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
Aurora Kinase B
Aurora Kinase C
Protein-Serine-Threonine Kinases
Mitosis
Protein Kinases
Phosphatidylinositol 3-Kinases
Phosphotransferases that catalyzes the conversion of 1-phosphatidylinositol to 1-phosphatidylinositol 3-phosphate. Many members of this enzyme class are involved in RECEPTOR MEDIATED SIGNAL TRANSDUCTION and regulation of vesicular transport with the cell. Phosphatidylinositol 3-Kinases have been classified both according to their substrate specificity and their mode of action within the cell.
MAP Kinase Signaling System
An intracellular signaling system involving the MAP kinase cascades (three-membered protein kinase cascades). Various upstream activators, which act in response to extracellular stimuli, trigger the cascades by activating the first member of a cascade, MAP KINASE KINASE KINASES; (MAPKKKs). Activated MAPKKKs phosphorylate MITOGEN-ACTIVATED PROTEIN KINASE KINASES which in turn phosphorylate the MITOGEN-ACTIVATED PROTEIN KINASES; (MAPKs). The MAPKs then act on various downstream targets to affect gene expression. In mammals, there are several distinct MAP kinase pathways including the ERK (extracellular signal-regulated kinase) pathway, the SAPK/JNK (stress-activated protein kinase/c-jun kinase) pathway, and the p38 kinase pathway. There is some sharing of components among the pathways depending on which stimulus originates activation of the cascade.
Spindle Apparatus
Phosphorylation
Calcium-Calmodulin-Dependent Protein Kinases
A CALMODULIN-dependent enzyme that catalyzes the phosphorylation of proteins. This enzyme is also sometimes dependent on CALCIUM. A wide range of proteins can act as acceptor, including VIMENTIN; SYNAPSINS; GLYCOGEN SYNTHASE; MYOSIN LIGHT CHAINS; and the MICROTUBULE-ASSOCIATED PROTEINS. (From Enzyme Nomenclature, 1992, p277)
Kinetochores
src-Family Kinases
A PROTEIN-TYROSINE KINASE family that was originally identified by homology to the Rous sarcoma virus ONCOGENE PROTEIN PP60(V-SRC). They interact with a variety of cell-surface receptors and participate in intracellular signal transduction pathways. Oncogenic forms of src-family kinases can occur through altered regulation or expression of the endogenous protein and by virally encoded src (v-src) genes.
Organophosphates
Carbon-containing phosphoric acid derivatives. Included under this heading are compounds that have CARBON atoms bound to one or more OXYGEN atoms of the P(=O)(O)3 structure. Note that several specific classes of endogenous phosphorus-containing compounds such as NUCLEOTIDES; PHOSPHOLIPIDS; and PHOSPHOPROTEINS are listed elsewhere.
Cell Cycle Proteins
Proteins that control the CELL DIVISION CYCLE. This family of proteins includes a wide variety of classes, including CYCLIN-DEPENDENT KINASES, mitogen-activated kinases, CYCLINS, and PHOSPHOPROTEIN PHOSPHATASES as well as their putative substrates such as chromatin-associated proteins, CYTOSKELETAL PROTEINS, and TRANSCRIPTION FACTORS.
M Phase Cell Cycle Checkpoints
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.
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).
p38 Mitogen-Activated Protein Kinases
A mitogen-activated protein kinase subfamily that regulates a variety of cellular processes including CELL GROWTH PROCESSES; CELL DIFFERENTIATION; APOPTOSIS; and cellular responses to INFLAMMATION. The P38 MAP kinases are regulated by CYTOKINE RECEPTORS and can be activated in response to bacterial pathogens.
Polyploidy
Cyclic AMP-Dependent Protein Kinases
Mitogen-Activated Protein Kinase 1
Chondroma
HeLa Cells
Aneugens
Microtubule-Associated Proteins
Apoptosis
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
Pyrimidines
Cell Cycle
The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.
Histones
p21-Activated Kinases
CDC2 Protein Kinase
Phosphoprotein with protein kinase activity that functions in the G2/M phase transition of the CELL CYCLE. It is the catalytic subunit of the MATURATION-PROMOTING FACTOR and complexes with both CYCLIN A and CYCLIN B in mammalian cells. The maximal activity of cyclin-dependent kinase 1 is achieved when it is fully dephosphorylated.
Mitogen-Activated Protein Kinase Kinases
A serine-threonine protein kinase family whose members are components in protein kinase cascades activated by diverse stimuli. These MAPK kinases phosphorylate MITOGEN-ACTIVATED PROTEIN KINASES and are themselves phosphorylated by MAP KINASE KINASE KINASES. JNK kinases (also known as SAPK kinases) are a subfamily.
