Aurora Kinase C: 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.Aurora Kinases: 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.Aurora Kinase A: 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.Aurora Kinase B: 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.Protein Kinase C: 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.Protein-Serine-Threonine Kinases: A group of enzymes that catalyzes the phosphorylation of serine or threonine residues in proteins, with ATP or other nucleotides as phosphate donors.Centrosome: The cell center, consisting of a pair of CENTRIOLES surrounded by a cloud of amorphous material called the pericentriolar region. During interphase, the centrosome nucleates microtubule outgrowth. The centrosome duplicates and, during mitosis, separates to form the two poles of the mitotic spindle (MITOTIC SPINDLE APPARATUS).Spindle Apparatus: A microtubule structure that forms during CELL DIVISION. It consists of two SPINDLE POLES, and sets of MICROTUBULES that may include the astral microtubules, the polar microtubules, and the kinetochore microtubules.Mitosis: A type of CELL NUCLEUS division by means of which the two daughter nuclei normally receive identical complements of the number of CHROMOSOMES of the somatic cells of the species.Aneugens: Agents which affect CELL DIVISION and the MITOTIC SPINDLE APPARATUS resulting in the loss or gain of whole CHROMOSOMES, thereby inducing an ANEUPLOIDY.Protein Kinase Inhibitors: Agents that inhibit PROTEIN KINASES.Period Circadian Proteins: Circadian rhythm signaling proteins that influence circadian clock by interacting with other circadian regulatory proteins and transporting them into the CELL NUCLEUS.Medical Oncology: A subspecialty of internal medicine concerned with the study of neoplasms.RNA Interference: 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.Biotechnology: 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.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Health Facility Merger: The combining of administrative and organizational resources of two or more health care facilities.Cystadenocarcinoma, Serous: A malignant cystic or semicystic neoplasm. It often occurs in the ovary and usually bilaterally. The external surface is usually covered with papillary excrescences. Microscopically, the papillary patterns are predominantly epithelial overgrowths with differentiated and undifferentiated papillary serous cystadenocarcinoma cells. Psammoma bodies may be present. The tumor generally adheres to surrounding structures and produces ascites. (From Hughes, Obstetric-Gynecologic Terminology, 1972, p185)Cystadenoma: A benign neoplasm derived from glandular epithelium, in which cystic accumulations of retained secretions are formed. In some instances, considerable portions of the neoplasm, or even the entire mass, may be cystic. (Stedman, 25th ed)Ovarian Neoplasms: Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.Simazine: A triazine herbicide.Ploidies: The degree of replication of the chromosome set in the karyotype.Genital Neoplasms, Female: Tumor or cancer of the female reproductive tract (GENITALIA, FEMALE).Aneuploidy: The chromosomal constitution of cells which deviate from the normal by the addition or subtraction of CHROMOSOMES, chromosome pairs, or chromosome fragments. In a normally diploid cell (DIPLOIDY) the loss of a chromosome pair is termed nullisomy (symbol: 2N-2), the loss of a single chromosome is MONOSOMY (symbol: 2N-1), the addition of a chromosome pair is tetrasomy (symbol: 2N+2), the addition of a single chromosome is TRISOMY (symbol: 2N+1).Cyclooctanes: A group of compounds with an 8-carbon ring. They may be saturated or unsaturated.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.Polycyclic Compounds: Compounds consisting of two or more fused ring structures.
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)
Produktübersicht anti-Aurora Kinase C Antikörper
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 ...
an 80 kDaleukocyte-endothelial cell adhesion molecule 1 LECAM-1).CD62L is expressed on most peripheral blood B cells |...
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 ...
AURKC (isoform 3) (Human) Recombinant Protein - (P5686) - Products - Abnova
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Addgene: AURKB A4.1 gRNA
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) DNA Test Lab Cost INR 30000.00 best genetic offer discount price Delhi Mumbai Kolkata Chennai Bangalore Hyderabad...
AURKB (17p13) [RUO] - Product: Leica Biosystems
Aurora B Kinase Enzyme System
Cooperation between mitotic kinesins controls the late stages of cytokinesis
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 …
Anti-Aurora B Monoclonal Antibody(Clone: AURKB/3121R)
Method of determination of cancer cell drug sensitivity towards Aurora kinase inhibitors and overcoming their resistance |...
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 Kinase | Cell Cycle|Epigenetics| CSNpharm
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 - Wikipedia
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 ...
PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer | Molecular...
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 ...
Aurora Kinases as Anticancer Drug Targets | Clinical Cancer Research
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 | CAS#1256137-14-0 | 1375795-62-2 | Aurora inhibitor | | MedKoo Biosciences
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.
Aurora kinase B | Aurora kinase B was identified in humans by a polymerase chain reaction screen for kinases that are...
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 (Aurora 2 or Serine/Threonine Protein Kinase 15 or Serine/Threonine Protein Kinase 6 or Serine/Threonine...
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 - Synthetic Small Molecule Inhibitors of...
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 ...
Aurora Kinase Inhibitor AT9283 in Treating Patients With Advanced or Metastatic Solid Tumors or Non-Hodgkin's Lymphoma -...
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 ...
A VX-680 (an Aurora Kinase Inhibitor) Study in Patients With Advanced Cancer (0457-002) - Full Text View - ClinicalTrials.gov
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 ...
The Aurora Kinase A polymorphisms are not associated with recurrencefree survival in prostate cancer patients - Fingerprint ...
Mouse monoclonal to Cyclin E2 | barasertib Mediated Aurora Kinase B Inhibition
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 ...
