinases. Sebti's work on the kinase Akt led to his interest in Triciribine. ... October 1, 2012). "RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor ...
Aurora kinase has two forms which are designated Aurora kinase A and Aurora kinase B. These proteins play a key role in mitosis ... In some human cancers, the expression and kinase activity of Aurora kinases have been up-regulated and has been looked into as ... A possible causes of multipolar spindle formation involve regulation of protein kinase family known as Aurora kinase. ... Jingyan Fu, Fu (26 January 2007). "Roles of Aurora Kinases in Mitosis and Tumorigenesis". Molecular Cancer Research. 5 (1): 1- ...
The CAS family member NEDD9 has also been shown to interact directly with AURKA (encoding Aurora-A kinase) to regulate cell ... it is possible that CASS4 may similarly interact with aurora-A kinase. CASS4 signaling may contribute to platelet activation ... "The focal adhesion scaffolding protein HEF1 regulates activation of the Aurora-A and Nek2 kinases at the centrosome". Nature ... These include association with FAK and Src family kinases at focal adhesions to transmit integrin-initiated signals to ...
"Drugging MYCN through an Allosteric Transition in Aurora Kinase A." Cancer Cell. 26 (3): 414-27. doi:10.1016/j.ccr.2014.07.015 ... N-Myc is also stabilized by aurora A which protects it from degradation. Drugs that target this interaction are under ... development, and are designed to change the conformation of aurora A. Conformational change in Aurora A leads to release of N- ... "Stabilization of N-Myc is a critical function of Aurora A in human neuroblastoma". Cancer Cell. 15 (1): 67-78. doi:10.1016/j. ...
Aurora B is a kinase active in late metaphase, and has been shown to function as a checkpoint for the proper attachments of ... Cimini, Daniela; Wan, Xiaohu; Hirel, Christophe B.; Salmon, E.D. (2006-09-05). "Aurora Kinase Promotes Turnover of Kinetochore ... When Aurora B was partially inhibited by a small molecule drug, Cimini et al. observed lagging chromatids at increasing ... "The Ska complex promotes Aurora B activity to ensure chromosome biorientation". The Journal of Cell Biology. 215 (1): 77-93. ...
"Expression of Aurora-B kinase and phosphorylated histone H3 in hepatocellular carcinoma". Anticancer Research. 26 (5A): 3585-93 ...
... is also important in activating and recruiting Aurora A kinase, a kinase responsible for phosphorylating TPX2 and ... In the presence of nuclear import factor importin α, TPX2 is bound and prevented from binding Aurora A kinase, though it is ... TPX2 recruits and activates Aurora A kinase by utilizing its short 43 amino acid long amino-terminal sequence to bind the ... Notably, this recognition between TPX2 and Aurora A is analogous to that between the cAMP-dependent protein kinase (cAPK) ...
"Survivin enhances Aurora-B kinase activity and localizes Aurora-B in human cells". J. Biol. Chem. 278 (1): 486-90. doi:10.1074/ ... Survivin has been shown to interact with: Aurora B kinase, CDCA8, Caspase 3, Caspase 7, Diablo homolog and INCENP. GRCh38: ...
Stabilization of DGL7 in cell occurs due to phosphorylation by Aurora A kinase. Expression of DGL7 is found in cancer and stem ... 2005). "Phosphorylation and stabilization of HURP by Aurora-A: implication of HURP as a transforming target of Aurora-A". Mol. ... Yu CT, Hsu JM, Lee YC, Tsou AP, Chou CK, Huang CY (July 2005). "Phosphorylation and stabilization of HURP by Aurora-A: ... implication of HURP as a transforming target of Aurora-A". Mol. Cell. Biol. 25 (14): 5789-800. doi:10.1128/MCB.25.14.5789- ...
2005). "The centrosomal protein Lats2 is a phosphorylation target of Aurora-A kinase". Genes Cells. 9 (5): 383-97. doi:10.1111/ ... 2005). "The Ste20-like kinase Mst2 activates the human large tumor suppressor kinase Lats1". Oncogene. 24 (12): 2076-86. doi: ... Large tumor suppressor kinase 2 (LATS2) is an enzyme that in humans is encoded by the LATS2 gene. This gene encodes a serine/ ... It interacts with the centrosomal proteins aurora-A and ajuba and is required for accumulation of gamma-tubulin and spindle ...
... has been shown to interact with INCENP, Survivin and Aurora B kinase. GRCh38: Ensembl release 89: ENSG00000134690 - ... "Phosphorylation and activation of cell division cycle associated 8 by aurora kinase B plays a significant role in human lung ...
Aurora kinases are required for proper spindle assembly and separation. Aurora A associates with centrosomes and is believed to ... Spindle assembly is largely regulated by phosphorylation events catalyzed by mitotic kinases. Cyclin dependent kinase complexes ... with many of these proteins serving as Aurora and Polo-like kinase substrates. In a properly formed mitotic spindle, bi- ... Polo-like kinase, also known as PLK, especially PLK1 has important roles in the spindle maintenance by regulating microtubule ...
"Phosphorylation of HsMis13 by Aurora B kinase is essential for assembly of functional kinetochore". J. Biol. Chem. 283 (39): ...
... has been shown to interact with: Aurora A kinase, CD29 NME3, Protein SET, RAR-related orphan receptor alpha, RAR-related ... "The centrosomal kinase Aurora-A/STK15 interacts with a putative tumor suppressor NM23-H1". Nucleic Acids Res. 30 (24): 5465-75 ... Nucleoside diphosphate kinase A is an enzyme that in humans is encoded by the NME1 gene. It is thought to be a metastasis ... Nucleoside diphosphate kinase (NDK) exists as a hexamer composed of 'A' (encoded by this gene) and 'B' (encoded by NME2) ...
He S, Yang S, Deng G, Liu M, Zhu H, Zhang W, Yan S, Quan L, Bai J, Xu N (2010). "Aurora kinase A induces miR-17-92 cluster ... "miR-17-5p Promotes migration of human hepatocellular carcinoma cells through the p38 mitogen-activated protein kinase-heat ...
... (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. It was investigated as a ... a selective Aurora A kinase inhibitor, in relapsed and refractory aggressive B- and T-cell non-Hodgkin lymphomas". Journal of ...
"Arabidopsis α Aurora Kinases Function in Formative Cell Division Plane Orientation". The Plant Cell. 23 (11): 4013-4024. doi: ... Another midline-localized protein, "two-in-on" (TIO), is a putative kinase and is also required for cytokinesis as shown by ... Oh, Sung Aeong; Bourdon, Valérie; Dickinson, Hugh G.; Twell, David; Park, Soon Ki (2014-03-01). "Arabidopsis Fused kinase TWO- ... The essential mechanism of MAPK cascade for phragmoplast expansion is suppressed by cyclin dependent kinase (CDK) activity ...
"Bora and the Kinase Aurora A Cooperatively Activate the Kinase Plk1 and Control Mitotic Entry". Science. 320 (5883): 1655-1658 ... This loop is further amplified indirectly through the coordinated interaction of the Aurora A kinase and the Bora cofactor. ... pathways which activate the Chk2 and Chk1 kinases, respectively. These kinases act upstream of Cdc25 and Wee1, the direct ... The main rad3 effector is the kinase Chk1, which is required for the G2-M arrest in response to DNA-damaging agents. Chk1 is an ...
Seki A, Coppinger JA, Jang CY, Yates JR, Fang G (June 2008). "Bora and the kinase Aurora a cooperatively activate the kinase ... These kinases phosphorylate and activate the effector kinases Chk2 and Chk1, respectively, which in turn phosphorylate the ... The G1 phase cyclin-dependent kinase works together with S phase cyclin-dependent kinase targeting p27 for degradation. In turn ... The cell is once more examined for sites of DNA damage or incomplete replication, and the kinases ATR and ATM are recruited to ...
Bell, G.P.; Fletcher, G.C.; Brain, R.; Thompson, B.J (2015). "Aurora kinases phosphorylate Lgl to induce mitotic spindle ... columnar pseudostratified epithelial cells must round up at mitosis in a process that involves the Aurora A and B kinases, ... Aguilar-Aragon, M.; Elbediwy, A.; Foglizzo, V.; Fletcher, G.C.; Li, V.S.W; Thompson, B.J. (2018). "Pak1 Kinase Maintains Apical ... but Cdc42 appears to act primarily via activating the kinases aPKC and Pak1 in Drosophila follicle cells. His laboratory also ...
BI811283 is a small molecule inhibitor of the aurora B kinase protein being developed by Boehringer Ingelheim for use as an ... a novel inhibitor of Aurora B kinase, on tumor senescence and apoptosis". J. Clin. Oncol. 28 (15 Suppl e13632): e13632. doi: ... Sutendra G, Michelakis ED (2013). "Pyruvate dehydrogenase kinase as a novel therapeutic target in oncology". Frontiers in ... studies with introducing thymidine kinase in gliomas, making them susceptible to aciclovir, are in their experimental stage. ...
"Aurora kinase A is a target of Wnt/beta-catenin involved in multiple myeloma disease progression". Blood. 114 (13): 2699-708. ...
2006). "Analysis of Aurora-A and hMPS1 mitotic kinases in mantle cell lymphoma". Int. J. Cancer. 118 (2): 357-63. doi:10.1002/ ... "Entrez Gene: TTK TTK protein kinase". Hanks SK, Quinn AM (1991). "Protein kinase catalytic domain sequence database: ... Dual specificity protein kinase TTK also known as Mps1 is an enzyme that in humans is encoded by the TTK gene. GRCh38: Ensembl ... 2003). "Human MPS1 Kinase Is Required for Mitotic Arrest Induced by the Loss of CENP-E from Kinetochores". Mol. Biol. Cell. 14 ...
Chen HL, Tang CJ, Chen CY, Tang TK (2005). "Overexpression of an Aurora-C kinase-deficient mutant disrupts the Aurora-B/INCENP ... and aurora-B kinase during male mouse meiosis". J. Cell Sci. 116 (Pt 6): 961-74. doi:10.1242/jcs.00330. PMID 12584241.. ... "Human INCENP colocalizes with the Aurora-B/AIRK2 kinase on chromosomes and is overexpressed in tumour cells". Chromosoma. 110 ( ... The ARK binding region has been found to be necessary and sufficient for binding to aurora-related kinase. This interaction has ...
The mitotic kinase aurora B phosphorylates histone H3 at serine 10, triggering a cascade of changes that mediate mitotic ... Ahn SH, Cheung WL, Hsu JY, Diaz RL, Smith MM, Allis CD (Jan 2005). "Sterile 20 kinase phosphorylates histone H2B at serine 10 ... SLBP are marked for degradation by phosphorylation at two threonine residues by cyclin dependent kinases, possibly cyclin A/ ... "Apoptotic phosphorylation of histone H2B is mediated by mammalian sterile twenty kinase". Cell. 113 (4): 507-17. doi:10.1016/ ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... protein kinase activity. • kinase activity. • protein serine/threonine kinase activity. • cyclin-dependent protein serine/ ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... Cyclin-dependent kinase 4 also known as cell division protein kinase 4 is an enzyme that in humans is encoded by the CDK4 gene ...
Montgomery, K. & Mak, A.S. (1984). „In vitro phosphorylation of tropomyosin by a kinase from chicken embryo". J. Biol. Chem. ... Aurora kinaza (Aurora A kinaza, Aurora B kinaza). Fas-aktivirana serin/treoninska kinaza (EC 2.7.11.8) ... deBelle, I. & Mak, A.S. (1987). „Isolation and characterization of tropomyosin kinase from chicken embryo". Biochim. Biophys. ...