JNK Mitogen-Activated Protein Kinases
Cell Cycle Checkpoints
Regulatory signaling systems that control the progression through the CELL CYCLE. They ensure that the cell has completed, in the correct order and without mistakes, all the processes required to replicate the GENOME and CYTOPLASM, and divide them equally between two daughter cells. If cells sense they have not completed these processes or that the environment does not have the nutrients and growth hormones in place to proceed, then the cells are restrained (or "arrested") until the processes are completed and growth conditions are suitable.
Mitogen-Activated Protein Kinase 3
Pyrazoles
Anaphase
Mutation
Protein-Tyrosine Kinases
Microtubules
Collagen Type XI
Chromosomal Proteins, Non-Histone
Cyclin-Dependent Kinases
Blastodisc
A small whitish spot on the surface of the EGG YOLK where cleavage begins. Upon fertilization the cytoplasm streams from the vegetal pole away from the yolk to the animal pole where cleavage will occur. This germinal area eventually flattens into a layer of cells (BLASTODERM) that covers the yolk completely.
Creatine Kinase
A transferase that catalyzes formation of PHOSPHOCREATINE from ATP + CREATINE. The reaction stores ATP energy as phosphocreatine. Three cytoplasmic ISOENZYMES have been identified in human tissues: the MM type from SKELETAL MUSCLE, the MB type from myocardial tissue and the BB type from nervous tissue as well as a mitochondrial isoenzyme. Macro-creatine kinase refers to creatine kinase complexed with other serum proteins.
MAP Kinase Kinase Kinases
Enzyme Inhibitors
Potoroidae
RNA, Small Interfering
Small double-stranded, non-protein coding RNAs (21-31 nucleotides) involved in GENE SILENCING functions, especially RNA INTERFERENCE (RNAi). Endogenously, siRNAs are generated from dsRNAs (RNA, DOUBLE-STRANDED) by the same ribonuclease, Dicer, that generates miRNAs (MICRORNAS). The perfect match of the siRNAs' antisense strand to their target RNAs mediates RNAi by siRNA-guided RNA cleavage. siRNAs fall into different classes including trans-acting siRNA (tasiRNA), repeat-associated RNA (rasiRNA), small-scan RNA (scnRNA), and Piwi protein-interacting RNA (piRNA) and have different specific gene silencing functions.
eIF-2 Kinase
A dsRNA-activated cAMP-independent protein serine/threonine kinase that is induced by interferon. In the presence of dsRNA and ATP, the kinase autophosphorylates on several serine and threonine residues. The phosphorylated enzyme catalyzes the phosphorylation of the alpha subunit of EUKARYOTIC INITIATION FACTOR-2, leading to the inhibition of protein synthesis.
Casein Kinase II
Casein Kinases
A group of protein-serine-threonine kinases that was originally identified as being responsible for the PHOSPHORYLATION of CASEINS. They are ubiquitous enzymes that have a preference for acidic proteins. Casein kinases play a role in SIGNAL TRANSDUCTION by phosphorylating a variety of regulatory cytoplasmic and regulatory nuclear proteins.
Protein Binding
Blotting, Western
Pyruvate Kinase
Ribosomal Protein S6 Kinases
A family of protein serine/threonine kinases which act as intracellular signalling intermediates. Ribosomal protein S6 kinases are activated through phosphorylation in response to a variety of HORMONES and INTERCELLULAR SIGNALING PEPTIDES AND PROTEINS. Phosphorylation of RIBOSOMAL PROTEIN S6 by enzymes in this class results in increased expression of 5' top MRNAs. Although specific for RIBOSOMAL PROTEIN S6 members of this class of kinases can act on a number of substrates within the cell. The immunosuppressant SIROLIMUS inhibits the activation of ribosomal protein S6 kinases.
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Signal Transduction
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Amino Acid Sequence
MAP Kinase Kinase 1
Centromere
Receptor Protein-Tyrosine Kinases
Thymidine Kinase
Extracellular Signal-Regulated MAP Kinases
A mitogen-activated protein kinase subfamily that is widely expressed and plays a role in regulation of MEIOSIS; MITOSIS; and post mitotic functions in differentiated cells. The extracellular signal regulated MAP kinases are regulated by a broad variety of CELL SURFACE RECEPTORS and can be activated by certain CARCINOGENS.
MAP Kinase Kinase 4
Microtubule-Organizing Center
Gene Expression Regulation, Enzymologic
Enzyme Activation
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.