May | 2019 | Aurora kinase B
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 ...
Aurora Kinase Inhibitors Products|Active Biopharma Corp
RCSB PDB - 3NRM: Imidazo[1,2-a]pyrazine-based Aurora Kinase Inhibitors
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.
Drug that interrupts a key stage of cell division shows promise in patients with advanced solid tumours
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 ...
February 2016 - Page 2 - Polo-Like Kinases and Aurora Kinases in Cancer Therapy
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 ...
Low Cost Lawn Care & Mowing Service in Aurora, CO | CVSHome
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.. ...
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May « 2012 « Meeting Notes
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 ...
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E-GEOD-42089 - The investigational Aurora kinase A inhibitor MLN8237 induces defects in cell viability and cell cycle...
PURPOSE: Despite over 70,000 new cases of bladder cancer in the United States annually, patients with advanced disease have a poor prognosis due to limited treatment modalities. We evaluate the role of Aurora A, identified as an upregulated candidate molecule in bladder cancer, in regulating bladder tumor growth. EXPERIMENTAL DESIGN: Gene expression in human bladder cancer samples was evaluated using RNA microarray and reverse-transcriptase PCR. The specific Aurora kinase A inhibitor MLN8237 (Millennium) was used to determine effects on bladder cancer cell growth using in vitro and in vivo models using malignant T24 and UM-UC-3 and papilloma-derived RT4 bladder cells. RESULTS: Urothelial carcinoma upregulates a set of 13 mitotic spindle associated transcripts, as compared to normal urothelium, including MAD2L1 (7.6-fold), BUB1B (8.8-fold), Aurora kinases A (5.6-fold) and Aurora kinase B (6.2-fold). Application of MLN8237 (10nM-1µM) to the human bladder tumor cell lines T24 and UM-UC-3 induced dose
Aurora kinase A promotes inflammation and tumorigenesis in mice and human gastric neoplasia<...
TY - JOUR. T1 - Aurora kinase A promotes inflammation and tumorigenesis in mice and human gastric neoplasia. AU - Katsha, Ahmed. AU - Soutto, Mohammed. AU - Sehdev, Vikas. AU - Peng, Dunfa. AU - Washington, M. Kay. AU - Piazuelo, M. Blanca. AU - Tantawy, Mohammed N.. AU - Manning, H. Charles. AU - Lu, Pengcheng. AU - Shyr, Yu. AU - Ecsedy, Jeffrey. AU - Belkhiri, Abbes. AU - El-Rifai, Wael. PY - 2013/1/1. Y1 - 2013/1/1. N2 - Background & Aims Chronic inflammation contributes to the pathogenesis of gastric tumorigenesis. The aurora kinase A (AURKA) gene is frequently amplified and overexpressed in gastrointestinal cancers. We investigated the roles of AURKA in inflammation and gastric tumorigenesis. Methods We used quantitative real-time reverse transcription polymerase chain reaction, immunofluorescence, immunohistochemistry, luciferase reporter, immunoblot, co-immunoprecipitation, and in vitro kinase assays to analyze AGS and MKN28 gastric cancer cells. We also analyzed Tff1-/- mice, growth of ...
aurora kinase inhibitor III | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY
Aurora kinases: shining lights on the therapeutic horizon?
The Aurora kinases have been implicated in tumorigenesis and are important regulators of diverse cell cycle events, ranging from the entry into mitosis, centrosome function, mitotic spindle formation, chromosome biorientation and segregation, and cytokinesis. The recent identification of novel bindi …
AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor...
The Aurora family of serine-threonine kinases are essential regulators of cell division in mammalian cells. Aurora-A and -B expression and kinase activity is elevated in a variety of human cancers and is associated with high proliferation rates and poor prognosis. AMG 900 is a highly potent and selective pan-aurora kinase inhibitor that has entered clinical evaluation in adult patients with advanced cancers. In mice, oral administration of AMG 900 blocks the phosphorylation of histone H3 on serine-10 (p-Histone H3), a proximal substrate of aurora-B and inhibits the growth of multiple human tumor xenografts, including multidrug-resistant models. In order to establish a preclinical pharmacokinetic-pharmacodynamic (PK-PD) relationship for AMG 900 that could be translated to the clinic, we used flow cytometry and laser scanning cytometry detection platforms to assess the effects on p-Histone H3 inhibition in terms of sensitivity, precision, and specificity, in human tumor xenografts in conjunction with
Humans instantly recognize a previously seen face while familiar. have an | barasertib Mediated Aurora Kinase B Inhibition
Humans instantly recognize a previously seen face while familiar. have an intrinsic ability to detect familiar inputs. This ability does not require a specialized wiring diagram or supervision and Rabbit Polyclonal to MCPH1 can consequently be expected to emerge naturally in developing cortical circuits. stands for the Euclidean range between the two neurons a and b. and C are guidelines used by CSIM that determine connectivity and synaptic strength, respectively. As raises, both the connection probability and the average connection size Neratinib will increase. The base value of C depends on the type Neratinib of connection: it is arranged to 0.3, 0.2, 0.4, and 0.1 for EE, EI IE, and II contacts, where E and I stand for excitatory and inhibitory neurons. The values are based on recordings from rodent cortical mind areas (Gupta et al., 2000). The actual value of C is definitely modulated by a user-defined parameter, Cscale. Input layer neurons are all excitatory. Contacts from input neurons to ...