Aurora at Jupiter's north pole as seen in ultraviolet light by the Hubble Space Telescope. ... B irradiation-induced G2 cell cycle arrest in human keratinocytes by inhibitory phosphorylation of the cdc2 cell cycle kinase ...
"Frequent alterations in the expression of serine/threonine kinases in human cancers". Cancer Research 66 (16): 8147-54. PMID ... Aurora kinaza (Aurora A kinaza, Aurora B kinaza). Fas-aktivirana serin/treoninska kinaza (EC 2.7.11.8) ...
"BRCA1 interacts with and is required for paclitaxel-induced activation of mitogen-activated protein kinase kinase kinase 3". ... "BRCA1 phosphorylation by Aurora-A in the regulation of G2 to M transition". J. Biol. Chem. 279 (19): 19643-8. doi:10.1074/jbc. ... kinase and ATM and Rad3 related kinase mediate phosphorylation of Brca1 at distinct and overlapping sites. In vivo assessment ... ATM/ATR are kinases activated by DNA damage. Mutation of serine residues may affect localization of BRCA1 to sites of DNA ...
1997). „Mitogen-activated protein kinase kinase 7 is an activator of the c-Jun NH2-terminal kinase". Proc. Natl. Acad. Sci. U.S ... Aurora kinaza (Aurora A kinaza, Aurora B kinaza). Fas-aktivirana serin/treoninska kinaza (EC 2.7.11.8) ... 1997). „Mitogen-activated protein kinases activate the serine/threonine kinases Mnk1 and Mnk2". EMBO J. ENGLAND. 16 (8): 1909- ... 2003). „The N and C termini of the splice variants of the human mitogen-activated protein kinase-interacting kinase Mnk2 ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... protein kinase activity. • PDZ domain binding. • SH3 domain binding. • scaffold protein binding. • metal ion binding. • kinase ... "Entrez Gene: CIT citron (rho-interacting, serine/threonine kinase 21)".. *^ a b c Madaule P, Furuyashiki T, Reid T, Ishizaki T ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... The complex also contains 2 regulatory enzymes, a kinase and a phosphorylase. The BCKDHA gene encodes the alpha subunit of E1, ... Receptor protein serine/threonine kinase (EC 2.7.11.30). *Bone morphogenetic protein receptors *BMPR1 ...
BRCA1 interacts with and is required for paclitaxel-induced activation of mitogen-activated protein kinase kinase kinase 3». ... full-length BARD1 mediates Aurora B degradation, cancer-associated BARD1beta scaffolds Aurora B and BRCA2». Cancer Res. 69 (3 ... kinase and ATM and Rad3 related kinase mediate phosphorylation of Brca1 at distinct and overlapping sites. In vivo assessment ... O'Brien, K A; Lemke S J, Cocke K S, Rao R N, Beckmann R P (1999). «Casein kinase 2 binds to and phosphorylates BRCA1». Biochem ...
"Protein kinase C and lipid signaling for sustained cellular responses" (ABSTRACT). FASEB J. 9 (7): 484-96. PMID 7737456 ... Aurora kinaza (Aurora A kinaza, Aurora B kinaza). Fas-aktivirana serin/treoninska kinaza (EC 2.7.11.8) ... "The extended protein kinase C superfamily". Biochem. J. 332 ( Pt 2): 281-92. PMC 1219479. PMID 9601053 ...
Soderling TR (1999). „The Ca-calmodulin-dependent protein kinase cascade". Trends in Biochemical Sciences. 24 (6): 232-6. PMID ... Aurora kinaza (Aurora A kinaza, Aurora B kinaza). Fas-aktivirana serin/treoninska kinaza (EC 2.7.11.8) ... Lisman, J. E. (1985) A mechanism for memory storage insensitive to molecular turnover: a bistable autophosphorylating kinase. ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... kinase activity. • protein binding. • ATP binding. • protein serine/threonine kinase activity. • protein kinase activity. ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by the second ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... protein kinase activity. • protein serine/threonine kinase activity. • protein binding. • ATP binding. • magnesium ion binding ... Microtubule-associated serine/threonine-protein kinase 1 is an enzyme that in humans is encoded by the MAST1 gene.[5] ...
Dhillon AS, Kolch W (2002). "Untying the regulation of the Raf-1 kinase". Arch. Biochem. Biophys. 404 (1): 3-9. PMID 12127063. ... Aurora kinaza (Aurora A kinaza, Aurora B kinaza). Fas-aktivirana serin/treoninska kinaza (EC 2.7.11.8) ... Li P, Wood K, Mamon H, Haser W, Roberts T (February 1991). "Raf-1: a kinase currently without a cause but not lacking in ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... Dual specificity mitogen-activated protein kinase kinase 6 also known as MAP kinase kinase 6 (MAPKK 6) or MAPK/ERK kinase 6 is ... protein kinase binding. • protein serine/threonine kinase activity. • identical protein binding. • MAP kinase kinase activity. ... kinase kinase. MAP kinases, also known as extracellular signal-regulated kinases (ERKs), act as an integration point for ...
Brachyury, Axl, MEK, and Aurora kinase A are molecular drivers of these programs, and inhibitors are currently in clinical ... "Casein Kinase II (CK2) as a Therapeutic Target for Hematological Malignancies". Current Pharmaceutical Design. 23 (1): 95-107. ... kinase (PI3K)/AKT axis, Hedgehog signaling pathway, nuclear factor-kappaB and Activating Transcription Factor 2 have also been ... is a potent TGF-β type I receptor kinase inhibitor that was demonstrated to reduce the size, the growth rate of tumors, and the ...
For example, phosphorylation of Serine 194 on RalA by the kinase Aurora A results in the relocation of RalA to the inner ... whereas phosphorylation of Serine 198 on RalB by the kinase PKC results in the relocation of RalB to other internal membranes ...
... it triggers transporter phosphorylation via protein kinase A (PKA) and protein kinase C (PKC) signaling, ultimately resulting ... Morgenthaler TI, Kapur VK, Brown T, Swick TJ, Alessi C, Aurora RN, Boehlecke B, Chesson AL Jr, Friedman L, Maganti R, Owens J, ... Psychostimulants] increase cAMP levels in striatum, which activates protein kinase A (PKA) and leads to phosphorylation of its ... calcium/calmodulin protein kinases) signaling, which, in addition to phosphorylating CREB, also phosphorylates HDAC5.. Figure 2 ...
December 2012). "Inhibiting aurora kinases reduces tumor growth and suppresses tumor recurrence after chemotherapy in patient- ... Utilizing PDX triple negative breast cancer models, scientists found that aurora kinase inhibitors slows tumor growth rate and ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... protein tyrosine kinase activity. • nucleotide binding. • MAP kinase kinase activity. • protein kinase activity. • protein ... kinase kinase. MAP kinases, also known as extracellular signal-regulated kinases (ERKs), act as an integration point for ... This protein kinase lies upstream of MAP kinases and stimulates the enzymatic activity of MAP kinases upon activation by a wide ...
Aurora at Jupiter's north pole as seen in ultraviolet light by the Hubble Space Telescope. ... B irradiation-induced G2 cell cycle arrest in human keratinocytes by inhibitory phosphorylation of the cdc2 cell cycle kinase ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... protein serine/threonine kinase activity. • ATP binding. • kinase activity. • protein binding. Cellular component. • cell ... Serine/threonine-protein kinase 19 is an enzyme that in humans is encoded by the STK19 gene.[5][6][7] ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... MAP kinase kinase kinase (MAP3K or MKKK). *MAP kinase kinase kinases *MAP3K1 ... A mitogen-activated protein kinase (MAPK or MAP kinase) is a type of protein kinase that is specific to the amino acids serine ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... kinase activity. • protein binding. • RNA polymerase II carboxy-terminal domain kinase activity. • ATP binding. • protein ... Cell division protein kinase 8 is an enzyme that in humans is encoded by the CDK8 gene.[5][6] ...
... full-length BARD1 mediates Aurora B degradation, cancer-associated BARD1beta scaffolds Aurora B and BRCA2". Cancer Research. 69 ... kinase binding. • RNA binding. • protein heterodimerization activity. • ubiquitin-protein transferase activity. • protein ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... A major target of Akt kinases is glycogen synthase kinase-3. EC 2.7.1.37 Pelle. is a serine/threonine kinase that can ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... A serine/threonine protein kinase (EC 2.7.11.1) is a kinase enzyme that phosphorylates the OH group of serine or threonine ( ...
Myosin-heavy-chain kinase (EC 2.7.11.7). *Aurora kinase *Aurora A kinase ... protein kinase activity. • cAMP-dependent protein kinase activity. • ADP binding. • AMP-activated protein kinase activity. • ... Dephospho-(reductase kinase) kinase (EC 2.7.11.3). *AMP-activated protein kinase α *PRKAA1 ... cAMP-dependent protein kinase regulator activity. • protein kinase binding. • ATP binding. • adenyl ribonucleotide binding. ...
Aurora C is a member of mitotic serine/threonine kinases that regulate centrosome maturation, chromosome segregation, and ... Recombinant full-length human AURORA C was expressed by baculovirus in Sf9 insect cells using an N-terminal GST tag. ... Use with ADP-Glo™ Kinase Assay. The ADP-Glo™ Kinase Assay is a luminescent kinase assay that measures ADP formed from a kinase ... The AURORA C Kinase Enzyme System can be purchased with or without the ADP-Glo™ Kinase Assay reagents. Used together, the ADP- ...
Aurora A belongs to a multigenic family of mitotic serine/threonine kinases, which are involved in the control of chromosome ... Recombinant full-length human Aurora A was expressed by baculovirus in Sf9 cells using an N-terminal GST tag. ... Aurora A NCBI Database Entry. The Aurora A Kinase Enzyme System can be purchased with or without the ADP-Glo™ Kinase Assay ... Use with ADP-Glo™ Kinase Assay. The ADP-Glo™ Kinase Assay is a luminescent kinase assay that measures ADP formed from a kinase ...
B kinase with putative anti-tumoral activity. Inhibitors of aurora kinases were shown to induce apoptosis in vitro and in vivo ... Aurora kinase inhibitor ZM447439 induces apoptosis via mitochondrial pathways.. Li M1, Jung A, Ganswindt U, Marini P, Friedl A ... ZM447439 (ZM) is a potent and selective inhibitor of aurora-A and - ...
Aurora-A kinase complexed with AMPPNP. Kukimoto-Niino, M., Murayama, K., Shirouzu, M., Yokoyama, S.. To be published. ... Serine/threonine-protein kinase 6. A. 285. Homo sapiens. Mutation(s): 3 Gene Names: AURKA, AIK, AIRK1, ARK1, AURA, AYK1, BTAK, ...
Aurora kinase A. A. 282. Homo sapiens. Mutation(s): 1 Gene Names: AURKA, AIK, AIRK1, ARK1, AURA, AYK1, BTAK, IAK1, STK15, STK6 ... Functional Role of Conserved HxD-histidine in the Catalytic Core of Protein Kinase. Zhang, L., Wang, J., Hou, L., Cao, P., Wu, ...
The human genome contains three members the Aurora kinase family: Aurora A kinase, Aurora B kinase and Aurora C kinase. The ... Aurora A and Aurora B kinases play important roles in mitosis. The Aurora A kinase is associated with centrosome maturation and ... Aurora A phosphorylation directs the cytoplasmic polyadenylation translation of mRNAs, like the MAP kinase kinase kinase ... contain orthologues only to Aurora A and Aurora B. In all studied species, the three Aurora mitotic kinases localize to the ...