Nuclear Proteins
1-Phosphatidylinositol 4-Kinase
Phosphotransferases (Alcohol Group Acceptor)
Neoplasms
Glycogen Synthase Kinase 3
Mitogen-Activated Protein Kinases
A superfamily of PROTEIN-SERINE-THREONINE KINASES that are activated by diverse stimuli via protein kinase cascades. They are the final components of the cascades, activated by phosphorylation by MITOGEN-ACTIVATED PROTEIN KINASE KINASES, which in turn are activated by mitogen-activated protein kinase kinase kinases (MAP KINASE KINASE KINASES).
CDC2-CDC28 Kinases
Proto-Oncogene Proteins
Meiosis
Xenograft Model Antitumor Assays
Isoenzymes
I-kappa B Kinase
rho-Associated Kinases
A group of intracellular-signaling serine threonine kinases that bind to RHO GTP-BINDING PROTEINS. They were originally found to mediate the effects of rhoA GTP-BINDING PROTEIN on the formation of STRESS FIBERS and FOCAL ADHESIONS. Rho-associated kinases have specificity for a variety of substrates including MYOSIN-LIGHT-CHAIN PHOSPHATASE and LIM KINASES.
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).
Chromosomes
Protein Kinase C-delta
Cell Division
Protein Kinase C-alpha
Transfection
Intracellular Signaling Peptides and Proteins
Proteins and peptides that are involved in SIGNAL TRANSDUCTION within the cell. Included here are peptides and proteins that regulate the activity of TRANSCRIPTION FACTORS and cellular processes in response to signals from CELL SURFACE RECEPTORS. Intracellular signaling peptide and proteins may be part of an enzymatic signaling cascade or act through binding to and modifying the action of other signaling factors.
Drug Resistance, Neoplasm
Models, Biological
Gene Expression Regulation, Neoplastic
Molecular Targeted Therapy
G2 Phase
Cyclin B1
Cell Survival
Diacylglycerol Kinase
Drug Screening Assays, Antitumor
Binding Sites
AMP-Activated Protein Kinases
Intracellular signaling protein kinases that play a signaling role in the regulation of cellular energy metabolism. Their activity largely depends upon the concentration of cellular AMP which is increased under conditions of low energy or metabolic stress. AMP-activated protein kinases modify enzymes involved in LIPID METABOLISM, which in turn provide substrates needed to convert AMP into ATP.
Dose-Response Relationship, Drug
Mice, Nude
Chordata
Tumor Cells, Cultured
RNA, Messenger
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Imidazoles
Substrate Specificity
Proto-Oncogene Proteins c-akt
Saccharomycetales
Serine
Focal Adhesion Kinase 1
A non-receptor protein tyrosine kinase that is localized to FOCAL ADHESIONS and is a central component of integrin-mediated SIGNAL TRANSDUCTION PATHWAYS. Focal adhesion kinase 1 interacts with PAXILLIN and undergoes PHOSPHORYLATION in response to adhesion of cell surface integrins to the EXTRACELLULAR MATRIX. Phosphorylated p125FAK protein binds to a variety of SH2 DOMAIN and SH3 DOMAIN containing proteins and helps regulate CELL ADHESION and CELL MIGRATION.
Down-Regulation
Pyridines
Cell Transformation, Neoplastic
Protein Structure, Tertiary
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
Myosin-Light-Chain Kinase
An enzyme that phosphorylates myosin light chains in the presence of ATP to yield myosin-light chain phosphate and ADP, and requires calcium and CALMODULIN. The 20-kDa light chain is phosphorylated more rapidly than any other acceptor, but light chains from other myosins and myosin itself can act as acceptors. The enzyme plays a central role in the regulation of smooth muscle contraction.
Janus Kinase 2
A Janus kinase subtype that is involved in signaling from GROWTH HORMONE RECEPTORS; PROLACTIN RECEPTORS; and a variety of CYTOKINE RECEPTORS such as ERYTHROPOIETIN RECEPTORS and INTERLEUKIN RECEPTORS. Dysregulation of Janus kinase 2 due to GENETIC TRANSLOCATIONS have been associated with a variety of MYELOPROLIFERATIVE DISORDERS.
Oocytes
Recombinant Fusion Proteins
Focal Adhesion Protein-Tyrosine Kinases
Microscopy, Fluorescence
Ribosomal Protein S6 Kinases, 90-kDa
A family of ribosomal protein S6 kinases that are structurally distinguished from RIBOSOMAL PROTEIN S6 KINASES, 70-KDA by their apparent molecular size and the fact they contain two functional kinase domains. Although considered RIBOSOMAL PROTEIN S6 KINASES, members of this family are activated via the MAP KINASE SIGNALING SYSTEM and have been shown to act on a diverse array of substrates that are involved in cellular regulation such as RIBOSOMAL PROTEIN S6 and CAMP RESPONSE ELEMENT-BINDING PROTEIN.