Although the MAPK pathway is frequently deregulated in cancer, inhibitors targeting RAF or MEK have so far shown clinical activity only in BRAF- and NRAS-mutant melanoma. Improvements in efficacy may be possible by combining inhibition of mitogenic signal transduction with inhibition of cell-cycle progression. We have studied the preclinical pharmacology of BI 847325, an ATP-competitive dual inhibitor of MEK and Aurora kinases. Potent inhibition of MEK1/2 and Aurora A/B kinases by BI 847325 was demonstrated in enzymatic and cellular assays. Equipotent effects were observed in BRAF-mutant cells, whereas in KRAS-mutant cells, MEK inhibition required higher concentrations than Aurora kinase inhibition. Daily oral administration of BI 847325 at 10 mg/kg showed efficacy in both BRAF- and KRAS-mutant xenograft models. Biomarker analysis suggested that this effect was primarily due to inhibition of MEK in BRAF-mutant models but of Aurora kinase in KRAS-mutant models. Inhibition of both MEK and Aurora ...
Hesperadin | ≥99%(HPLC) | Selleck | Aurora Kinase inhibitor ...
AMG 900 | CAS 945595-80-2 | AbMole BioScience | AMG 900 Price
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FGF3 - Polo-Like Kinases and Aurora Kinases in Cancer Therapy
volume is one of a series beneath the general proceeding of and tummy cancer. times which effects the ultimate coding of T cells. For instance a danger indication for a particular antigen costimulation polarisation Rilpivirine localisation termination continuation and healing up process are necessary to induce a highly effective and appropriate defense response. It really is of remember that within a chronic inflammatory procedure that there surely is energetic immune system suppression of cell-mediated immunity which obviously must include any tumour development. The next section looks at the difficult network of inflammatory chemokines and Rilpivirine their function in tumour development and progression to greatly help know how they may result in tumour progression and exactly how they might be manipulated to improve an immune system response. It could certainly appear they are involved with tumour development vascularity and metastases and therefore represent potential healing targets. For ...
Integration of metabolic and immune system responses during pet advancement guarantees - Aurora Kinases as Druggable Targets in...
Integration of metabolic and immune system responses during pet advancement guarantees energy stability permitting both protection and development. energy death and imbalance. Hyperactive proinflammatory and tension signaling through NF-κB/Relish Jun N-terminal kinase and FOXO in mutants deregulates genes very important to immune defense digestive function and lipid fat burning capacity. Reducing the dose of either FOXO or Relish normalizes both lipid gene and metabolism expression in mutants. The function of Atf3 is normally conserved as individual ATF3 averts a number of the mutant phenotypes enhancing their survival. The single Atf3 might incorporate the varied roles of two related mammalian proteins. INTRODUCTION Animal development and development depend on coordinated features of body organs to stability energy intake and storage space under optimum or challenging circumstances such as meals scarcity or pathogen strike. When unfortunate circumstances are temporary pets survive by ...
Using multispectral optical observations to identify the acceleration mechanism responsible for flickering aurora
We present an analysis of flickering (2-10 Hz) auroras observed with a state-of-the-art multispectral imaging system, Auroral Structure and Kinetics, located in Tromso, Norway. Short (1-2 s) periods of flickering aurora have been identified in which the frequency of the brightness oscillations decreases or increases smoothly over time. To the authors knowledge this is the first detailed analysis of such "chirps" in flickering aurora or field-aligned bursts. We have found that the electron precipitation energy is strongly anticorrelated with the flickering frequency during all identified chirps. This result is consistent with the theory that flickering aurora is caused by the resonance interaction between electromagnetic ion cyclotron waves and precipitating electrons and that the wave parallel phase velocity is the primary factor determining the electron acceleration produced by this mechanism. Other current theories known to the authors cannot completely explain our observations.. ...
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ZM 447439 | Aurora B inhibitor | ZM447439 | CAS [331771-20-1] | Axon 1541 | Axon Ligand™ with |99% purity available from stock...
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Shit! Bring the…help me!". The words floated down to her from the ceiling of the night. As she was carried on, Cassandra thought that she should be more concerned about what she was managing to hear. It certainly didnt sound good, but…well, she just couldnt bring herself to care. She knew Aurora would patch her up, so why be worried? She wouldnt die here; she had too much she was looking forward to, and certainly had too much left to do. She refused to believe that childbirth would kill her when her foes had failed. As ironic as that death would be, it wouldnt be hers. It just didnt fit. She wished she could tell the doctor that, but her mouth wasnt working and Aurora wasnt a telepath. So that was a lost cause.. Not that it mattered, really. Cassandra felt like shed earned a break from the chaos, so she was going to enjoy her nap. Let the others fret over her; for now, she was done with fighting. Instead she drifted through her mindscapes, traveling over seas of grasses and rolling ...
... 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 ...
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: 414-27. doi:10.1016/j.ccr.2014.07.015. PMC ... 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. ...
2002). "Human TPX2 is required for targeting Aurora-A kinase to the spindle". J. Cell Biol. 158 (4): 617-23. doi:10.1083/jcb. ... TPX2 has been shown to interact with Aurora A kinase , KIF15, and Ran. GRCh38: Ensembl release 89: ENSG00000088325 - Ensembl, ... "Human TPX2 is required for targeting Aurora-A kinase to the spindle". J. Cell Biol. United States. 158 (4): 617-23. doi:10.1083 ... Bayliss R, Sardon T, Vernos I, Conti E (2003). "Structural basis of Aurora-A activation by TPX2 at the mitotic spindle". Mol. ...
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- ...
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 ...
... 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) ...