Aurora kinase Aurora A kinase Aurora C kinase INCENP Spindle assembly checkpoint GRCh38: Ensembl release 89: ENSG00000178999 - ... Phosphorylation of CENP-A at serine 7 by Aurora A kinase recruits Aurora B to the centromere. Aurora B, itself, can also ... The Aurora kinases associate with microtubules during chromosome movement and segregation. Aurora kinase B localizes to ... Aurora B kinase has been shown to interact with: BARD1, BIRC5, and CDCA8 TACC1. FBXL2. Abnormally elevated levels of Aurora B ...
The kinases Aurora-A, -B and -C represent a family of s … ... Aurora-kinase inhibitors as anticancer agents Nat Rev Cancer. ... The kinases Aurora-A, -B and -C represent a family of such targets and several small-molecule inhibitors have been shown to ... What have these studies taught us about the therapeutic potential of inhibiting this family of kinases? ...
... Biochem Soc Trans. 2009 Oct;37(Pt 5):976-80. doi: 10.1042/ ... Destabilization of incorrect attachments requires the Ipl1/Aurora B kinase, which phosphorylates kinetochore substrates that ... The present review focuses on how Aurora B regulates attachments in response to centromere tension. ...
Compare Aurora Kinase B ELISA Kits from leading suppliers on Biocompare. View specifications, prices, citations, reviews, and ... Aurora Kinase B ELISA Kits. The ELISA (enzyme-linked immunosorbent assay) is a well-established antibody-based tool for ... Your search returned 58 Aurora Kinase B ELISA ELISA Kit across 7 suppliers. ... Mouse/Human/Rat Phospho-AURKB / Aurora-B (Thr232) ELISA Kit (Cell-Based Phosphorylation ELISA) ...
Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of ... IPR011009, Kinase-like_dom_sf. IPR000719, Prot_kinase_dom. IPR017441, Protein_kinase_ATP_BS. IPR008271, Ser/Thr_kinase_AS. ... IPR011009, Kinase-like_dom_sf. IPR000719, Prot_kinase_dom. IPR017441, Protein_kinase_ATP_BS. IPR008271, Ser/Thr_kinase_AS. ... Belongs to the protein kinase superfamily. Ser/Thr protein kinase family. Aurora subfamily.PROSITE-ProRule annotation. Manual ...
VX-680 inhibits Aurora A and Aurora B kinase activity in human cells.. Tyler RK1, Shpiro N, Marquez R, Eyers PA. ... VX-680, also known as MK-0457, is a member of a diverse group of small molecules that inhibit the Aurora kinases, and has shown ... Taken together, these data identify Aurora A and Aurora B as dual intracellular targets of VX-680. ... consistent with inhibition of the mitotic protein kinase Aurora B. In this study, we have investigated the effects of VX-680 in ...
MLN8054 inhibits recombinant Aurora A kinase activity in vitro and is selective for Aurora A over the family member Aurora B in ... B) IC50 values of MLN8054 against recombinant Aurora A, Aurora B, and a panel of other selected kinases. Kinase activity was ... Aurora A and Aurora B are structurally related serine/threonine protein kinases that function during mitosis. In humans, these ... The selectivity of MLN8054 for Aurora A over the structurally related Aurora B kinase was evaluated in HCT-116 tumor cells by ...
Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. Find all ... The Aurora B kinase assay:. For the Aurora B kinase assay, HeLa cells are lysed in a buffer containing 50 mM NaCl. The whole ... less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2. ... Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, ...
Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells. Sasai, ... Mitotic requirement for aurora A kinase is bypassed in the absence of aurora B kinase. Yang, H., Burke, T., Dempsey, J., Diaz, ... Human Aurora/Ipl1-related kinase 2 (Aurora-B) is a key regulator of mitosis [19]. ... Inactivation of aurora A activates checkpoint kinase BubR1 in an aurora B-dependent manner [27]. ...
Aurora A kinase controls cell cycle progression and mitosis by interacting with different proteins. Protein kinase C regulates ... A small molecule inhibitor of protein kinase c and aurora a kinase in cancer models has been produced at McGill University. ... Two proteins that are commonly associated with some of these cellular pathways in tumor progression are aurora A kinase and ... This technology is a small molecule inhibitor that is able to selectively target both Protein kinase C and Aurora A kinase in ...
Aurora Kinase B (Aurora 1 or Aurora And IPL1 Like Midbody Associated Protein 1 or Serine/Threonine Protein Kinase 12 or Serine/ ... Kinase B - Pipeline Review, H2 2018 drug pipelines has been added to ResearchAndMarkets.coms offering. ... Aurora Kinase B (Aurora 1 or Aurora And IPL1 Like Midbody Associated Protein 1 or Serine/Threonine Protein Kinase 12 or Serine/ ... Threonine Protein Kinase 5 or Serine/Threonine Protein Kinase Aurora B or STK1 or AURKB or EC 2.7.11.1) pipeline Target ...
Aurora kinase A AURKA role in cancer, overall survival in patients with bladder cancer, sequential gene expression profiling, ... The Role of Aurora Kinase A in Bladder Cancer - Expert Commentary May 15, 2019 Aurora kinase A (AURKA) plays a vital role in ...
Ausgesuchte Qualitäts-Hersteller für Aurora Kinase C Antikörper. Hier bestellen. ... Monoklonale und polyklonale Aurora Kinase C Antikörper für viele Methoden. ... aurora kinase C , ARK-3 , aurora 3 , aurora-related kinase 3 , aurora/IPL1-related kinase 3 , aurora/IPL1/EG2 protein 2 , ... serine/threonine-protein kinase aurora-C , aurora B , aurora/Ipl1/Eg2 protein 1 , serine/threonine kinase 13 (aurora/IPL-like) ...
The human aurora kinase family comprises three members: Aurora A, B and C (AURKA, AURKB and AURKC). Aurora A is important in ... Aurora kinases are a highly conserved family of enzymes which add phospho-groups to Serine/Threonine residues of substrate ... The involvement of these kinases in cell division and deregulated expression of aurora A and B in tumor cells (often resulting ... BioVision proudly offers several aurora kinase inhibitors including the ones mentioned above and more. ...
Aurora Kinases as Druggable Targets in Cancer Therapy » Blog Archives Menu Not Found. Skip to content *Home ...
Aurora A (IC50 = 0.004 uM) over Aurora B (IC50 = 0.172 uM). Find all the information about MLN8054 for cell signaling research. ... Aurora Kinase Inhibitors with Unique Features. * Pan Aurora Kinase Inhibitors. Danusertib (PHA-739358) : Pan-Aurora kinase ... less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2. ... Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, ...
Mitotic requirement for aurora A kinase is bypassed in the absence of aurora B kinase. FEBS Lett 2005;579:3385-91. ... Aurora-C kinase is a novel chromosomal passenger protein that can complement aurora-B kinase function in mitotic cells. Cell ... Aurora Kinases. The aurora family comprises three related kinases that share the highest degree of sequence homology in their ... that aurora kinases are appropriate drug targets; and that inhibitors of these particular aurora kinases can add to the cancer ...
Selected quality suppliers for anti-Aurora Kinase B antibodies. ... Order monoclonal and polyclonal Aurora Kinase B antibodies for ... aurora kinase B-Sv1 , aurora kinase B-Sv2 , aurora- and Ipl1-like midbody-associated protein 1 , aurora-1 , aurora-B , aurora- ... Serine/threonine-protein kinase aurora-B-B , aurora kinase B-B , aurora-B-B , aurora/IPL1-related kinase 2-B , serine/threonine ... serine/threonine kinase a , aurora kinase B , serine/threonine-protein kinase 12-like , Aurora/IPL1-related kinase 2-B , Serine ...
A) Inhibition in vivo of aurora-B kinase in tumor cells. Tet-o-MYC/Eμ-SR-tTA transgenic mice maintained on a doxycycline-free ... B) Reversible inhibition of aurora-B kinase by VX-680. RPE-MYC cells were treated for 3 d with 300 nM VX-680 and then ... Therapeutic potential of a synthetic lethal interaction between the MYC proto-oncogene and inhibition of aurora-B kinase. Dun ... Therapeutic potential of a synthetic lethal interaction between the MYC proto-oncogene and inhibition of aurora-B kinase ...
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... Demidov D., Van Damme D., ... Aurora-like kinases play key roles in chromosome segregation and cytokinesis in yeast, plant, and animal systems. Here, we ... which share high amino acid identities with the Ser/Thr kinase domain of yeast Ipl1 and animal Auroras. Structure and ... whereas the diversification of plant alpha and beta Aurora kinases predates the origin of land plants. The transcripts and ...
The effect of the clinical Aurora-kinase inhibitor VX680 on proliferation of 20 human-myeloma-cell-lines and survival of 5 ... We found Aurora-A and -B to be expressed at varying frequencies in primary myeloma-cells of different patient-cohorts, Aurora-C ... In conclusion, using gene expression profiling, Aurora-kinase inhibitors as promising therapeutic option for newly-diagnosed ... absent Aurora-A expression show a significantly higher proliferation rate, but neither a higher absolute number of chromosomal ...
Aurora kinase inhibition is a new mechanism of action. It helps to create the structure that separates chromosomes in cells, an ... Like most Aurora kinases, those compounds dont distinguish between the A and B forms. According to Niculescu, MLN8237s ... There are no approved Aurora kinases on the market; however, there are others in development, including AT9283 from Cancer ... Millennium Starts Pivotal Trial of Its Aurora Kinase Drug MLN8237 in PTCL ...
Aurora kinase A, Serine/threonine kinase 15, Aurora/IPL1-related kinase 1, Breast tumor-amplified kinase, Aurora-A, Aurora- ... AURKA (Aurora Kinase A) belongs to the mitotic serine/threonine kinases family. AURKA is a cell cycle-regulated kinase which ... related kinase 1, hARK1, AURKA, AIK, ARK1, AURA, BTAK, STK15, STK6, STK7, STK15, AURORA2, MGC34538. ...
