• 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-A is a serine-threonine kinase implicated in the assembly and maintenance of the mitotic spindle. (unibas.ch)
  • A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
  • An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. (lookformedical.com)
  • Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
  • A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)
  • Aurora kinase A (AURKA), which is a member of serine/threonine kinase family, plays a critical role in regulating mitosis. (encyclopedia.pub)
  • The mammalian Aurora kinase family contains three serine/threonine kinase members that participate in cell division. (rndsystems.com)
  • Mitogen-activated protein kinase kinase kinases (MAPKKKs) are serine-threonine protein kinases that initiate protein kinase signaling cascades. (bvsalud.org)
  • We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. (rcsb.org)
  • Our results suggest the potential for therapeutic application of Aurora kinase B inhibitors in the treatment of Group 3 medulloblastoma. (oncotarget.com)
  • In addition, Vertex could earn additional milestone payments for the development of Aurora kinase inhibitors outside the area of oncology. (vrtx.com)
  • Aurora kinases are implicated in the onset and progression of many different human cancers, and novel Aurora kinase inhibitors such as VX-680 have the potential to play an important future role in the treatment and management of a wide range of tumor types. (vrtx.com)
  • We are pleased to enter this collaboration with Merck, which shares our vision of Aurora kinase inhibitors as a class of drugs that may have the potential to transform the future of cancer treatment," said Joshua Boger, Ph.D., Chairman and CEO of Vertex. (vrtx.com)
  • Indeed, we observed partial restoration of dexamethasone sensitivity with a combination of dexamethasone and inhibitors targeting either these kinases or β-catenin. (lu.se)
  • Further progression from adenoma-to-carcinoma is frequently associated with 20q gain and overexpression of Aurora kinase A (AURKA). (vu.nl)
  • As discussed in detail below, biochemical, biophysical, structural, and cellular evidences have shown that the redox modification of the cysteine residues of AURKA affects both the phosphorylation state of Thr288 and the conformation state of structural elements critical for the kinase activity, leading to the regulation of AURKA activity. (encyclopedia.pub)
  • So far, several lines of evidence have shown that H 2 O 2 -induced regulation of the AURKA activity, possibly through direct oxidation of Cys290 present in the activation segment of the kinase domain. (encyclopedia.pub)
  • As the spindle formation is the process that is mainly governed by the kinase activity of AURKA, these observations led to the hypothesis that H 2 O 2 regulates the activity of AURKA [ 27 ] [ 28 ] . (encyclopedia.pub)
  • By using a direct in vivo shRNA screen, we show that liver cancer cells that have mutations in the gene encoding the tumor suppressor protein p53 (Trp53 in mice and TP53 in humans) and that are driven by the oncoprotein NRAS become addicted to MYC stabilization via a mechanism mediated by aurora kinase A (AURKA). (scite.ai)
  • As a molecular mechanism, we demonstrate that PTPRD interacts with aurora kinase A (AURKA), an oncogenic protein that is over-expressed in multiple forms of cancer, including neuroblastoma. (biomedcentral.com)
  • Aurora 2) functions during prophase of mitosis and is required for correct duplication and separation of the centrosomes (the microtubule organising centres in eukaryotic cells). (wikipedia.org)
  • Roles of Aurora Kinases in Mitosis and Tumorigenesis" (PDF). (wikipedia.org)
  • The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. (rcsb.org)
  • Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. (lookformedical.com)
  • An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
  • An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. (lookformedical.com)
  • One of the key regulatory kinases involved in multiple stages of mitosis is Aurora kinase B. We hypothesized that medulloblastoma cells that overexpress MYC would be uniquely sensitized to the apoptotic effects of Aurora B inhibition. (oncotarget.com)
  • Nbl1 (novel Borealin-like 1) physically associates with known CPC components, affects the kinase activity and stability of the S. pombe Aurora B homologue, Ark1, colocalizes with known CPC subunits during mitosis, and shows sequence similarity to human Borealin. (uky.edu)
  • The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacological profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. (rcsb.org)
  • LY3295668 is a selective inhibitor of Aurora A with Kis of 0.8 nM and 1038 nM for Aurora A and B, respectively. (targetmol.com)
  • PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and. (targetmol.com)
  • SCH-1473759 hydrochloride is an inhibitor of aurora(aurora A and B with IC50s of 4 and 13 nM, respectively). (targetmol.com)
  • TC-A 2317 hydrochloride is an inhibitor of Aurora kinase A with a Ki of 1.2 nM compared to Aurora kinase B with a Ki of 101 nM. (targetmol.com)
  • In this study, we investigated the effect of AKI603, a novel small molecule inhibitor of Aurora kinase A (AurA) to overcome resistance mediated by BCR-ABL-T315I mutation. (scite.ai)
  • Aurora A activity is positively-regulated by the spindle protein TPX2, and has recently been shown to be a target for thiol-containing molecules, such as Coenzyme A. Aurora B (a.k.a. (wikipedia.org)
  • Aurora 1) functions in the attachment of the mitotic spindle to the centromere. (wikipedia.org)
  • Here we show that human Aurora-A binds to TPX2, a prominent component of the spindle apparatus. (unibas.ch)
  • Binding studies demonstrated that the NH2 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. (unibas.ch)
  • In turn, Aurora-A might regulate the function of TPX2 during spindle assembly. (unibas.ch)
  • The protein encoded by this gene is a cell cycle-regulated kinase that appears to be involved in microtubule formation and/or stabilization at the spindle pole during chromosome segregation. (antikoerper-online.de)
  • Evidence that the Ipl1-Sli15 (Aurora kinase-INCENP) complex promotes chromosome bi-orientation by altering kinetochore-spindle pole connections. (pasteur.fr)
  • In yeast, the ortholog of the Aurora B-INCENP protein kinase complex (Ipl1-Sli15) may have a role in this crucial process, because it is necessary to prevent attachment of sister kinetochores to microtubules from the same spindle pole. (pasteur.fr)
  • Those transformed cells form tumours when implanted in immunodeficient mice, indicating that the kinase is an oncogene. (lookformedical.com)
  • In this paper we analyzed the participation of Aurora kinase B (AurKB) in the DENV replicative cycle using the specific AurKB inhibitor ZM447439. (mendeley.com)
  • Aurora A overexpression in many malignant tumor types suggests that it may be directly involved in NEOPLASTIC CELL TRANSFORMATION. (lookformedical.com)
  • In human, aurora-A has focused a lot of attention, since its overexpression has been found to be correlated with the grade of various solid tumours. (lookformedical.com)
  • However, overexpression of aurora-A in particular cell lines such as NIH3T3 is sufficient to induce growth on soft agar. (lookformedical.com)
  • MYC overexpression sensitized medulloblastoma cells to cell death upon Aurora B inhibition. (oncotarget.com)
  • Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1. (targetmol.com)
  • We analyzed the clinical data and performed immunohistochemistry for Epidermal growth factor receptor (EGFR) and Aurora kinase A (Aurora-A) expression in 180 SCCHN patients. (oncotarget.com)
  • The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (lookformedical.com)
  • Alisertib inhibits the interaction between N-myc and its stabilizing factor Aurora-A, inhibiting N-myc signaling, and suppressing tumor growth. (unitn.it)
  • Finally, we evaluate a functional interaction between Fry and NDR1 kinase, providing evidence of an evolutionarily conserved complex required for morphogenesis. (nature.com)
  • Aurora Kinases" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (rush.edu)
  • 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)
  • Preclinical results for VX-680 reported by Vertex scientists in early 2004 demonstrated for the first time that a compound targeting the Aurora mechanism could induce tumor regression in human models of solid tumor cancers. (vrtx.com)
  • In Merck, we have a partner that is a global leader in the development and commercialization of innovative medicines, and one with the breadth of capabilities and resources that we expect to be required to establish the clinical benefit of an Aurora kinase inhibitor across a spectrum of solid tumors and hematologic cancers. (vrtx.com)
  • The expression of Aurora-A phosphorylation-mimetic mutants of NDEL1 efficiently rescued the defects of centrosomal maturation and separation which are characteristic of Aurora-A-depleted cells. (elsevierpure.com)
  • Our findings suggest that Aurora-A-mediated phosphorylation of NDEL1 is essential for centrosomal separation and centrosomal maturation and for mitotic entry. (elsevierpure.com)
  • Conclusions: Although the study did not meet its primary endpoint, a subset of patients with advanced prostate cancer and molecular features supporting Aurora-A and N-myc activation achieved significant clinical benefit from single-agent alisertib. (unitn.it)