Mir-17 microRNA precursor family
"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 ... "Microtubule-Associated Kinase-like Protein RUNKEL Needed for Cell Plate Expansion in Arabidopsis Cytokinesis". Current Biology ... Oh, Sung Aeong; Bourdon, Valérie; Dickinson, Hugh G.; Twell, David; Park, Soon Ki (2014-03-01). "Arabidopsis Fused kinase TWO- ...
Cell cycle checkpoint
"Bora and the Kinase Aurora A Cooperatively Activate the Kinase Plk1 and Control Mitotic Entry". Science. 320 (5883): 1655-1658 ... These kinases phosphorylate and activate the effector kinases Chk2 and Chk1, respectively, which in turn phosphorylate the ... Plk1 is activated at the G2/M transition by the Aurora A and Bora, which accumulate during G2 and form an activation complex. ... The cell is once more examined for sites of DNA damage or incomplete replication, and the kinases ATR and ATM recruited to ...
Experimental cancer treatment
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). Rein DT, ... 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. ...
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 ...
Plays an important role in regulation of the kinase activity of AURKA/Aurora-A for mitotic commitment. JUB (gene) has been ... Hirota T, Kunitoku N, Sasayama T, Marumoto T, Zhang D, Nitta M, Hatakeyama K, Saya H (2003). "Aurora-A and an interacting ... Augments Mitogen-Activated Protein Kinase Activity in Fibroblasts, and Promotes Meiotic Maturation of Xenopus Oocytes in a Grb2 ... Protein Ajuba Influences Interleukin-1-Induced NF-κB Activation by Affecting the Assembly and Activity of the Protein Kinase Cζ ...
Chen HL, Tang CJ, Chen CY, Tang TK (2005). "Overexpression of an Aurora-C kinase-deficient mutant disrupts the Aurora-B/INCENP ... The ARK binding region has been found to be necessary and sufficient for binding to aurora-related kinase. This interaction has ... Leverson JD, Huang HK, Forsburg SL, Hunter T (April 2002). "The Schizosaccharomyces pombe aurora-related kinase Ark1 interacts ... and aurora-B kinase during male mouse meiosis". J. Cell Sci. 116 (Pt 6): 961-74. doi:10.1242/jcs.00330. PMID 12584241. ...
2005). "Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells ... Chen HL, Tang CJ, Chen CY, Tang TK (2005). "Overexpression of an Aurora-C kinase-deficient mutant disrupts the Aurora-B/INCENP ... "Entrez Gene: AURKC aurora kinase C". Human AURKC genome location and AURKC gene details page in the UCSC Genome Browser. ... This gene encodes a member of the Aurora subfamily of serine/threonine protein kinases. The encoded protein is a chromosomal ...
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/ ...
Cyclin-dependent kinase 4
Myosin-heavy-chain kinase (EC 184.108.40.206). *Aurora kinase *Aurora A kinase ... protein kinase activity. • kinase activity. • protein serine/threonine kinase activity. • cyclin-dependent protein serine/ ... Dephospho-(reductase kinase) kinase (EC 220.127.116.11). *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 ...
Tropomiozin kinaza - Википедија, слободна енциклопедија
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 18.104.22.168) ... deBelle, I. & Mak, A.S. (1987). „Isolation and characterization of tropomyosin kinase from chicken embryo". Biochim. Biophys. ...
Serin/treonin-specifična proteinska kinaza
"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 ...
Mitogenom-aktivirana proteinska kinaza 1 - Википедија, слободна енциклопедија
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 22.214.171.124) ... 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 126.96.36.199). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 188.8.131.52). *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 184.108.40.206). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 220.127.116.11). *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 18.104.22.168). *Bone morphogenetic protein receptors *BMPR1 ...
BRCA1 - Wikipédia, a enciclopédia livre
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 ...
Proteinska kinaza C
"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 22.214.171.124) ... "The extended protein kinase C superfamily". Biochem. J. 332 ( Pt 2): 281-92. PMC 1219479. PMID 9601053 ...
Ca2+/kalmodulin-zavisne proteinske kinaze - Википедија, слободна енциклопедија
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 126.96.36.199) ... Lisman, J. E. (1985) A mechanism for memory storage insensitive to molecular turnover: a bistable autophosphorylating kinase. ...
Myosin-heavy-chain kinase (EC 188.8.131.52). *Aurora kinase *Aurora A kinase ... kinase activity. • protein binding. • ATP binding. • protein serine/threonine kinase activity. • protein kinase activity. ... Dephospho-(reductase kinase) kinase (EC 184.108.40.206). *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 220.127.116.11). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 18.104.22.168). *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. ...
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 22.214.171.124) ... 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 126.96.36.199). *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 ...
... 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 ...
Patient derived xenograft
Myosin-heavy-chain kinase (EC 188.8.131.52). *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 ...
فرابنفش - ویکیپدیا، دانشنامهٔ آزاد
Myosin-heavy-chain kinase (EC 184.108.40.206). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 220.127.116.11). *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. ...
Mitogen-activated protein kinase
Myosin-heavy-chain kinase (EC 18.104.22.168). *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 22.214.171.124). *AMP-activated protein kinase α *PRKAA1 ...
Cyclin-dependent kinase 8
Myosin-heavy-chain kinase (EC 126.96.36.199). *Aurora kinase *Aurora A kinase ... Dephospho-(reductase kinase) kinase (EC 188.8.131.52). *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. ...