Tyrosine
Reverse Transcriptase Polymerase Chain Reaction
Protein Kinase C-epsilon
A protein kinase C subtype that was originally characterized as a CALCIUM-independent, serine-threonine kinase that is activated by PHORBOL ESTERS and DIACYLGLYCEROLS. It is targeted to specific cellular compartments in response to extracellular signals that activate G-PROTEIN-COUPLED RECEPTORS; TYROSINE KINASE RECEPTORS; and intracellular protein tyrosine kinase.
Sequence Alignment
The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.
Chromosomal Instability
Base Sequence
MAP Kinase Kinase Kinase 1
Calcium-Calmodulin-Dependent Protein Kinase Type 2
A multifunctional calcium-calmodulin-dependent protein kinase subtype that occurs as an oligomeric protein comprised of twelve subunits. It differs from other enzyme subtypes in that it lacks a phosphorylatable activation domain that can respond to CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE KINASE.
Saccharomyces cerevisiae Proteins
Tumor Suppressor Protein p53
Catalytic Domain
Protein Kinase C beta
PKC beta encodes two proteins (PKCB1 and PKCBII) generated by alternative splicing of C-terminal exons. It is widely distributed with wide-ranging roles in processes such as B-cell receptor regulation, oxidative stress-induced apoptosis, androgen receptor-dependent transcriptional regulation, insulin signaling, and endothelial cell proliferation.
Cell cycle-dependent expression and centrosome localization of a third human aurora/Ipl1-related protein kinase, AIK3. (1/1165)
We earlier isolated cDNAs encoding novel human protein kinases AIK and AIK2 sharing high amino acid sequence identities with Drosophila Aurora and Saccharomyces cerevisiae Ipl1 kinases whose mutations cause abnormal chromosome segregation. In the present study, a third human cDNA (AIK3) highly homologous to aurora/IPL1 was isolated, and the nucleotide sequence was determined. This cDNA encodes 309 amino acids with a predicted molecular mass of 35.9 kDa. C-terminal kinase domain of AIK3 protein shares high amino acid sequence identities with those of Aurora/Ipl1 family protein kinases including human AIK, human AIK2, Xenopus pEg2, Drosophila Aurora, and yeast Ipl1, whereas the N-terminal domain of AIK3 protein shares little homology with any other Aurora/Ipl1 family members. AIK3 gene was assigned to human chromosome 19q13.43, which is a frequently deleted or rearranged region in several tumor tissues, by fluorescence in situ hybridization, somatic cell hybrid panel, and radiation hybrid cell panel. Northern blot analyses revealed that AIK3 expression was limited to testis. The expression levels of AIK3 in several cancer cell lines were elevated severalfold compared with normal fibroblasts. In HeLa cells, the endogenous AIK3 protein level is low in G1/S, accumulates during G2/M, and reduces after mitosis. Immunofluorescence studies using a specific antibody have shown that AIK3 is localized to centrosome during mitosis from anaphase to cytokinesis. These results suggest that AIK3 may play a role(s) in centrosome function at later stages of mitosis. (+info)The conserved protein kinase Ipl1 regulates microtubule binding to kinetochores in budding yeast. (2/1165)
Chromosome segregation depends on kinetochores, the structures that mediate chromosome attachment to the mitotic spindle. We isolated mutants in IPL1, which encodes a protein kinase, in a screen for budding yeast mutants that have defects in sister chromatid separation and segregation. Cytological tests show that ipl1 mutants can separate sister chromatids but are defective in chromosome segregation. Kinetochores assembled in extracts from ipl1 mutants show altered binding to microtubules. Ipl1p phosphorylates the kinetochore component Ndc10p in vitro and we propose that Ipl1p regulates kinetochore function via Ndc10p phosphorylation. Ipl1p localizes to the mitotic spindle and its levels are regulated during the cell cycle. This pattern of localization and regulation is similar to that of Ipl1p homologs in higher eukaryotes, such as the human aurora2 protein. Because aurora2 has been implicated in oncogenesis, defects in kinetochore function may contribute to genetic instability in human tumors. (+info)Novel protein kinases Ark1p and Prk1p associate with and regulate the cortical actin cytoskeleton in budding yeast. (3/1165)