  • Whitehouse Station, NJ and Cambridge, MA, June 22, 2004 -- Merck & Co., Inc. (NYSE: MRK) and Vertex Pharmaceuticals Incorporated (Nasdaq: VRTX) announced today that they have entered into a global collaboration to develop and commercialize VX-680, Vertex's lead Aurora kinase inhibitor that is expected to enter clinical development this year for the treatment of cancer. (vrtx.com)
  • In addition, the companies will conduct a joint research program to characterize VX-680's activity across a broad range of cancer types as well as to identify follow-on drug candidates directed at Aurora kinases, using molecular profiling approaches and microarray technologies pioneered by Merck. (vrtx.com)
  • This agreement places a significant value on our innovations in the area of Aurora kinases and cancer, and highlights Vertex's progress in realizing our 2004 business development and collaborative revenue objectives," Boger added. (vrtx.com)
  • The human Aurora kinases present a similar domain organization, with a N-terminal domain of 39-129 residues in length, a related Ser/Thr protein kinase domain and a short C-terminal domain containing 15-20 residues. (wikipedia.org)
  • MK-0457, an Aurora kinase and BCR-ABL inhibitor, was studied on a Phase I/II study in 77 patients with refractory hematologic malignancies. (northwestern.edu)
  • AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I). (targetmol.com)
  • These kinases lead to β-catenin stabilization through phosphorylation-dependent inactivation of GSK-3β either directly or indirectly. (lu.se)
  • Aurora inhibitor 1 is a potent Aurora inhibitor (IC50: ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase). (targetmol.com)
  • MBM-17 is a potent inhibitor of NIMA-related kinase 2 (Nek2,IC50 of 3 nM). (targetmol.com)
  • This collaboration unites Vertex's drug discovery leadership targeting Aurora kinases with Merck's proprietary molecular profiling technologies and clinical development infrastructure in oncology. (vrtx.com)
  • Interestingly, NDEL1 phosphorylated by Aurora-A was rapidly downregulated thereafter by ubiquitination-mediated protein degradation. (elsevierpure.com)
  • We observed that dexamethasone exposure caused upregulation of Aurora kinase and its various downstream effector kinases such as JAK, p38, mTOR, and S6K. (lu.se)
  • TPX2 was identified by mass spectrometry as a major protein coimmunoprecipitating specifically with Aurora-A from mitotic HeLa cell extracts. (unibas.ch)
  • Here, we show that Aurora-A phosphorylates NDEL1 at Ser251 at the beginning of mitotic entry. (elsevierpure.com)
  • Covalent Aurora A regulation by the metabolic integrator coenzyme A". Redox Biology. (wikipedia.org)
  • MK-0457 is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases. (targetmol.com)
  • The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)
  • DMC promotes abnormal cell division by inhibiting the synthesis of the cell cycle checkpoint kinase Protein phosphatase 2A (PP2A), leading to increased cell vulnerability to DNA damage, disordered replication, and death. (bvsalud.org)
  • Aurora C (AURKC) works in germ-line cells and little is known about its function. (wikipedia.org)
  • Here we report that a circumscribed exposure to the aurora kinase inhibitor, VX-680, selectively kills cells that overexpress Myc. (nih.gov)
  • The kinase inhibition does not alter the viral protein production/secretion or genome replication but impaired the viral yield without altering the percentage of infected cells. (mendeley.com)
  • Differentially expressed epigenome modifiers, including aurora kinases A and B, in immune cells in rheumatoid arthritis in humans and mouse models. (rush.edu)
  • The specific inhibition of Aurora kinase B was achieved in MYC- overexpressing medulloblastoma cells with AZD1152-HQPA. (oncotarget.com)
  • Nuclear expression of protein kinase CK2α is reportedly elevated in human carcinomas, but mechanisms underlying its variable localization in cells are poorly understood. (bvsalud.org)
  • Hier sind Aurora Kinase A ELISA Kits für eine Vielzahl von Species wie anti-Human Aurora Kinase A, anti-Mouse Aurora Kinase A, anti-Rat Aurora Kinase A zu finden. (antikoerper-online.de)
  • Comparing pan-Aurora kinase and Aurora-A targeting hints towards a strong and clinically relevant biological effect mediated via Aurora kinase B. Taken together, our findings characterize a new poor risk group in SCCHN patients defined by elevated EGFR and Aurora-A protein expression. (oncotarget.com)
  • Below are the most recent publications written about "Aurora Kinases" by people in Profiles. (rush.edu)
  • Combined Aurora kinase and EGFR targeting using a monoclonal anti-EGFR antibody was more effective compared to single EGFR and Aurora kinase inhibition. (oncotarget.com)