  • Aurora kinase inhibitor ZM447439 induces apoptosis via mitochondrial pathways. (nih.gov)
  • ZM447439 (ZM) is a potent and selective inhibitor of aurora-A and -B kinase with putative anti-tumoral activity. (nih.gov)
  • VX-680 also exhibits potent cytotoxicity when compared to the well documented Aurora B inhibitor ZM447439. (nih.gov)
  • MLN8054 is a selective small-molecule Aurora A kinase inhibitor that has entered Phase I clinical trials for advanced solid tumors. (pnas.org)
  • In human tumor xenografts, MLN8054 induced mitotic accumulation and apoptosis, phenotypes consistent with inhibition of Aurora A. MLN8054 is a selective inhibitor of Aurora A kinase that robustly inhibits growth of human tumor xenografts and represents an attractive modality for therapeutic intervention of human cancers. (pnas.org)
  • In this report, we describe MLN8054, an orally active small-molecule inhibitor of Aurora A kinase that has entered clinical development. (pnas.org)
  • MLN8054, a Potent and Selective Inhibitor of Aurora A Kinase Activity. (pnas.org)
  • A small molecule inhibitor of protein kinase c and aurora a kinase in cancer models has been produced at McGill University. (mcgill.ca)
  • This technology is a small molecule inhibitor that is able to selectively target both Protein kinase C and Aurora A kinase in low nanomolar ranges. (mcgill.ca)
  • MLN8054 was the first orally administered Aurora A–selective inhibitor to be tested in human clinical trials for the treatment of colorectal cancer. (biovision.com)
  • MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. (selleckchem.com)
  • MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase with an IC50 of 4 nM, which shows >40-fold more selective inhibitory activity for Aurora A compared with Aurora B. [1] 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. (selleckchem.com)
  • The effect of the clinical Aurora-kinase inhibitor VX680 on proliferation of 20 human-myeloma-cell-lines and survival of 5 primary myeloma-cell-samples was tested. (archives-ouvertes.fr)
  • Millennium, a unit of Takeda Pharmaceutical Co. Ltd., may soon be able to add peripheral T-cell lymphoma (PTCL) to its list of cancers that can be treated with its investigational Aurora A kinase inhibitor, MLN8237 (alisertib). (bioworld.com)
  • Cambridge, Mass.-based Millennium will face more direct competition from EntreMed Inc., of Rockville, Md., with its Aurora A/angiogenic kinase inhibitor ENMD-2076. (bioworld.com)
  • Danusertib (Danu) is a pan-inhibitor of Aurora kinases and a third-generation breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1 (Bcr-Abl) tyrosine kinase inhibitor, but its antitumor effect and underlying mechanisms in the treatment of human breast cancer remain elusive. (dovepress.com)
  • Here we characterise the Aurora kinase inhibitor CCT137690, a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays and exhibits anti-proliferative activity against a wide range of human solid tumour cell lines. (aacrjournals.org)
  • The purpose of this study was to determine the maximum-tolerated dose (MTD), pharmacokinetics and safety profile for two different dosing regimens of barasertib, a selective inhibitor of Aurora B Kinase. (springer.com)
  • Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours. (sigmaaldrich.com)
  • This phase I study (ClinicalTrials.gov ID: NCT00424632) evaluated the safe dose, pharmacokinetics, and pharmacodynamics of the aurora kinase A and B inhibitor, PF-03814735. (sigmaaldrich.com)
  • We have studied the preclinical pharmacology of BI 847325, an ATP-competitive dual inhibitor of MEK and Aurora kinases. (aacrjournals.org)
  • Targeting hepatocarcinogenesis model in C56BL6 mice with pan-aurora kinase inhibitor Danusertib. (auth.gr)
  • To elucidate the expression of Aurora kinases (AURK) and the anticancer effects of pan-aurora kinase inhibitor Danusertib in hepatocarcinogenesis model in C56Bl6 mice. (auth.gr)
  • Thirty mice C56Bl6 were randomly divided into Group A or control, Group B animals who underwent experimental hepatocarcinogenesis with diethylnitrosamine (DEN), and Group C animals with DEN-induced hepatocarcinogenenesis that treated with pan-aurora kinase inhibitor Danusertib. (auth.gr)
  • The discovery that activated forms of Aurora A can have different dynamic properties raises the possibility that inhibitor molecules could be designed to exploit these differences and block specific activities of Aurora A in cancer cells. (elifesciences.org)
  • Importantly, concurrent inhibition of NIK or c-Abl disrupts Aurora inhibitor-induced feedback activation of STAT3 and sensitizes myeloma cells to Aurora inhibitors, implicating a combined inhibition of Aurora and NIK or c-Abl kinases as potential therapies for multiple myeloma. (haematologica.org)
  • Also In May, the drug giant made another acquisition to strengthen its cancer franchise by announcing an agreement to acquire AurKa Pharma, a company established by TVM Capital Life Science to develop oncology compound AK-01, an Aurora kinase A inhibitor that was originally discovered at Lilly. (thefreedictionary.com)
  • AurKa Pharma was established as part of the TVM Life Science Ventures VII fund, to develop an Aurora kinase A inhibitor called AK-01, an oncology compound that was originally discovered through a Lilly research and development program. (thefreedictionary.com)
  • AurKa Pharma is a company established by investment advisory and fund managers group TVM Capital Life Science to develop oncology compound AK-01, an Aurora kinase A inhibitor that was originally discovered at Lilly. (thefreedictionary.com)
  • Alisertib (MLN8237) is an investigational, orally available, selective Aurora A kinase inhibitor in clinical development for the treatment of solid tumors and hematological malignancies. (aspetjournals.org)
  • The Aurora Kinase Inhibitor II, also referenced under CAS 331770-21-9, controls the biological activity of Aurora Kinase. (merckmillipore.com)
  • A cell-permeable anilinoquinazoline compound that acts as a potent, selective, and ATP-competitive inhibitor of Aurora kinases (IC 50 = 310 nM and 240 nM for Aurora A and B, respectively, 1.25 µM in MCF7 cells). (merckmillipore.com)
  • A cell-permeable, potent, selective, and ATP-competitive inhibitor of Aurora kinases (IC 50 = 310 nM and 240 nM for Aurora A and B, respectively, 1.25 µM in MCF7 cells). (merckmillipore.com)
  • Barasertib-hQPA is a highly selective inhibitor of aurora-B kinase that has shown tumouricidal activity against a range tumour cell lines including those of leukaemic AML origin. (biomedcentral.com)
  • The Aurora Kinase/Cdk Inhibitor, also referenced under CAS 443797-96-4, controls the biological activity of Aurora Kinase/Cdk. (merckmillipore.com)
  • A cell-permeable triazolylsulfonamido compound that acts a reversible, ATP-competitive kinase inhibitor with selectivities towards Aurora kinases (IC 50 = 11 and 15 nM for Aurora-A, Aurora-B, respectively) and Cdk's (IC 50 = 9, 4, and 3 nM for Cdk1/B, Cdk2/A, and Cdk2/E, respectively). (merckmillipore.com)
  • The Aurora Kinase Inhibitor III, also referenced under CAS 879127-16-9, controls the biological activity of Aurora Kinase. (emdmillipore.com)
  • A cell-permeable 2,4-dianilinopyrimidine compound that acts as an ATP-competitive, potent, but non-selective inhibitor of Aurora A (IC 50 = 42 nM). (emdmillipore.com)
  • SERS and MD simulation studies of a kinase inhibitor demonstrate the emergence of a potential drug discovery tool. (semanticscholar.org)
  • We characterize the screen using a focused tool compound kinase inhibitor library. (gla.ac.uk)
  • Though the first Aurora kinase inhibitor, alisertib, entered the clinic several years ago, success has been limited possibly because of inhibition of Aurora B and C as well as off-target effects on unrelated proteins. (bellbrooklabs.com)
  • The functional relevance of this newly discovered regulatory axis is found to be highly correlated with triple-negative breast cancer, suggesting that an inhibitor for Aurora A will be valuable in similar cancers. (bellbrooklabs.com)
  • Effect of Food on the Pharmacokinetics of the Investigational Aurora A Kinase Inhibitor Alisertib (MLN8237) in Patients with Advanced Solid Tumors. (escholarship.org)
  • The VEGF Receptor Tyrosine Kinase Inhibitor Pazopanib in Combination with the MEK Inhibitor Trametinib in Advanced Solid Tumors and Differentiated Thyroid Cancers. (escholarship.org)
  • 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)
  • It has recently been demonstrated that Coenzyme A (CoA) is a highly selective ATP-competitive inhibitor of Aurora A kinase. (ucl.ac.uk)
  • The first, conserved the pantothenamide tail and focused on replacing the adenosine moiety of CoA with a heteroaromatic head group based around VX680 - a known inhibitor of the Aurora kinases. (ucl.ac.uk)
  • Aurora kinase A also known as serine/threonine-protein kinase 6 is an enzyme that in humans is encoded by the AURKA gene. (wikipedia.org)
  • Aurora A is a member of a family of mitotic serine/threonine kinases. (wikipedia.org)
  • Phosphorylation of CENP-A at serine 7 by Aurora A kinase recruits Aurora B to the centromere. (wikipedia.org)
  • Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. (uniprot.org)
  • Aurora A and Aurora B are structurally related serine/threonine protein kinases that function during mitosis. (pnas.org)
  • Aurora Kinase B (Aurora 1 or Aurora And IPL1 Like Midbody Associated Protein 1 or Serine/Threonine Protein Kinase 12 or Serine/Threonine Protein Kinase 5 or Serine/Threonine Protein Kinase Aurora B or STK1 or AURKB or EC 2.7.11.1) pipeline Target constitutes close to 16 molecules. (pharmiweb.com)
  • Aurora kinases are a highly conserved family of enzymes which add phospho-groups to Serine/Threonine residues of substrate proteins functioning in chromatid segregation during cell division. (biovision.com)
  • The human aurora family of serine-threonine kinases comprises three members, which act in concert with many other proteins to control chromosome assembly and segregation during mitosis. (aacrjournals.org)
  • AURKA (Aurora Kinase A) belongs to the mitotic serine/threonine kinases family. (prospecbio.com)
  • Aurora kinases are serine/threonine kinases that function as key regulators of mitosis and are frequently overexpressed in human cancers. (eur.nl)
  • Aurora kinases are a group of serine/threonine kinases responsible for the regulation of mitosis. (eurekaselect.com)
  • Aurora-A is a serine-threonine kinase implicated in the assembly and maintenance of the mitotic spindle. (rupress.org)
  • Although these processes are diverse and executed by a cadre of functional classes of proteins, posttranslational protein phosphorylation by a small group of serine-threonine kinases orchestrates many aspects of most steps from mitotic entry to exit. (sciencemag.org)
  • Aurora Kinase 1 and 2 encode cell cycle-regulated serine/threonine kinases that are involved in microtubule spindle activities during mitosis and meiosis. (leicabiosystems.com)
  • Many epithelial cancers show cell cycle dysfunction tightly correlated with the overexpression of the serine/threonine kinase Aurora A (AURKA). (elifesciences.org)
  • The Aurora kinase family (EC 2.7.11.1) is a collection of highly related serine/threonine kinases that functions as a key regulator of mitosis, essential for accurate and equal segregation of genomic material from parent to daughter cells. (axonmedchem.com)
  • Any of a family of three highly homologous serine/threonine kinases (Aurora kinase A, Aurora kinase B and Aurora kinase C), which play a critical role in regulating many processes that are pivotal to mitosis. (thefreedictionary.com)
  • Aurora Kinase A (Aurora 2 or Serine/Threonine Protein Kinase 15 or Serine/Threonine Protein Kinase 6 or Serine/Threonine Protein Kinase Aurora A or Aurora/IPL1 Related Kinase 1 or AURKA or EC 2.7.11.1) pipeline Target constitutes close to 13 molecules. (marketresearch.com)
  • Aurora Kinase A (Aurora 2 or Serine/Threonine Protein Kinase 15 or Serine/Threonine Protein Kinase 6 or Serine/Threonine Protein Kinase Aurora A or Aurora/IPL1 Related Kinase 1 or AURKA or EC 2.7.11.1) - Aurora kinase A also known as serine/threonine-protein kinase 6 is an enzyme that contributes to the regulation of cell cycle progression. (marketresearch.com)
  • It also reviews key players involved in Aurora Kinase A (Aurora 2 or Serine/Threonine Protein Kinase 15 or Serine/Threonine Protein Kinase 6 or Serine/Threonine Protein Kinase Aurora A or Aurora/IPL1 Related Kinase 1 or AURKA or EC 2.7.11.1) targeted therapeutics development with respective active and dormant or discontinued projects. (marketresearch.com)