Ark1p (actin regulating kinase 1) was identified as a yeast protein that binds to Sla2p, an evolutionarily conserved cortical actin cytoskeleton protein. Ark1p and a second yeast protein, Prk1p, contain NH2-terminal kinase domains that are 70% identical. Together with six other putative kinases from a number of organisms, these proteins define a new protein kinase family that we have named the Ark family. Lack of both Ark1p and Prk1p resulted in the formation of large cytoplasmic actin clumps and severe defects in cell growth. These defects were rescued by wild-type, but not by kinase-dead versions of the proteins. Elevated levels of either Ark1p or Prk1p caused a number of actin and cell morphological defects that were not observed when the kinase-dead versions were overexpressed instead. Ark1p and Prk1p were shown to localize to actin cortical patches, making these two kinases the first signaling proteins demonstrated to be patch components. These results suggest that Ark1p and Prk1p may be downstream effectors of signaling pathways that control actin patch organization and function. Furthermore, results of double-mutant analyses suggest that Ark1p and Prk1p function in overlapping but distinct pathways that regulate the cortical actin cytoskeleton. (+info)Centrosomal kinase AIK1 is overexpressed in invasive ductal carcinoma of the breast. (4/1165)
A centrosomal serine/threonine kinase, AIK1(3)/breast tumor amplified kinase/aurora2, which was recently identified as an oncogene, shows high amino acid identity with chromosome segregation kinases, fly Aurora, and yeast Ipl1. Immunohistochemical analyses of invasive ductal adenocarcinomas of the breast revealed that overexpression of AIK1 was observed in 94% of the cases, irrespective of the histopathological type, whereas the protein was not detected in normal ductal and lobular cells. Benign breast lesions including fibrocystic disease and fibroadenoma (epithelial components) displayed weakly detectable AIK1 expression in part of the lesions. This is the first immunohistochemical report of AIK1 expression in primary human breast carcinomas. Although the physiological function(s) of AIK1 kinase during cell division remains to be determined, the markedly high positivity of AIK1 staining in the cancer lesions suggested a possible involvement of its overexpression in the tumorigenesis of some of breast cancer cells. (+info)The Xenopus laevis aurora-related protein kinase pEg2 associates with and phosphorylates the kinesin-related protein XlEg5. (5/1165)
We have previously reported on the cloning of XlEg5, a Xenopus laevis kinesin-related protein from the bimC family (Le Guellec, R., Paris, J., Couturier, A., Roghi, C., and Philippe, M. (1991) Mol. Cell. Biol. 11, 3395-3408) as well as pEg2, an Aurora-related serine/threonine kinase (Roghi, C., Giet, R., Uzbekov, R., Morin, N., Chartrain, I., Le Guellec, R., Couturier, A., Doree, M., Philippe, M., and Prigent, C. (1998) J. Cell Sci. 111, 557-572). Inhibition of either XlEg5 or pEg2 activity during mitosis in Xenopus egg extract led to monopolar spindle formation. Here, we report that in Xenopus XL2 cells, pEg2 and XlEg5 are both confined to separated centrosomes in prophase, and then to the microtubule spindle poles. We also show that pEg2 co-immunoprecipitates with XlEg5 from egg extracts and XL2 cell lysates. Both proteins can directly interact in vitro, but also through the two-hybrid system. Furthermore immunoprecipitated pEg2 were found to remain active when bound to the beads and phosphorylate XlEg5 present in the precipitate. Two-dimensional mapping of XlEg5 tryptic peptides phosphorylated in vivo first confirmed that XlEg5 was phosphorylated by p34(cdc2) and next revealed that in vitro pEg2 kinase phosphorylated XlEg5 on the same stalk domain serine residue that was phosphorylated in metabolically labeled XL2 cells. The kinesin-related XlEg5 is to our knowledge the first in vivo substrate ever reported for an Aurora-related kinase. (+info)Stu-7/air-2 is a C. elegans aurora homologue essential for chromosome segregation during embryonic and post-embryonic development. (6/1165)
We have isolated a new sterile uncoordinated C. elegans mutant, stu-7, which is defective in post-embryonic cell divisions in a regionally-specific fashion. The anterior of the worm is relatively unaffected whereas the mid-body and/or posterior are markedly thin, often resulting in worms having a central 'waist'. We have cloned stu-7 and found that it encodes a member of the recently expanding aurora sub-family of serine/threonine kinases. Elimination of maternal as well as zygotic stu-7 expression reveals that stu-7 is essential for mitosis from the first embryonic cell cycle onwards and is required for chromosome segregation though not for centrosome separation or for setting up a bipolar spindle. Multicopy expression of stu-7 also causes mitotic defects, suggesting that the level of this protein must be tightly controlled in order to maintain genetic stability during development. (+info)Cdc20 associates with the kinase aurora2/Aik. (7/1165)