Serine/threonine-specific protein kinase
Myosin-heavy-chain kinase (EC 184.108.40.206). *Aurora kinase *Aurora A kinase ... A major target of Akt kinases is glycogen synthase kinase-3. EC 220.127.116.11 Pelle. is a serine/threonine kinase that can ... Dephospho-(reductase kinase) kinase (EC 18.104.22.168). *AMP-activated protein kinase α *PRKAA1 ... A serine/threonine protein kinase (EC 22.214.171.124) is a kinase enzyme that phosphorylates the OH group of serine or threonine ( ...
Myosin-heavy-chain kinase (EC 126.96.36.199). *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 188.8.131.52). *AMP-activated protein kinase α *PRKAA1 ... cAMP-dependent protein kinase regulator activity. • protein kinase binding. • ATP binding. • adenyl ribonucleotide binding. ...
Produktübersicht anti-Aurora Kinase C Antikörper
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) ...
Aurora C kinase is an essential regulator of cytokinesis seeing that
... Posted on February 5, 2018 at 10:38 pm.. Aurora C kinase ... Since overexpression of Aurora C kinase is normally linked with many types of cancers with high proliferative PF-03814735 ... Aurora C localization in midbody is required and important for controlling abscission time. In this model, Aurora C ... Amount?7. Model for mitotic regulations of Aurora C in cells by FBXL2 and Camera. (A) In the event of a chromosome connection ...
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an 80 kDaleukocyte-endothelial cell adhesion molecule 1 LECAM-1).CD62L is expressed on most peripheral blood B cells |...
Aurora kinase B (AurkB) is usually ubiquitously expressed while Aurora kinase C (AurkC) is usually specifically expressed in ... 4 Aurora kinase B and C affected pluripotency genes expression and cell fate during early morula stage. (A) Relative genes ... The kinase domains of AurkB and AurkC were responsible for their different ability to phosphorylate Histone H3 Serine 10 ( ... Collectively, our results are the first demonstration that the Decitabine price activity of mitotic kinases can influence cell ...
aurora kinase | PNAS
Aurora kinase-induced phosphorylation excludes transcription factor RUNX from the chromatin to facilitate proper mitotic ... A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X ... Activation loop phosphorylation of a protein kinase is a molecular marker of organelle size that dynamically reports flagellar ...
Aurora kinase - Wikipedia
As mentioned above, there are three classes of aurora kinases: Aurora A (a.k.a. Aurora 2) functions during prophase of mitosis ... Aurora kinases are serine/threonine kinases that are essential for cell proliferation. The enzyme helps the dividing cell ... Aurora inhibitor Bolanos-Garcia V M. Aurora kinases. The International Journal of Biochemistry & Cell Biology 37 (2005) 1572- ... Giet R, Prigent C. Aurora/Ipl1p-related kinases, a new oncogenic family of mitotic serine-threonine kinases. Journal of Cell ...
Aurora A kinase - Wikipedia
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 C Kinase Enzyme System
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 Kinase Enzyme System
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 ...
Aurora-kinase inhibitors as anticancer agents
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? ...
Aurora kinase inhibitor ZM447439 induces apoptosis via mitochondrial pathways. - PubMed - NCBI
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 - ...
RCSB PDB - 4O0W: Crystal structures of human kinase Aurora A
RCSB PDB - 4UYN: SAR156497 an exquisitely selective inhibitor of Aurora kinases
AURORA KINASE A. A. 287. Homo sapiens. Mutation(s): 0 Gene Names: AURKA, AIK, AIRK1, ARK1, AURA, AYK1, BTAK, IAK1, STK15, STK6 ... Sar156497, an Exquisitely Selective Inhibitor of Aurora Kinases.. Carry, J., Clerc, F., Minoux, H., Schio, L., Mauger, J., Nair ... The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and ... The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and ...
Aurora kinase B - DrugBank
Aurora Kinase B ELISA Kits | Biocompare.com
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) ...
Aurora kinases: shining lights on the therapeutic horizon?
The Aurora kinases have been implicated in tumorigenesis and are important regulators of diverse cell cycle events, ranging ... Aurora kinases: shining lights on the therapeutic horizon? Oncogene. 2005 Jul 28;24(32):5005-15. doi: 10.1038/sj.onc.1208752. ... The Aurora kinases have been implicated in tumorigenesis and are important regulators of diverse cell cycle events, ranging ... This review details new developments in the field and analyses the potential of Aurora kinases as anticancer targets. ...
VX-680 inhibits Aurora A and Aurora B kinase activity in human cells. - PubMed - NCBI
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 ...
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase | PNAS
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 | ≥99%(HPLC) | Selleck | Aurora Kinase inhibitor ...
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 Kinase B - Pipeline Review, H2 2018 - ResearchAndMarkets.com - PharmiWeb.com
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 184.108.40.206) pipeline Target ...
Aurora Kinase Inhibitors
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. ...
R547 - Aurora Kinases as Druggable Targets in Cancer Therapy
MLN8054 | Aurora Kinase inhibitor | Read Reviews & Product Use Citations
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, ...
Aurora Kinases as Anticancer Drug Targets | Clinical Cancer Research
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 ...
Product Overview anti-Aurora Kinase B Antibodies
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 ...
Aurora Kinases: New Targets for Cancer Therapy | Clinical Cancer Research
Pan Aurora kinase inhibition. NCT00099346. Merck & Co.. Advanced cancer. Pan Aurora kinase inhibition. NCT00104351. Merck & Co. ... Aurora-B inhibition. NCT00338182. AstraZeneca. Advanced solid tumors. PHA-739358. Pan Aurora kinase inhibition. NCT00335868. ... Aurora Kinases: New Targets for Cancer Therapy. Richard D. Carvajal, Archie Tse and Gary K. Schwartz ... Aurora Kinases: New Targets for Cancer Therapy Message Subject (Your Name) has forwarded a page to you from Clinical Cancer ...