  • Aurora Kinase B (Aurora 1 or Aurora And IPL1 Like Midbody Associated Protein 1 or Serine/Threonine Protein Kinase 12 or Serine/Threonine Protein Kinase 5 or Serine/Threonine Protein Kinase Aurora B or STK1 or AURKB or EC 2.7.11.1) - Aurora B kinase is a protein that functions in the attachment of the mitotic spindle to the centromere. (marketresearch.com)
  • Furthermore, this report also reviews key players involved in Aurora Kinase B (Aurora 1 or Aurora And IPL1 Like Midbody Associated Protein 1 or Serine/Threonine Protein Kinase 12 or Serine/Threonine Protein Kinase 5 or Serine/Threonine Protein Kinase Aurora B or STK1 or AURKB or EC 2.7.11.1) targeted therapeutics development with respective active and dormant or discontinued projects. (marketresearch.com)
  • Aurora A Kinase, along with -B and -C, are members of a family of serine/threonine protein kinases that play critical roles in coordinating mitosis, including establishment of the mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. (bellbrooklabs.com)
  • Aurora kinases are highly conserved serine/threonine kinases in eukaryotes, involved in many processes during cell division. (roche.com)
  • We have identified two human homologues of these genes, termed aurora1 and aurora2 , that encode cell‐cycle‐regulated serine/threonine kinases. (embopress.org)
  • The Aurora family members of serine/threonine kinases, Aurora A, B and C, play key roles in the regulation of cell division. (oncotarget.com)
  • This research project has focused on the Aurora kinases, a family of serine/threonine kinases which play a central role in chromosome segregation and cell division during mitosis. (ucl.ac.uk)
  • Aurora kinase family of serine/threonine kinases, frequently overexpressed in human cancers and implicated in tumorigenesis, induce chromosomal instability and oncogenic transformation when expressed at elevated levels in mammalian cells in vitro and in vivo. (elsevier.com)
  • A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (rush.edu)
  • We applied energetic analysis to this question and characterized the activation process of the serine/threonine kinase Aurora-A by phosphorylation and by its protein partner, targeting protein for Xenopus kinesin-like protein 2 (TPX2). (bath.ac.uk)
  • The Xenopus, Drosophila, and Caenorhabditis elegans genomes, on the other hand, contain orthologues only to Aurora A and Aurora B. In all studied species, the three Aurora mitotic kinases localize to the centrosome during different phases of mitosis. (wikipedia.org)
  • Aurora A and Aurora B kinases play important roles in mitosis. (wikipedia.org)
  • Finally, Aurora A helps orchestrate an exit from mitosis by contributing to the completion of cytokinesis- the process by which the cytoplasm of the parent cell is split into two daughter cells. (wikipedia.org)
  • Though the exact mechanism by which Aurora A aids cytokinesis is unknown, it is well documented that it relocalizes to the mid-body immediately before the completion of mitosis. (wikipedia.org)
  • Chromosomal segregation during mitosis as well as meiosis is regulated by kinases and phosphatases. (wikipedia.org)
  • 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)
  • Increased Aurora A expression occurs in a variety of human cancers and induces chromosomal abnormalities during mitosis associated with tumor initiation and progression. (pnas.org)
  • Despite similarities in name and structure, Aurora A and Aurora B carry out distinct activities in mitosis. (pnas.org)
  • Aurora A is expressed early in mitosis and localizes to centrosomes and proximal mitotic spindles ( 3 ). (pnas.org)
  • Aurora B localizes to kinetochores in mitosis and to the midbody during cytokinesis ( 3 ), where it phosphorylates several proteins, including INCENP (inner centromere protein), Histone H3, and RacGAP, among others ( 4 , 14 ). (pnas.org)
  • Hesperadin treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization, which can be specifically ascribed to the inhibition of Aurora B function during the process of chromosome attachment. (selleckchem.com)
  • Two proteins that are commonly associated with some of these cellular pathways in tumor progression are aurora A kinase and protein kinase C. Aurora A kinase controls cell cycle progression and mitosis by interacting with different proteins. (mcgill.ca)
  • Aurora B is the catalytic component of the chromosomal passenger complex which coordinates events during segregation of the chromatids during mitosis, histone modification (epigenetic regulation) and cytokinesis. (biovision.com)
  • Additionally, we demonstrate that Aurora A kinase associates with inner centromere protein (INCENP) during mitosis and that INCENP is competent to drive accumulation of the kinase to the centromere region of mitotic chromosomes. (rupress.org)
  • These findings reveal that both Aurora A and B contribute to kinetochore-microtubule attachment dynamics, and they uncover an unexpected role for Aurora A in late mitosis. (rupress.org)
  • Protein phosphorylation by a small number of kinases, in particular Aurora A, Aurora B, the cyclin-dependent kinase-cyclin complex Cdk1/cyclinB, and Polo-like kinase 1 (Plk1), orchestrates almost every step of cell division, from entry into mitosis to cytokinesis. (sciencemag.org)
  • The localization of Aurora A to centrosomes and proximal microtubules is distinct from that of Aurora B and C, which bind to centromeres early in mitosis before translocating to the central spindle in anaphase and the midbody during cytokinesis. (sciencemag.org)
  • The Aurora kinases regulate key stages of mitosis including centrosome maturation, spindle assembly, chromosome segregation and cytokinesis. (aacrjournals.org)
  • Aurora B is the catalytic component of the chromosomal passenger complex (CPC), which is critical for the correct progression through and completion of mitosis. (thefreedictionary.com)
  • Mitosis begins in mammalian cells when a protein accumulates between cell divisions and interacts with a second protein to initiate a cascade of kinase activation. (sciencemag.org)
  • Aurora A kinase is activated by 2-ME in S-phase as well as during mitosis, and phosphorylates CHIP at S273. (aacrjournals.org)
  • Like for all aurora-A kinases, the Xenopus pEg2 kinase level peaks in G(2)/M and is hardly detectable in G(1) cells, suggesting that the protein is degraded upon exit from mitosis as reported for the human aurora-A kinase. (inserm.fr)
  • Therefore, there is an urgent need to research and develop new treatments and one of the recent areas of cancer research has targeted components of mitosis, mainly the mitotic kinases. (ucl.ac.uk)
  • 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)
  • Although Aurora B is regarded as the "master regulator" of kinetochore-microtubule attachment, other mitotic kinases likely contribute to Hec1 phosphorylation. (rupress.org)
  • In this study, we demonstrate that Aurora A kinase regulates kinetochore-microtubule dynamics of metaphase chromosomes, and we identify Hec1 S69, a previously uncharacterized phosphorylation target site in the Hec1 tail, as a critical Aurora A substrate for this regulation. (rupress.org)
  • Nevertheless, the role of Aurora-dependent phosphorylation in establishing asymmetry might be conserved. (plantcell.org)
  • In many cases, these changes are brought about by reversible phosphorylation, and several protein kinases and phosphatases undergo at least transient association with either centrosomes or spindle MTs ( Nigg, 2001 ). (rupress.org)
  • Activation of Aurora A can impinge on YAP activity through direct phosphorylation. (ovid.com)
  • To discover more about the functions of Aurora A, Aurora B, and kinases of the Plk family, we mapped mitotic phosphorylation sites to these kinases through the combined use of quantitative phosphoproteomics and selective targeting of kinase activities by small-molecule inhibitors. (sciencemag.org)
  • CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. (aacrjournals.org)
  • Aurora Kinase 2 is regulated by phosphorylation which is important both for its activity and stability. (leicabiosystems.com)
  • Using fluorescence resonance energy transfer-based biosensors to measure localized phosphorylation dynamics in living cells, we found that phosphorylation of an Aurora B substrate at the kinetochore depended on its distance from the kinase at the inner centromere. (sciencemag.org)
  • Thus, centromere tension can be sensed by increased spatial separation of Aurora B from kinetochore substrates, which reduces phosphorylation and stabilizes kinetochore microtubules. (sciencemag.org)
  • Many eukaryotic protein kinases are activated by phosphorylation on a specific conserved residue in the regulatory activation loop, a post-translational modification thought to stabilize the active DFG-In state of the catalytic domain. (elifesciences.org)
  • Here we use a battery of spectroscopic methods that track different catalytic elements of the kinase domain to show that the ~100 fold activation of the mitotic kinase Aurora A (AurA) by phosphorylation occurs without a population shift from the DFG-Out to the DFG-In state, and that the activation loop of the activated kinase remains highly dynamic. (elifesciences.org)
  • The enzymes that catalyze this process, called protein kinases, are themselves controlled by the phosphorylation of a flexible region called the activation loop. (elifesciences.org)
  • For many years it had been thought that the purpose of activation loop phosphorylation was to clamp the otherwise flexible activation loop in an active state that allows molecules that need to be phosphorylated to bind to the kinase. (elifesciences.org)
  • In the absence of phosphorylation on the activation loop, kinase activity is usually restrained by rearrangements of the activation loop and DFG motif into specific autoinhibited conformations. (elifesciences.org)
  • Here, 2-ME stimulation activates CHIP by phosphorylation via Aurora kinase A (AURKA). (aacrjournals.org)
  • Aurora A kinase inhibitors and RNAi knockdown of Aurora A transcript selectively blocked CHIP phosphorylation and AR degradation. (aacrjournals.org)
  • Prostate cancer cells expressing a S273A mutant of CHIP have attenuated AR degradation upon 2-ME treatment compared to cells expressing wild-type CHIP, supporting the idea that CHIP phosphorylation by Aurora A activates its E3 ligase activity for the AR. (aacrjournals.org)
  • Accumulated NIK converts c-Abl tyrosine kinase from a nuclear proapoptotic into a cytoplasmic antiapoptotic effector by inducing its phosphorylation at Thr735, Tyr245 and Tyr412 residues, and, by entering into a trimeric complex formation with c-Abl and STAT3, increases both the transcriptional activity of STAT3 and expression of the antiapoptotic STAT3 target genes PIM1 and PIM2. (haematologica.org)
  • Phosphorylation by aurora kinase A induces Mdm2-mediated destabilization and inhibition of p53," Nature Genetics, vol. (thefreedictionary.com)
  • Live-cell imaging of a Forster resonance energy transfer (FRET)-based aurora kinase phosphorylation sensor revealed that midzone substrates were less phosphorylated in AAK-inhibited cells, despite the fact that midzone levels of active phosphorylated ABK (pABK) were normal. (thefreedictionary.com)
  • In human cancer cells, these dual inhibitors block the auto-phosphorylation of Aurora A (Thr-288) and the phosphorylation of the Aurora B substrate histone H3 (Ser-10) and the JAK2 substrate STAT3 (Tyr-705). (oncotarget.com)
  • Protein kinases are activated by phosphorylation and by the binding of activator proteins. (bath.ac.uk)
  • Based on this analysis, we propose a revised, fluid model of Aurora-A activation in which the first step is a reduction in the mobility of the activation loop by either TPX2 binding or phosphorylation. (bath.ac.uk)
  • Furthermore, our results suggest that unphosphorylated Aurora-A bound to the mitotic spindle by TPX2 is catalytically active and that the phosphorylation state of Aurora-A is an inaccurate surrogate for its activity. (bath.ac.uk)
  • Comparison with other kinases showed that kinetic characterization detects those kinases whose activation loops undergo a rearrangement upon phosphorylation and thus whose unphosphorylated state offers a distinct target for the development of Type II inhibitors. (bath.ac.uk)
  • Dodson, C & Bayliss, R 2012, ' Activation of Aurora-A Kinase by Protein Partner Binding and Phosphorylation Are Independent and Synergistic ', Journal of Biological Chemistry , vol. 287, pp. 1150-1157. (bath.ac.uk)
  • Aurora kinase A (AURKA) plays a vital role in several cancers, but little is known about its role in bladder cancer. (urotoday.com)
  • The human aurora kinase family comprises three members: Aurora A, B and C (AURKA, AURKB and AURKC). (biovision.com)