Cdc20/fizzy family proteins are involved in activation of the anaphase-promoting complex/cyclosome, which catalyzes the ubiquitin-dependent proteolysis of cell cycle regulatory proteins such as anaphase inhibitors and mitotic cyclins, leading to chromosome segregation and exit from mitosis. Previous work has shown that human Cdc20 (hCdc20/p55CDC) associates with one or more kinases. We report here that Cdc20-associated myelin basic protein kinase activity peaks sharply in early M phase (embryonic cells) or in G2 phase (somatic cells). In HeLa cells, Cdc20 is associated with the kinase aurora2/Aik. Aurora2/Aik is a member of the aurora/Ipl1 family of kinases that, like Cdc20, previously has been shown to be localized at mitotic spindle poles and is involved in regulating chromosome segregation and maintaining genomic stability. The demonstration that Cdc20 is associated with aurora2/Aik suggests that some function of Cdc20 is carried out or regulated through its association with aurora2/Aik. (+info)Sli15 associates with the ipl1 protein kinase to promote proper chromosome segregation in Saccharomyces cerevisiae. (8/1165)
The conserved Ipl1 protein kinase is essential for proper chromosome segregation and thus cell viability in the budding yeast Saccharomyces cerevisiae. Its human homologue has been implicated in the tumorigenesis of diverse forms of cancer. We show here that sister chromatids that have separated from each other are not properly segregated to opposite poles of ipl1-2 cells. Failures in chromosome segregation are often associated with abnormal distribution of the spindle pole-associated Nuf2-GFP protein, thus suggesting a link between potential spindle pole defects and chromosome missegregation in ipl1 mutant cells. A small fraction of ipl1-2 cells also appears to be defective in nuclear migration or bipolar spindle formation. Ipl1 associates, probably directly, with the novel and essential Sli15 protein in vivo, and both proteins are localized to the mitotic spindle. Conditional sli15 mutant cells have cytological phenotypes very similar to those of ipl1 cells, and the ipl1-2 mutation exhibits synthetic lethal genetic interaction with sli15 mutations. sli15 mutant phenotype, like ipl1 mutant phenotype, is partially suppressed by perturbations that reduce protein phosphatase 1 function. These genetic and biochemical studies indicate that Sli15 associates with Ipl1 to promote its function in chromosome segregation. (+info)
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October | 2015 | Thrombin Inhibitors
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MK-0457 Alone and in Combination With Docetaxel Inhibits Ovarian Cancer Growth In Vivo | Libbys H*O*P*E*
The Aurora kinase inhibitor ZM447439 accelerates first meiosis in mouse oocytes by overriding the spindle assembly checkpoint -...
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Aurora B-INCENP localization at centromeres/inner kinetochores is required for chromosome bi-orientation in budding yeast<...
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Divisive Tension | Science Signaling
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Aurora kinase
... there are three classes of aurora kinases in multicellular organisms, including humans: Aurora A (a.k.a. Aurora 2) functions ... Aurora kinases are serine/threonine kinases that are essential for cell proliferation. They are phosphotransferase enzymes that ... 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 kinase B
Aurora kinase Aurora A kinase Aurora C kinase INCENP Spindle assembly checkpoint GRCh38: Ensembl release 89: ENSG00000178999 - ... Phosphorylation of CENP-A at serine 7 by Aurora A kinase recruits Aurora B to the centromere. Aurora B, itself, can also ... The Aurora kinases associate with microtubules during chromosome movement and segregation. Aurora kinase B localizes to ... Aurora B kinase has been shown to interact with: BARD1, BIRC5, and CDCA8 TACC1. FBXL2. Abnormally elevated levels of Aurora B ...
Aurora kinase C
Although yeast contain only one Aurora kinase and C. elegans and Drosophila contain only two, mammals have three Aurora kinases ... "Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells". Cell ... "Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells". Cell ... Aurora kinase C, also Serine/threonine-protein kinase 13 is an enzyme that in humans is encoded by the AURKC gene. This gene ...
Aurora kinase A
The human genome contains three members of the aurora kinase family: Aurora kinase A, Aurora kinase B and Aurora C kinase. The ... Aurora A and Aurora B kinases play important roles in mitosis. The Aurora kinase A is associated with centrosome maturation and ... Aurora A phosphorylation directs the cytoplasmic polyadenylation translation of mRNA's, 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 ...
Spindle checkpoint
... 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 ...