Identification and dynamics of two classes of aurora-like kinases in Arabidopsis and other plants.
... 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 ...
Archive ouverte HAL - Inhibition of Aurora-kinases for tailored risk adapted treatment of multiple myeloma.
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 ...
Millennium Starts Pivotal Trial of Its Aurora Kinase Drug MLN8237 in PTCL | BioWorld
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 ...
AURKA Enzyme Human Recombinant | Aurora Kinase A | ProSpec
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. ...
Abstract 2387: Interplay between Aurora A kinase and BRCA1 promotes genetic stability | Cancer Research
Abstract 2387: Interplay between Aurora A kinase and BRCA1 promotes genetic stability. Christine M. Marion, Vanessa Yu and ... Interplay between Aurora A kinase and BRCA1 promotes genetic stability. [abstract]. In: Proceedings of the 105th Annual Meeting ... Aurora A kinase inhibition stabilizes the metaphase checkpoint and reduces the population of proliferating polyploid/aneuploidy ... Abstract 2387: Interplay between Aurora A kinase and BRCA1 promotes genetic stability ...
Aurora Kinase A and Ninein Interacting Protein (AUNIP) Antikörper
Weitere Produktkategorien zu Aurora Kinase A and Ninein Interacting Protein Antikörper * 24 anti-Aurora Kinase A and Ninein ... Weitere Antikörper gegen Aurora Kinase A and Ninein Interacting Protein Interaktionspartner. Mouse (Murine) Aurora Kinase A and ... Top anti-Aurora Kinase A and Ninein Interacting Protein Antikörper auf antikoerper-online.de. Showing 10 out of 24 products:. ... Human Aurora Kinase A and Ninein Interacting Protein (AUNIP) Interaktionspartner * AIBp (zeige APOA1BP Antikörper) may not only ...
Phase 1 Study Of Aurora Kinase Inhibitor PF-03814735 In Patients With Advanced Solid Tumors - Tabular View - ClinicalTrials.gov
Phase 1 Study Of Aurora Kinase Inhibitor PF-03814735 In Patients With Advanced Solid Tumors. The safety and scientific validity ... Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase ... Phase 1 Study Of Aurora Kinase Inhibitor PF-03814735 In Patients With Advanced Solid Tumors. ... Pharmacokinetic And Pharmacodynamic Trial Of The Oral Single Agent Aurora Kinase Inhibitor PF-03814735 In Patients With ...
AURKBMitoticExpressionSerineProtein kinasePhosphorylationPatients with advanced solid tumorsAURKATumorsRegulatesCytokinesisTargetsInhibitSubstratesInhibition of Aurora kinaseHuman aurora kinaseVitroPathwaysProteinsInvestigational Aurora A kinase inhibitTumorigenesisMLN8237SpindleAlisertib2018CancersRegulateGeneRegulatorsDrosophilaTyrosine kinaseAntineoplastic AgentsTherapeuticSmall-molecule inhibitorsSelective inhibitor of Aurora B kinaExpression of Aurora kinasesInhibitors of aurora kinasesMaturationCentromerePotentEnzymesMammalianIncreased kinase activityCatalytic domainCancerPolyploidyCellularMitotic progressionXenopusPhaseHighly selectiveAssayTPX2Apoptosis
- Aurora kinase B (AurkB) is usually ubiquitously expressed while Aurora kinase C (AurkC) is usually specifically expressed in gametes and preimplantation embryos. (healthyfutureforkids.com)
- The kinase domains of AurkB and AurkC were responsible for their different ability to phosphorylate Histone H3 Serine 10 (H3S10P) and regulate metaphase timing. (healthyfutureforkids.com)
- Aurora kinases are serine/threonine kinases that are essential for cell proliferation. (wikipedia.org)
- Giet R, Prigent C. Aurora/Ipl1p-related kinases, a new oncogenic family of mitotic serine-threonine kinases. (wikipedia.org)
- 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)
- The Aurora family of serine/threonine kinases is essential for mitosis. (rcsb.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 220.127.116.11) 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 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 18.104.22.168) 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)
- 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 22.214.171.124) 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 126.96.36.199) - 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 188.8.131.52) 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 184.108.40.206) - Aurora B kinase is a protein that functions in the attachment of the mitotic spindle to the centromere. (researchmoz.us)
- 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 220.127.116.11) targeted therapeutics development with respective active and dormant or discontinued projects. (researchmoz.us)
- 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)
- 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)
- 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)
- Aurora kinase is an important class of serine/threonine kinases responsible for the regulation of cell mitosis. (creative-diagnostics.com)
- The human Aurora kinases present a similar domain organization, with a N-terminal domain of 39-129 residues in length, a protein kinase domain and a short C-terminal domain containing 15-20 residues. (wikipedia.org)
- In keeping with many protein kinase inhibitors, this compound is not a monospecific agent, and its cellular specificity remains largely unknown. (nih.gov)
- Kimura, Matsuda, Yoshioka, Okano: Cell cycle-dependent expression and centrosome localization of a third human aurora/Ipl1-related protein kinase, AIK3. (antikoerper-online.de)
- Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. (patentsencyclopedia.com)
- 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)
- 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)
- 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)
- This process relies largely on increased phosphorylation of kinetochore substrates of Aurora B kinase at misaligned versus aligned kinetochores. (elsevier.com)
- Current models explain this differential phosphorylation by spatial changes in the position of substrates relative to a constant pool of kinase at the inner centromere. (elsevier.com)
- Aurora B is enriched at misaligned centromeres in these cells, and the dynamic range of Aurora B substrate phosphorylation at misaligned versus aligned kinetochores is increased. (elsevier.com)
- Our results suggest a feedback mechanism in which Aurora B both regulates and is regulated by chromosome attachment to the spindle, which amplifies the differential phosphorylation of kinetochore substrates and increases the efficiency of error correction. (elsevier.com)
- Like any kinase, Auroras function via the phosphorylation of their substrates. (ugent.be)
- Preliminary evidence indicates that the animal aurora kinase phosphorylation motif is at least partially conserved in plant substrates of aurora kinases. (ugent.be)