  • AURKA is a cell cycle-regulated kinase which may be involved in microtubule formation and/or stabilization at the spindle pole during chromosome segregation. (prospecbio.com)
  • AIBp (zeige APOA1BP Antikörper ) may not only be required for the dynamic movement of Aurora-A (zeige AURKA Antikörper ) at the centrosomes and spindle apparatus during the cell cycle, but may also be important during brain tumorigenesis. (antikoerper-online.de)
  • Depletion of one such molecule, aurora kinase A (Aurka), resulted in compromised self-renewal and consequent differentiation. (lu.se)
  • Aurora Kinase 2, also known as AurkA, STK15, BTAK, ARK1 and AIK1, localizes to interphase and mitotic centrosomes and to the spindle poles. (leicabiosystems.com)
  • In a recent study of 25 prostatic adenocarcinomas with Paneth cell-like neuroendocrine differentiation, 45% showed amplification of the Aurora Kinase A (AURKA) gene, which was associated with a higher percentage of Paneth cell-like neuroendocrine differentiation throughout the tumor, ductal features and a higher Gleason score. (thefreedictionary.com)
  • The Aurora A kinase is associated with centrosome maturation and separation and thereby regulates spindle assembly and stability. (wikipedia.org)
  • The Aurora B kinase is a chromosome passenger protein and regulates chromosome segregation and cytokinesis. (wikipedia.org)
  • Aurora B has been shown to bind to end-binding protein 1 (EB1), a protein that regulates microtubule dynamics. (wikipedia.org)
  • The present review focuses on how Aurora B regulates attachments in response to centromere tension. (nih.gov)
  • Aurora B kinase regulates chromosome-spindle attachments by phosphorylating kinetochore substrates that bind microtubules. (sciencemag.org)
  • Aurora A regulates several important steps in cell division, and plays important roles in several kinds of cancer. (elifesciences.org)
  • Metazoans appear to contain three distinct aurora-related kinases, each one of which regulates a different set of mitotic events. (biologists.org)
  • In each system, aurora A kinase controls spindle formation while aurora B kinase regulates chromosome disjunction and cytokinesis. (biologists.org)
  • Very recent studies have revealed that Aurora A acts as a positive regulator of the Yes-associated protein (YAP), a downstream effector in the Hippo pathway, which regulates tissue homeostasis and organ size during development. (bellbrooklabs.com)
  • We show that the aurora-B kinase AIR-2 regulates the selective release of chromosome cohesion during Caenorhabditis elegans meiosis. (rupress.org)
  • Aurora A regulates centrosome function during M phase and is required for initial activation of CDK1 at centrosomes and phosphorylates numerous target proteins. (roche.com)
  • Aurora A regulates chromosome maturation and mitotic spindle formation, Aurora B controls chromosomal segregation and cytokinesis [ 1 , 2 ] whereas Aurora C is involved in meiosis [ 3 ]. (oncotarget.com)
  • Aurora-C interactions with members of the Chromosome Passenger Complex ( CPC ), Survivin (zeige BIRC5 Antikörper ) and Inner Centromere Protein (INCENP (zeige INCENP Antikörper )) in reference to known Aurora-B (zeige AURKB Antikörper ) interactions to understand the functional significance of Aurora-C overexpression in human cancer cells, is reported. (antikoerper-online.de)
  • 279 Aurora Kinase B (AURKB) Antibodies from 32 manufacturers are available on www.antibodies-online.com. (antibodies-online.com)
  • Downstream analyses show that all of the compounds that induce tetraploid senescence inhibit Aurora kinase B (AURKB). (gla.ac.uk)
  • Numerous kinetochore targets of Aurora kinases have been determined in organisms ranging from yeast to man. (wikipedia.org)
  • The kinases Aurora-A, -B and -C represent a family of such targets and several small-molecule inhibitors have been shown to block their function. (nih.gov)
  • Taken together, these data identify Aurora A and Aurora B as dual intracellular targets of VX-680. (nih.gov)
  • Indeed, proteins intimately involved in the regulation of the cell cycle ( 6 ), particularly cell cycle-associated kinases ( 7 , 8 ), have been suggested as possible new anticancer targets. (aacrjournals.org)
  • Aurora A and B overexpression has also been associated with various human cancers and as such, they have been extensively studied as novel anti-mitotic drug targets. (aacrjournals.org)
  • Although a number of mitotic kinases have been identified, their targets and the intricacies of mitotic signal transduction pathways are just beginning to be understood. (asm.org)
  • The findings reveal an important functional interaction between NIK, Abl and Aurora kinases, and identify the NIK, c-Abl and PIM survival kinases as potential pharmacological targets for improving the efficacy of Aurora inhibitors in myeloma. (haematologica.org)
  • 3] Aurora Kinases: New Targets for Cancer Therapy. (axonmedchem.com)
  • Thus, the combined data provide new information on host cell kinases involved in viral replication and uncovered potential targets for future antiviral strategies. (ovid.com)
  • The implication of the auroras in tumourigenesis and the fact that that they are kinases, amenable to small molecule inhibition, makes them attractive targets for anticancer drug development. (biomedcentral.com)
  • The Aurora kinases regulate multiple aspects of mitotic progression, and their overexpression in diverse tumor types makes them appealing oncology targets. (semanticscholar.org)
  • The compound also targets Aurora A kinase and tubulin in vitro and in cells, which can explain the observed spindle anomalies. (oup.com)
  • Therefore, these kinases are highly sought after as targets for the discovery of new anticancer drugs and intense efforts have been made to prepare specific pharmacological inhibitors [ 10 ]. (oncotarget.com)
  • As a result, Aurora-A and -B are being investigated as potential targets for cancer therapy and multiple agents targeting the kinases are in early phase clinical trials with some having yielded encouraging results. (elsevier.com)
  • This chapter discusses functional involvement of Aurora kinase-A and -B in the regulation of cell proliferation and cancer-relevant cellular pathways validating their significance as cancer therapeutic targets. (elsevier.com)
  • Aurora A localizes next to the centrosome late in the G1 phase and early in the S phase. (wikipedia.org)
  • γ-tubulins, the base structure from which centrosomal microtubules polymerize, are also recruited by Aurora A. Without Aurora A the centrosome does not accumulate the quantity of γ-tubulin that normal centrosomes recruit prior to entering anaphase. (wikipedia.org)
  • Inactivating mutations in Aurora A or targeted protein depletion in cells derived from Drosophila melanogaster , Xenopus laveis , Caenorhabditis elegans , and human tumors prevent centrosome maturation, resulting in improper formation of the mitotic spindle ( 5 - 9 ). (pnas.org)
  • Kimura, Matsuda, Yoshioka, Okano: Cell cycle-dependent expression and centrosome localization of a third human aurora/Ipl1-related protein kinase, AIK3. (antikoerper-online.de)
  • Aurora A is important in centrosome function and duplication, mitotic entry and bipolar spindle assembly. (biovision.com)
  • Aurora A has been implicated in the G 2 -M transition ( 5 - 9 ), centrosome maturation and separation, as well as the formation of a bipolar spindle ( 4 ). (sciencemag.org)
  • Aurora Kinase 2 overexpression leads to centrosome amplification, chromosome instability and transformation in mammalian cells. (leicabiosystems.com)
  • These results indicate that murine Aurora-A facilitates, but is not absolutely required for, mitotic entry in murine embryonic fibroblasts and is essential for centrosome separation and bipolar spindle formation in vitro and in vivo. (asm.org)
  • Our data further show that estrogens, interacting with the estrogen receptor α, elicit persistent Aurora A kinase over expression that may affect abnormal centrosome duplication, and together with the loss of p53wt activity by the over expression of MDM2 lead to estrogen-induced oncogenesis. (ku.edu)
  • Why do polyploid cells containing abnormal centrosome numbers induced by Aurora not get eliminated at cell-cycle checkpoints? (inserm.fr)
  • Consistent with its role in spindle formation, aurora A kinase associates with the centrosome and microtubules. (biologists.org)
  • Aurora A is able to phosphorylate diverse substrates, making it vital in regulating spindle fiber alignment of chromosomes in anaphase for normal centrosome separation. (bellbrooklabs.com)
  • Aurora-A is frequently overexpressed in cancers, and its dysregulation is believed to drive tumorigenesis by causing chromosomal instability and tumor cell heterogeneity 2,3 Research on abnormal Aurora A kinase levels have shown centrosome amplification, aneuploidy from failure in cytokinesis, and cell transformation in cases of over-expression which can be linked to carcinogenesis and tumorigenesis. (bellbrooklabs.com)
  • These include the Drosophila aurora and yeast Ipl1 kinases that are required for centrosome maturation and chromosome segregation. (embopress.org)
  • Among the down-regulated genes revealed by cDNA microarray analyses, we identified Aurora-A, a centrosome kinase that plays a critical role in regulating M phase events and is frequently amplified in several types of cancer. (uniprot.org)
  • Aurora A expression in tumors is often associated with gene amplification, genetic instability, poor histologic differentiation, and poor prognosis. (aacrjournals.org)
  • Aurora B is frequently expressed at high levels in a variety of tumors, often coincidently with aurora A, and expression level has also been associated with increased genetic instability and clinical outcome. (aacrjournals.org)
  • In recent years, several small-molecule aurora kinase inhibitors have been developed that exhibit preclinical activity against a wide range of solid tumors. (aacrjournals.org)
  • Inhibition of both MEK and Aurora kinase in KRAS-mutant tumors was observed when BI 847325 was administered once weekly at 70 mg/kg. (aacrjournals.org)
  • To understand the molecular and cellular events involved in solely estrogen-induced oncogenesis, we studied the role of mitotic kinases, Aurora A and B, and the MDM2-p53wt pathway in estrogen-elicited oncogenesis, using two animal tumor models, the estrogen-induced tumors of the kidney in male Syrian hamsters, and the mammary gland in female ACI rats. (ku.edu)
  • Overexpression of Aurora-A readily transforms rat-1 and NIH3T3 cells, but not primary cells, whereas overexpression of Aurora-B induces metastasis after implantation of tumors in nude mice. (inserm.fr)
  • Aurora A, B and C kinases are found overexpressed in solid tumors, including colorectal, breast, and ovarian as well as leukemia [ 4 , 5 ]. (oncotarget.com)
  • In keeping with many protein kinase inhibitors, this compound is not a monospecific agent, and its cellular specificity remains largely unknown. (nih.gov)
  • Danu induced the activation of p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinases 1 and 2 (Erk1/2) and inhibited the activation of protein kinase B (Akt)/mammalian target of rapamycin (mTOR) signaling pathways in breast cancer cells. (dovepress.com)
  • show that the static model is incorrect in a protein kinase called Aurora A. In this enzyme, the phosphorylated activation loop continues to switch back and forth between active and inactive states. (elifesciences.org)
  • Aurora B complexes with three other proteins, Survivin, Borealin and INCENP. (wikipedia.org)
  • The transcripts and proteins of all three kinases are most abundant in tissues containing dividing cells. (uniprot.org)
  • The interaction with certain proteins not only contributes to kinase activation but also governs the spatially and temporally distinct subcellular localization of the three family members. (sciencemag.org)
  • Synthetic peptide near the C-terminus of human Aurora kinase A, B, and C proteins. (roche.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)
  • Overexpression of both active and inactive Aurora Kinase 2 can lead to polyploidy. (leicabiosystems.com)
  • A number of reports indicated that Aurora-A or Aurora-B overexpression represented a negative prognostic factor in several human malignancies. (plos.org)
  • As Aurora kinases are overexpressed in a large number of cancers, and ectopic expression of Aurora generates polyploid cells containing multiple centrosomes, it has been tempting to suggest that Aurora overexpression provokes genetic instability underlying the tumorigenesis. (inserm.fr)
  • They are strongly linked to cancer progression, and while overexpression of Aurora A and B occurs in many cancers, neither is regarded as an oncoprotein (as oncogenic mutations are required to promote tumour progression). (thefreedictionary.com)