Aurora inhibitor
Aurora kinase inhibitors are a putative drug class for treating cancer. The Aurora kinase enzymes could be potential targets ... There are three mammalian aurora kinase genes, encoding aurora A, B and C. Intense investigation has focused on aurora A and B ... Aurora-B (Serine/threonine-protein kinase 12, AIK2, AIM1, ARK2, STK12) Aurora-C (Serine/threonine-protein kinase 13, AIE2, AIK3 ... Aurora kinases, so named because the scattered mitotic spindles generated by mutant forms resemble the Aurora Borealis, have ...
Multipolar spindles
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- ...
KRP (biochemistry)
This process is associated with Aurora B Protein Kinase. When Aurora B's function is disrupted, MCAK ability to locate ... Andrews PD, Ovechkina Y, Morrice N, Wagenbach M, Duncan K, Wordeman L, Swedlow JR (February 2004). "Aurora B regulates MCAK at ... There are other environments in which MCAK's function is impaired, absent impact on its associated kinase. For example, alpha- ...
Sapacitabine
"Cyclin Dependent Kinase (CDK) and Aurora Kinase (AK) inhibitors , Cyclacel R&D for anticancer drugs acting on cell cycle". www. ...
Hesperadin
... works as an inhibitor, attaching to the active sites of Aurora A and Aurora B kinases. Hauf, Silke; Cole, Richard W ... Hesperadin is an aurora kinase inhibitor. The small molecule inhibits chromosome alignment and segregation by limiting the ... function of mitotic kinases Aurora B and Aurora A. Hesperadin causes cells to enter anaphase much faster, sometimes before the ... Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms". Molecular Microbiology. 72 (2): 442- ...
Spindle apparatus
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 ...
Midbody (cell biology)
MKLP1 TEX14 CEP55 Aurora Kinase B Paweletz N (January 2001). "Walther Flemming: pioneer of mitosis research". Nature Reviews. ...
Phragmoplast
"Arabidopsis α Aurora Kinases Function in Formative Cell Division Plane Orientation". The Plant Cell. 23 (11): 4013-4024. doi: ... Another midline-localized protein, "two-in-on" (TIO), is a putative kinase and is also required for cytokinesis as shown by ... Oh, Sung Aeong; Bourdon, Valérie; Dickinson, Hugh G.; Twell, David; Park, Soon Ki (2014-03-01). "Arabidopsis Fused kinase TWO- ... The essential mechanism of MAPK cascade for phragmoplast expansion is suppressed by cyclin dependent kinase (CDK) activity ...
Barry James Thompson
Bell, G.P.; Fletcher, G.C.; Brain, R.; Thompson, B.J (2015). "Aurora kinases phosphorylate Lgl to induce mitotic spindle ... columnar pseudostratified epithelial cells must round up at mitosis in a process that involves the Aurora A and B kinases, ... Aguilar-Aragon, M.; Elbediwy, A.; Foglizzo, V.; Fletcher, G.C.; Li, V.S.W; Thompson, B.J. (2018). "Pak1 Kinase Maintains Apical ... but Cdc42 appears to act primarily via activating the kinases aPKC and Pak1 in Drosophila follicle cells. His laboratory also ...
Anaphase lag
Aurora B is a kinase active in late metaphase, and has been shown to function as a checkpoint for the proper attachments of ... Cimini, Daniela; Wan, Xiaohu; Hirel, Christophe B.; Salmon, E.D. (2006-09-05). "Aurora Kinase Promotes Turnover of Kinetochore ... When Aurora B was partially inhibited by a small molecule drug, Cimini et al. observed lagging chromatids at increasing ... "The Ska complex promotes Aurora B activity to ensure chromosome biorientation". The Journal of Cell Biology. 215 (1): 77-93. ...
DOT1L
"Expression of Aurora-B kinase and phosphorylated histone H3 in hepatocellular carcinoma". Anticancer Research. 26 (5A): 3585-93 ...
TPX2
... is also important in activating and recruiting Aurora A kinase, a kinase responsible for phosphorylating TPX2 and ... In the presence of nuclear import factor importin α, TPX2 is bound and prevented from binding Aurora A kinase, though it is ... TPX2 recruits and activates Aurora A kinase by utilizing its short 43 amino acid long amino-terminal sequence to bind the ... Notably, this recognition between TPX2 and Aurora A is analogous to that between the cAMP-dependent protein kinase (cAPK) ...
Said Sebti
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 ...
DLGAP5
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- ...