- Phosphorylation of MAP65-1 by Arabidopsis Aurora Kinases Is Required for Efficient Cell Cycle Progression. (ugent.be)
- DYRK1A and DYRK 2 (Dual-specificity tyrosine phosphorylation-regulated kinase) inhibitor. (hellobio.com)
Patients with advanced solid tumors1
- 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)
- MLN8054 is a selective small-molecule Aurora A kinase inhibitor that has entered Phase I clinical trials for advanced solid tumors. (pnas.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)
- 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)
- In fact, targeted agents, such as epidermal growth factor receptor inhibitor or antiangiogenic tyrosine kinase inhibitors, do shrink tumors in some patients (i.e., a cytotoxic effect), whereas emerging data suggest that exploitation of the molecular targets of standard chemotherapy (e.g., using ERCC1 as a predictive biomarker for platinum compounds) is now an achievable goal in the clinic. (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)
- 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 VEGF Receptor Tyrosine Kinase Inhibitor Pazopanib in Combination with the MEK Inhibitor Trametinib in Advanced Solid Tumors and Differentiated Thyroid Cancers. (escholarship.org)
- 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)
- The present review focuses on how Aurora B regulates attachments in response to centromere tension. (biochemsoctrans.org)
- Aurora B kinase regulates chromosome-spindle attachments by phosphorylating kinetochore substrates that bind microtubules. (sciencemag.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 B is also one of the essential kinases for normal cytokinesis, which regulates various stages of cytokinesis through different substrate molecules. (creative-diagnostics.com)
- 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)
- 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)
- 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)
- In cytokinesis, Aurora B further aggregates into the intermediate. (creative-diagnostics.com)
- 2005). Whereas the Beta type Aurora of Arabidopsis localizes to centromeric regions, both Alpha type Auroras associate with the prophase spindle, kinetochore fibers during metaphase and anaphase and accumulate at the forming cell plate during cytokinesis, both in tobacco BY-2 cells as in Arabidopsis root cells. (ugent.be)
- 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)
- This review details new developments in the field and analyses the potential of Aurora kinases as anticancer targets. (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)
- 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)
- 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)
- 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)
- 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)
- 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)
- Downstream analyses show that all of the compounds that induce tetraploid senescence inhibit Aurora kinase B (AURKB). (gla.ac.uk)
- Central to this regulation is Aurora B kinase, which phosphorylates kinetochore substrates to promote microtubule turnover. (rupress.org)
- Destabilization of incorrect attachments requires the Ipl1/Aurora B kinase, which phosphorylates kinetochore substrates that directly interact with microtubules. (biochemsoctrans.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)
- To investigate the causality of the aberrant division plane orientations, we are hunting for aurora kinase substrates. (ugent.be)
Inhibition of Aurora kinase1
Human aurora kinase1
- Inhibitors of aurora kinases were shown to induce apoptosis in vitro and in vivo. (nih.gov)
- We report herein the discovery and optimization of a novel series of tricyclic molecules that has led to SAR156497, an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy. (rcsb.org)
- 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)
- 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)
- 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. 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)
- 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)
- 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)
- 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)
- Aurora kinase inhibitor ZM447439 induces apoptosis via mitochondrial pathways. (nih.gov)
- 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)
- 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 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)
- 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)
- Purpose Review aberrations of insulin signaling to atypical proteins kinase C (aPKC) in muscles and liver that generate cardiovascular risk elements, including, weight problems, hypertriglyceridemia, hypercholesterolemia, insulin level of resistance and blood sugar intolerance in type 2 diabetes mellitus (T2DM), and obesity-associated metabolic symptoms (MetSyn). (biomasswars.com)
- as well as the downstream molecule extracellular indication regulated proteins kinase (ERK) 1/2, which induced the upregulation of p53 and Bcl-2-linked X proteins, mediating the next mobile apoptosis and proliferation in IECs. (biomasswars.com)
- Aurora B can regulate this process by acting on checkpoint proteins (Mps1, Mad, Bud). (creative-diagnostics.com)
Investigational Aurora A kinase inhibit1
- Aurora 1) functions in the attachment of the mitotic spindle to the centromere. (wikipedia.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)
- 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)
- Aurora A is important in centrosome function and duplication, mitotic entry and bipolar spindle assembly. (biovision.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)
- Formation of the bipolar spindle requires activation of Aurora-A by the targeting protein for XKLP2 (TPX2). (aacrjournals.org)
- Activated Aurora-A then recruits spindle assembly factors, such as Eg5, that are necessary for the formation of the bipolar spindle. (aacrjournals.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)
- 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)
- 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)
- Consistent with its role in spindle formation, aurora A kinase associates with the centrosome and microtubules. (biologists.org)
- Aurora kinase was first discovered in Drosophila mutants and was named for its abnormal spindle morphology like the Northern Lights. (creative-diagnostics.com)
- In addition, Aurora A is also distributed on the spindle microtubes. (creative-diagnostics.com)
- Deletion of Aurora-A or inhibition of its activity can cause centrosome separation failure, which ultimately leads to the appearance of a monopolar spindle. (creative-diagnostics.com)