  • In general, we found that TRAP220/MED1 expression is required for high basal levels of Aurora-A gene expression and that ectopic overexpression of TRAP220/MED1 coactivates transcription from the Aurora-A gene promoter. (uniprot.org)
  • Inhibitors of aurora kinases were shown to induce apoptosis in vitro and in vivo. (nih.gov)
  • MLN8054 inhibits recombinant Aurora A kinase activity in vitro and is selective for Aurora A over the family member Aurora B in cultured cells. (pnas.org)
  • Although these molecules were found to inhibit both Aurora A and Aurora B protein kinases in vitro , the major cellular phenotypic response they produced was consistent with inhibition of Aurora B ( 15 , 18 , 21 - 24 ). (pnas.org)
  • Doyle, Lee, Selesniemi, Styer, Rueda: The impact of vitrification on murine germinal vesicle oocyte In vitro maturation and aurora kinase A protein expression. (antikoerper-online.de)
  • An in vitro kinase assay demonstrated that AtAurora1 preferentially phosphorylates histone H3 at Ser 10 but not at Ser 28 or Thr 3, 11, and 32. (uniprot.org)
  • The premature termination of M phase was found to be a consequence of precocious inactivation of SAC caused by a direct inhibitory effect of the compound on Aurora B kinase in vitro and in cells. (oup.com)
  • Importantly, we have developed dual Aurora and JAK inhibitors, AJI-214 and AJI-100, which potently inhibit Aurora A, Aurora B and JAK2 in vitro. (oncotarget.com)
  • The phylogenetic analysis of available Aurora sequences from different eukaryotic origins suggests that, although a plant Aurora gene has been duplicated early in the evolution of plants, the paralogs nevertheless maintained a role in cell cycle-related signal transduction pathways. (uniprot.org)
  • 4 2 Among these, mutations in the genes encoding NF-κB-inducing kinase (NIK) or its negative regulators TRAF2, TRAF3, cIAP1, and cIAP2 lead to increased stability of NIK and subsequent aberrant activation of the non-canonical and canonical NF-κB pathways. (haematologica.org)
  • The major signaling pathways activated by EGFR are the RAS-RAF-MAP kinase pathway, which is mainly involved in proliferation, and the PI3K-PTEN-AKT pathway, which is mainly involved in survival [ 16 ]. (oncotarget.com)
  • Recent findings on the interactions of Aurora kinases with tumor suppressor gene and oncogene-regulated networks as well as involvement in other nonmitotic processes such as ciliary disassembly affecting important signaling pathways and developmental disorders termed ciliopathies, have led to a greater recognition of the functional significance of these kinases in development and disease. (elsevier.com)
  • Among the three members of the kinase family, Aurora- A, -B, and -C identified in humans, Aurora-A and -B have been reported to express at detectable levels in most proliferating somatic cells and characterized in detail for their involvement in cellular pathways relevant to cell proliferation and development of cancer-associated phenotypes. (elsevier.com)
  • The Aurora A gene is amplified and overexpressed in cancers originating from multiple tissue types ( 19 ). (pnas.org)
  • Further, aurora kinase gene polymorphisms are associated with increased risk or early onset of cancer. (aacrjournals.org)
  • Structure and expression of AtAurora1 and AtAurora2 suggest that these genes arose by a recent gene duplication, whereas the diversification of plant alpha and beta Aurora kinases predates the origin of land plants. (uniprot.org)
  • Relevant molecular alterations encountered in thyroid cancer progression comprise gene rearrangements of tyrosine kinase receptors, such as the RET/PTC and NTRK1, activating point mutations of the RAS and BRAF genes, and the oncogenic fusion protein PAX8-PPARγ [ 7 ]. (plos.org)
  • A gene on chromosome 17p13.1 that encodes Aurora kinase B, which is involved in regulating many mitotic events. (thefreedictionary.com)
  • We developed a conditional null mutation in the mouse Aurora-A gene to investigate Aurora-A functions in primary cells ex vivo and in vivo. (asm.org)
  • Deregulation of Aurora kinase gene expression in human testicular germ cell tumours. (thefreedictionary.com)
  • In contrast, inhibition of Aurora A kinase promoted an enhancement of viral early-late gene expression, suggesting a putative role of Aurora A signaling in host defense. (ovid.com)
  • Regulation of Aurora-A kinase gene expression via GABP recruitment of TRAP220/MED1. (uniprot.org)
  • Finally, we present evidence suggesting that TRAP/Mediator is recruited to the Aurora-A gene via direct interactions between TRAP220/MED1 and the Ets-related transcription factor GABP. (uniprot.org)
  • VX-680, also known as MK-0457, is a member of a diverse group of small molecules that inhibit the Aurora kinases, and has shown significant potential as an anti-cancer agent. (nih.gov)
  • This suggests that Aurora Kinase 2 can behave as a dominant negative mutant and inhibit other aurora kinases. (leicabiosystems.com)
  • and 3) agents that inhibit Aurora activity would be expected to increase AR levels and signaling, thereby promoting prostate cancer growth. (aacrjournals.org)
  • Indirect immunofluorescence showed that Aurora B and EB1 colocalize during anaphase on the central spindle and in the midbody during cytokinesis. (wikipedia.org)
  • Inhibition of Aurora B in mammalian cells prevents proper alignment of chromosomes to the spindle plate, inhibits cytokinesis, and results in the formation of multinucleated cells ( 15 - 18 ). (pnas.org)
  • Aurora-like kinases play key roles in chromosome segregation and cytokinesis in yeast, plant, and animal systems. (uniprot.org)
  • Complementation assays showed that the Arabidopsis α group Aurora kinases are functionally divergent from the single β group member AUR3 and that AUR1 functions in division plane orientation prior to cytokinesis. (plantcell.org)
  • Aurora A is required for spindle formation while aurora B is required for chromosome condensation and cytokinesis. (biologists.org)
  • Aurora kinases play an essential role in orchestrating chromosome alignment, segregation and cytokinesis during mitotic progression, with both aurora-A and B frequently over-expressed in a variety of human malignancies. (biomedcentral.com)
  • The use of several small molecule aurora kinase inhibitors as potential anticancer therapeutic is being investigated. (eur.nl)
  • Millennium said it believes that inhibition of Aurora kinase causes anomalies to occur during cell division, leading to apoptosis. (bioworld.com)
  • The families of cyclin-dependent (Cdk), Aurora, and Polo-like (Plk) kinases have emerged as the primary regulators of cell division. (sciencemag.org)
  • Indeed, exposure of tumor cells to inhibitors of Aurora kinase (Aurk) and Polo-like kinases (Plk), key regulators of G2-M, induces cell-cycle arrest, apoptosis, and enhanced sensitivity to conventional chemotherapy. (ca.gov)
  • Multiple regulators, many of which are kinases, are required to ensure that each event is completed in a timely fashion and in the proper order (reviewed in reference 46 ). (asm.org)
  • The Aurora kinases are key mitotic regulators in eukaryotes (reviewed in reference 45 ). (asm.org)
  • We investigated the effects of targeting the mitotic regulators aurora kinase A and B in pediatric acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). (eur.nl)
  • 1] Mitotic kinases as regulators of cell division and its checkpoints. (axonmedchem.com)
  • Especially protein kinases are important regulators of virus-host interaction indicated by remarkable kinome alterations induced upon HCMV infection. (ovid.com)
  • Interestingly, danusertib also inhibits several receptor tyrosine kinases such as Abl, Ret, FGFR-1 and TrkA. (eur.nl)
  • These tyrosine kinases are involved in the pathogenesis of a variety of malignancies and the observed multi-target inhibition may increase the antitumor activity resulting in extending the indication. (eur.nl)
  • Completing the structural family portrait of the human EphB tyrosine kinase domains. (semanticscholar.org)
  • VX-680 inhibits Aurora A and Aurora B kinase activity in human cells. (nih.gov)
  • Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. (selleckchem.com)
  • Hesperadin inhibits the ability of immunoprecipitated Aurora B to phosphorylate histone H3 with IC50 of 250 nM and markedly reduces the activity of other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) at a concentration of 1 μM. (selleckchem.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. (selleckchem.com)
  • Danusertib (formerly PHA-739358) is a small ATP competitive molecule that inhibits aurora A, B and C kinases. (eur.nl)
  • Danu arrested MCF7 and MDA-MB-231 cells in G 2 /M phase, accompanied by the downregulation of cyclin-dependent kinase 1 and cyclin B1 and upregulation of p21 Waf1/Cip1, p27 Kip1, and p53. (dovepress.com)
  • On the basis of these results, several confirmatory single-agent and combination studies have been initiated using alisertib and other inhibitors of aurora kinases in lymphoma. (ascopost.com)
  • Furthermore, siRNA silencing or pharmacological inhibition of Aurora A and JAK2 with Alisertib and Ruxolitinib, respectively, is more effective than blocking each kinase alone at suppressing anchorage-dependent and -independent growth and invasion as well as at inducing apoptosis. (oncotarget.com)
  • Aurora-A deletion increases apoptosis, suggesting that molecular therapies targeting Aurora-A may be effective in inducing tumor cell apoptosis. (asm.org)
  • Aurora B knockdown resulted in proliferation arrest and apoptosis, whereas aurora A knockdown caused no or only minor growth delay. (eur.nl)
  • 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)
  • What have these studies taught us about the therapeutic potential of inhibiting this family of kinases? (nih.gov)
  • Aurora-A conditional mutant mice provide a valuable system for further defining Aurora-A functions and for predicting effects of Aurora-A therapeutic intervention. (asm.org)
  • These results reveal a novel 2-ME→Aurora A→CHIP→AR pathway which promotes AR degradation via the proteasome, that may offer novel therapeutic opportunities for prostate cancer. (aacrjournals.org)
  • An intensive research effort over the past decade has led to the discovery of chemically distinct families of small molecule Aurora kinase inhibitors, many of which have demonstrated therapeutic potential in model systems. (semanticscholar.org)
  • Aurora-A Kinase as a Promising Therapeutic Target in Cancer. (bellbrooklabs.com)
  • Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237. (semanticscholar.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)
  • Here, weevaluated Aurora-A and Aurora-B mRNA expression and its prognostic relevance in a series of 87 papillary thyroid cancers (PTC), with a median follow-up of 63 months. (plos.org)
  • However, differently from other human solid cancers, detection of Aurora-A or Aurora-B mRNAs is not a prognostic biomarker inPTC patients. (plos.org)
  • Considering that Aurora kinase inhibitors are currently under clinical investigation in hematologic cancers, the identification of molecular events that limit the response to such agents is essential for enhancing clinical outcomes. (haematologica.org)
  • Additionally, Aurora A kinase plays an unexpected role in systematic tumor recurrences of glioblastoma, which opens new possibilities for selective inhibitors in treating one of the deadliest cancers. (bellbrooklabs.com)
  • Over-expression of Aurora-A or -B protein can lead to aneuploid cells and is frequently observed in various human cancers such as prostate, breast, and esophageal cancers. (roche.com)
  • Destabilization of incorrect attachments requires the Ipl1/Aurora B kinase, which phosphorylates kinetochore substrates that directly interact with microtubules. (nih.gov)
  • Here, we characterize three Arabidopsis thaliana protein kinases, designated AtAurora1, AtAurora2, and AtAurora3, which share high amino acid identities with the Ser/Thr kinase domain of yeast Ipl1 and animal Auroras. (uniprot.org)
  • As the cell cycle progresses, concentrations of Aurora A increase and the kinase associates with the mitotic poles and the adjacent spindle microtubules. (wikipedia.org)
  • Right before mitotic exit, Aurora A relocalizes to the mid-zone of the spindle. (wikipedia.org)
  • Aurora A is critical for proper formation of mitotic spindle. (wikipedia.org)
  • Furthermore, Aurora A is necessary for the proper separation of the centrosomes after the mitotic spindle has been formed. (wikipedia.org)