- In mammalian cells, interference with Aurora A or TPX2 can cause the formation of a multipolar spindle, indicating that the interaction of TPX2 with Aurora A is a necessary condition for the formation of a bipolar spindle. (creative-diagnostics.com)
- In addition to its role in centrosome separation, maturation, and spindle assembly, Aurora A also promotes cell entry into the dividing phase via Cyclin-B/Cdk1. (creative-diagnostics.com)
- After splitting into the late stage, Aurora B migrates from the centromere to the middle region of the central spindle and the cell cortex of the dividing groove. (creative-diagnostics.com)
- 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)
- 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. (wikipedia.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)
- The Aurora A gene is amplified and overexpressed in cancers originating from multiple tissue types ( 19 ). (pnas.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)
- 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)
- 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)
- Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases. (patentsencyclopedia.com)
- 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)
- 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)
- 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)
- 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)
- The aurora a gene is located on chromosome 20q13. (creative-diagnostics.com)
- The coding gene of Aurora B is located on chromosome 17p13. (creative-diagnostics.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)
- 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)
- 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)
- These include the Drosophila aurora and yeast Ipl1 kinases that are required for centrosome maturation and chromosome segregation. (embopress.org)
- What have these studies taught us about the therapeutic potential of inhibiting this family of kinases? (nih.gov)
- Aurora kinases: shining lights on the therapeutic horizon? (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)
- Our results demonstrate that combined targeting of EGFR and Aurora kinases represents a therapeutic means to activate cell cycle checkpoints and apoptosis in SCCHN. (oncotarget.com)
- The recent identification of novel binding partners and key downstream effectors, together with new small-molecule inhibitors that display efficacy against tumours, heralds an upsurge of interest in these critical kinases. (nih.gov)
- 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)
Selective inhibitor of Aurora B kina2
- 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)
- 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)
Expression of Aurora kinases3
- 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)
- To elucidate the expression of Aurora kinases (AURK) and the anticancer effects of pan-aurora kinase inhibitor Danusertib in hepatocarcinogenesis model in C56Bl6 mice. (jcancer.org)
Inhibitors of aurora kinases1
- 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)
- These findings indicate that in addition to Aurora B regulating kinetochore- microtubule binding, the kinetochore also controls Aurora B recruitment to the inner centromere. (elsevier.com)
- 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, a Potent and Selective Inhibitor of Aurora A Kinase Activity. (pnas.org)
- MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. (selleckchem.com)
- Potent inhibition of MEK1/2 and Aurora A/B kinases by BI 847325 was demonstrated in enzymatic and cellular assays. (aacrjournals.org)
- 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). (merckmillipore.com)
Increased kinase activity1
- 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)
- MLN8054 was the first orally administered Aurora AÃ¢â‚¬â€œselective inhibitor to be tested in human clinical trials for the treatment of colorectal cancer. (biovision.com)
- A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. (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)
- The reduced activity of Aurora B kinase resulted in polyploidy and suppression of cancer cell viability. (oup.com)
- 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)
- Perturbation of Aurora kinase expression or function might lead to cancer. (ed.ac.uk)
- In addition, Aurora kinase is involved in the process of tumor formation, and it has been found that some small molecules that target the aurora kinases have significant anti-cancer effects. (creative-diagnostics.com)
- More specifically, Aurora kinases play a crucial role in cellular division by controlling chromatid segregation. (wikipedia.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)
- 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)
- 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)
- 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)
- The aurora kinases were first identified in 1990 during a cDNA screen of Xenopus eggs. (wikipedia.org)
- In the case of the former, it has been suggested that Aurora A cooperates with the kinase Nek2 in Xenopus to dissolves the structure tethering the cell's centrosomes together. (wikipedia.org)
- Identification of a functional destruction box in the Xenopus laevis aurora-A kinase pEg2. (inserm.fr)
- Aurora A is activated by one or more phosphorylations and its activity peaks during the G2 phase to M phase transition in the cell cycle. (wikipedia.org)
- Aurora A localizes next to the centrosome late in the G1 phase and early in the S phase. (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)
- It is more than 40-fold selective for Aurora A than Aurora B. Phase 1. (selleckchem.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)
- It has recently been demonstrated that Coenzyme A (CoA) is a highly selective ATP-competitive inhibitor of Aurora A kinase. (ucl.ac.uk)
- SP-146 is a highly selective and non-ATP-competitive Aurora A/B inhibitor with IC50 values of 0.316nM 18.975 nM for Aurora A and Aurora B, respectively. (csnpharm.com)
- Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. (selleckchem.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)
- TPX2 was identified by mass spectrometry as a major protein coimmunoprecipitating specifically with Aurora-A from mitotic HeLa cell extracts. (rupress.org)
- Conversely, Aurora-A could be detected in TPX2 immunoprecipitates. (rupress.org)
- Conversely, depletion of Aurora-A by siRNA had no detectable influence on the localization of TPX2. (rupress.org)
- The released TPX2 binds to Aurora A and is phosphorylated, assisting Aurora A to locate on the microtube near the pole. (creative-diagnostics.com)