  • Without Aurora A, the mitotic spindle, depending on the organism, will either never separate or will begin to separate only to collapse back onto itself. (wikipedia.org)
  • Aurora B kinase is a protein that functions in the attachment of the mitotic spindle to the centromere. (wikipedia.org)
  • Specifically, Aurora B localizes to the chromosomes in prophase, the centromere in prometaphase and metaphase, and the central mitotic spindle in anaphase. (wikipedia.org)
  • Studies in several organisms indicate that Aurora B oversees chromosome biorientation by ensuring that appropriate connections are made between spindle microtubules and kinetochores. (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)
  • Aurora B inhibition may lead to an increase in the number of syntelic attachments (sister chromatid pairs in which both sister kinetochores are attached to microtubules radiating from the same spindle pole). (wikipedia.org)
  • A recent study has shown that one of these dual inhibitors also produces a phenotype consistent with Aurora A kinase inhibition, namely mitotic spindle abnormalities ( 27 ). (pnas.org)
  • Here we show that human Aurora-A binds to TPX2, a prominent component of the spindle apparatus. (rupress.org)
  • Binding studies demonstrated that the NH 2 terminus of TPX2 can directly interact with the COOH-terminal catalytic domain of Aurora-A. Although kinase activity was not required for this interaction, TPX2 was readily phosphorylated by Aurora-A. Upon siRNA-mediated elimination of TPX2 from cells, the association of Aurora-A with the spindle microtubules was abolished, although its association with spindle poles was unaffected. (rupress.org)
  • In turn, Aurora-A might regulate the function of TPX2 during spindle assembly. (rupress.org)
  • Furthermore, repositioning Aurora B closer to the kinetochore prevented stabilization of bi-oriented attachments and activated the spindle checkpoint. (sciencemag.org)
  • Aurora-A was previously implicated in mitotic entry and spindle assembly, although contradictory results prevented a clear understanding of the roles of Aurora-A in mammals. (asm.org)
  • We show here that conditional Aurora-A ablation in cultured embryonic fibroblasts causes impaired mitotic entry and mitotic arrest with a profound defect in bipolar spindle formation. (asm.org)
  • Germ line Aurora-A deficiency causes embryonic death at the blastocyst stage with pronounced cell proliferation failure, mitotic arrest, and monopolar spindle formation. (asm.org)
  • Aurora-A kinases are observed at centrosomes and adjacent spindle fibers, and current evidence supports key roles in regulating protein localization and function at centrosomes, as well as regulation of the assembly, stability, and function of the mitotic spindle (reviewed in reference 43 ). (asm.org)
  • Aurora A and Aurora B kinases are implicated in regulation of spindle assembly and correction of chromosomal segregation. (thefreedictionary.com)
  • Small-molecule inhibitors of human Aurora kinases have been identified by several groups. (pnas.org)
  • The involvement of these kinases in cell division and deregulated expression of aurora A and B in tumor cells (often resulting in genetic aberrations and thus leading to malignancy) together provided the incentive to identify and test small-molecule inhibitors of these kinases. (biovision.com)
  • The Aurora family includes a single member in yeasts ( Saccharomyces cerevisiae Ipl1p, Schizosaccharomyces pombe Ark1), two members each in Caenorhabditis elegans and Drosophila , and two or three members in vertebrates. (asm.org)
  • In thyroid cancer tissues a deregulated expression of Aurora kinases has been also demonstrated, butno information regarding its possible prognostic role in differentiated thyroid cancer is available. (plos.org)
  • The data reported here demonstrate that the expression of Aurora kinases is deregulated in the majority of PTC tissues, likely contributing to PTC progression. (plos.org)
  • Over-expression of Aurora kinases is reported to be associated with genetic instability and tumor formation [ 6 ] and several lines of evidence implicate Aurora kinases in malignant transformation [ 7 - 9 ]. (oncotarget.com)
  • [1] 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. (selleckchem.com)
  • Aurora kinases are strongly expressed in a broad range of cancer types. (aacrjournals.org)
  • The expression of aurora C in cancer is less well studied. (aacrjournals.org)
  • Genetic instability and cellular proliferation have been associated with Aurora-kinase expression in several cancer entities, including multiple myeloma. (archives-ouvertes.fr)
  • Aurora kinases have been regarded as a new target for cancer therapy, resulting in the development of Aurora kinase inhibitors. (eurekaselect.com)
  • Moreover, aberrant expression of YAP and Aurora A signaling is highly correlated with triple-negative breast cancer (TNBC). (ovid.com)
  • The analysis of Aurora-A and Aurora-B mRNA levels in PTC tissues, compared to normal matched tissues, revealed that their expression was either up- or down-regulatedin the majority of cancer tissues. (plos.org)
  • Aurora kinases, aneuploidy and cancer, a coincidence or a real link? (inserm.fr)
  • Would drugs against Aurora family members be of any help for cancer treatment? (inserm.fr)
  • The Aurora kinase inhibitors in cancer research and therapy. (thefreedictionary.com)
  • The reduced activity of Aurora B kinase resulted in polyploidy and suppression of cancer cell viability. (oup.com)
  • 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)
  • Danusertib was one of the first aurora kinase inhibitors to enter the clinic and has been studied in Phase I and II trials. (eur.nl)
  • Aurora-B is the catalytic component of the chromosomal passenger complex (CPC), which is composed of three additional non-catalytic subunits that direct its activity: survivin, inner centromere protein (INCENP) and borealin. (biomedcentral.com)
  • Intriguingly, expression of a dominant-negative and catalytically inactive form of Aurora B disrupted microtuble attachment to the kinetochore and prevented the association of dynein and centromere protein E (CENP-E) with kinetochores. (wikipedia.org)
  • In addition, disruption of Aurora A protein in tumor cells delays mitotic entry and progression, resulting in the accumulation of cells in the G 2 /M cell cycle phase ( 9 - 13 ). (pnas.org)
  • Increased Aurora A expression may lead to increased kinase activity, which is thought to contribute to tumor initiation and progression ( 20 ). (pnas.org)
  • This suspected oncogenic role of Aurora A, in addition to its essential role in mitotic progression, make it an attractive target for anticancer therapy. (pnas.org)
  • This paper reviews studies on Aurora kinases from recent years, including studies of their biological function, their relationship with tumor progression, and their inhibitors. (eurekaselect.com)
  • Additionally, topoisomerase II has been implicated in the regulation of Aurora B localization and enzymatic activity. (wikipedia.org)
  • Central to this regulation is Aurora B kinase, which phosphorylates kinetochore substrates to promote microtubule turnover. (rupress.org)
  • Aurora-A is a conserved kinase implicated in mitotic regulation and carcinogenesis. (asm.org)
  • In humans, these enzymes share 75% sequence homology in their kinase domains ( 1 , 2 ). (pnas.org)
  • In the case of the former, it has been suggested that Aurora A cooperates with the kinase Nek2 in Xenopus to dissolve the structure tethering the cell's centrosomes together. (wikipedia.org)
  • Therefore, without proper expression of Aurora A, the cell's centrosomes are never able to separate. (wikipedia.org)
  • For example, deletion of Aurora A in C. elegans results in an initial separation of the cell's centrosomes followed by an immediate collapse of the asters. (wikipedia.org)
  • 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)
  • In recent years, with the increase in Aurora kinase-related research, the important role of Aurora kinases in tumorigenesis has been gradually recognized. (eurekaselect.com)
  • Potent inhibition of MEK1/2 and Aurora A/B kinases by BI 847325 was demonstrated in enzymatic and cellular assays. (aacrjournals.org)
  • Aurora Kinase B - Pipeline Review, H2 2018 - ResearchAndM. (pharmiweb.com)
  • The "Aurora Kinase B - Pipeline Review, H2 2018" drug pipelines has been added to ResearchAndMarkets.com's offering. (pharmiweb.com)
  • In 2017, the global Aurora Kinase C market size was xx million US$ and it is expected to reach xx million US$ by the end of 2025, with a CAGR of xx.x % between 2018 and 2025. (rnrmarketresearch.com)
  • To analyze and study the global Aurora Kinase C sales, value, status (2013-2017) and forecast (2018-2025). (rnrmarketresearch.com)
  • We therefore hypothesize that forced alterations in Aurora A expression may influence this process by acting, directly or indirectly, as an upstream regulator of BRCA1 expression, thereby preventing polyploidy and stabilizing the genome. (aacrjournals.org)
  • It is known that Aurora kinase A and JAK2 pathway activation contributes to GVHD. (thefreedictionary.com)
  • Aurora A and JAK2 kinases are involved in cell division and tumor cell survival, respectively. (oncotarget.com)
  • Here we demonstrate that ectopic expression of Aurora A and JAK2 together is more effective than each alone at inducing non-transformed cells to grow in an anchorage-independent manner and to invade. (oncotarget.com)
  • Taken together, our genetic and pharmacological studies indicate that targeting Aurora A and JAK2 together is a more effective approach than each kinase alone at inhibiting malignant transformation and warrant further advanced pre clinical investigations of dual Aurora A/JAK2 inhibitors as potential anti tumor agents. (oncotarget.com)
  • The aurora kinases were first identified in 1990 during a cDNA screen of Xenopus eggs. (wikipedia.org)
  • Identification of a functional destruction box in the Xenopus laevis aurora-A kinase pEg2. (inserm.fr)
  • Members of the aurora kinase family regulate a range of mitotic processes. (biologists.org)
  • Although there is evidence to suggest that Aurora C might be a chromosomal passenger protein, the cellular function of it is less clear. (wikipedia.org)
  • Aurora B is a chromosomal passenger protein. (wikipedia.org)
  • The catalytic activity of protein kinases is regulated by finely-tuned allosteric mechanisms that reversibly switch the kinase domain between active and inactive conformational states ( Huse and Kuriyan, 2002 ). (elifesciences.org)
  • We identified for the first time a sequence RxxL in the C-terminal end of the kinase catalytic domain. (inserm.fr)
  • Three aurora kinases have been identified in humans and designated as Aurora-A, -B, and -C. They mostly consist of two domains: a regulatory domain in the NH2 terminus and a catalytic domain in the COOH terminus. (roche.com)
  • In addition to predicting previously unknown functions, this work establishes additional substrate-recognition motifs for these kinases and provides an analytical template for further use in dissecting kinase signaling events in other areas of cellular signaling and systems biology. (sciencemag.org)
  • Stringent regulatory control of protein kinases is critically important for the integrity of cellular signal transduction. (elifesciences.org)
  • Here we report a novel approach of kinome profiling with an outcome that suggests an important role of specific cellular protein kinases, such as AMPK, ABL2 and Aurora A. Inhibition of AMPK and ABL kinases showed a significant reduction, whereas inhibition of Aurora A kinase led to a slight activation of HCMV replication, as measured in a GFP reporter-based replication assay. (ovid.com)
  • The cellular geography of aurora kinases. (bellbrooklabs.com)
  • Description: Measuring inhibition of kinase activity in a biochemical assay. (guidetopharmacology.org)
  • Description: In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM. (guidetopharmacology.org)
  • Description: Inhibitory concentration determined in a Reaction Biology kinase sreening assay. (guidetopharmacology.org)
  • Find out more about how the high throughput screening (HTS) assays work on BellBrook's kinase assay page. (bellbrooklabs.com)
  • In the absence of Aurora A mad2, a protein that normally dissipates once a proper kinetochore-microtubule connection is made, remains present even into metaphase. (wikipedia.org)
  • Hesperadin and nocodazole treatment in HeLa cells abolishes kinetochore localization of BubR1 and diminishes the intensity of Bub1 at kinetochores, suggesting that Aurora B function is required for efficient kinetochore recruitment of BubR1 and Bub1, which in turn might be necessary for prolonged checkpoint signaling. (selleckchem.com)