LATS2
2005). "The centrosomal protein Lats2 is a phosphorylation target of Aurora-A kinase". Genes Cells. 9 (5): 383-97. doi:10.1111/ ... 2005). "The Ste20-like kinase Mst2 activates the human large tumor suppressor kinase Lats1". Oncogene. 24 (12): 2076-86. doi: ... Large tumor suppressor kinase 2 (LATS2) is an enzyme that in humans is encoded by the LATS2 gene. This gene encodes a serine/ ... It interacts with the centrosomal proteins aurora-A and ajuba and is required for accumulation of gamma-tubulin and spindle ...
TTK (gene)
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 ...
CDCA8
... has been shown to interact with INCENP, Survivin and Aurora B kinase. GRCh38: Ensembl release 89: ENSG00000134690 - ... "Phosphorylation and activation of cell division cycle associated 8 by aurora kinase B plays a significant role in human lung ...
DSN1
"Phosphorylation of HsMis13 by Aurora B kinase is essential for assembly of functional kinetochore". J. Biol. Chem. 283 (39): ...
I-motif DNA
"126 Development of a new series of tricyclic pyrimido-indole inhibitors targeting Aurora kinases". European Journal of Cancer ...
Alisertib
... (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. It was investigated as a ... a selective Aurora A kinase inhibitor, in relapsed and refractory aggressive B- and T-cell non-Hodgkin lymphomas". Journal of ... Protein kinase inhibitors, Benzoic acids, Fluoroarenes, Abandoned drugs, Takeda Pharmaceutical Company brands, Chloroarenes, ...
K562 cells
The problem with K562 cells, and many other cancer cell types, is an overabundance of Aurora kinases. These kinases play a role ... However, the overabundance of Aurora kinases allows for uncontrolled cellular division, resulting in cancer. Inhibiting these ... This gene targets the cyclin-dependent kinase inhibitor, p21, and causes cell differentiation, cell cycle arrest in G1, and ...
NEDD9
"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 ...
Centrin 1
2006). "The GIT-associated kinase PAK targets to the centrosome and regulates Aurora-A". Mol. Cell. 20 (2): 237-49. doi:10.1016 ...
CASS4
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 ...
N-Myc
"Drugging MYCN through an Allosteric Transition in Aurora Kinase A." Cancer Cell. 26 (3): 414-27. doi:10.1016/j.ccr.2014.07.015 ... N-Myc is also stabilized by aurora A which protects it from degradation. Drugs that target this interaction are under ... development, and are designed to change the conformation of aurora A. Conformational change in Aurora A leads to release of N- ... "Stabilization of N-Myc is a critical function of Aurora A in human neuroblastoma". Cancer Cell. 15 (1): 67-78. doi:10.1016/j. ...
NME1
... 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) ...
Andrea Musacchio
... and for his contributions to the understanding of the role of the kinase Aurora B, Mps1 and Haspin in mitosis. In 2008, the ... Santaguida, S; Vernieri, C; Villa, F; Ciliberto, A; Musacchio, A (Apr 20, 2011). "Evidence that Aurora B is implicated in ... "Mechanism of Aurora B activation by INCENP and inhibition by hesperadin". Molecular Cell. 18 (3): 379-91. doi:10.1016/j.molcel. ... "A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B." (PDF). The Journal of Cell Biology. 199 (2 ...
NUMB (gene)
Wirtz-Peitz F, Nishimura T, Knoblich JA (October 2008). "Linking cell cycle to asymmetric division: Aurora-A phosphorylates the ... 1995). "A protein-binding domain, EH, identified in the receptor tyrosine kinase substrate Eps15 and conserved in evolution". ... atypical protein kinase C). In the sensory organ precursor (SOP) cell, the PAR proteins localize to the posterior pole of the ...
Shugoshin N terminal protein domain
Shugoshin is a crucial target of Bub1 kinase that plays a central role in the cohesion of chromosomes during cell division. The ... "Shugoshin enables tension-generating attachment of kinetochores by loading Aurora to centromeres". Genes Dev. 21 (4): 420-35. ...
ST motif
Aurora, R; Rose GD (1998). "Helix Capping". Protein Science. 7 (1): 21-38. doi:10.1002/pro.5560070103. PMC 2143812. PMID ... SPXX or STXX are frequently found at DNA-binding sites and also that they are recognized as substrates by some protein kinases ...
Kinesin-like protein KIF11
Bishop JD, Han Z, Schumacher JM (2005). "The Caenorhabditis elegans Aurora B kinase AIR-2 phosphorylates and is required for ... Rapley J, Nicolas M, Groen A, Regue L, Bertran MT, Caelles C, Avruch J, Roig J (2008). "The NIMA-family kinase Nek6 ... Blangy A, Arnaud L, Nigg EA (1997). "Phosphorylation by p34cdc2 protein kinase regulates binding of the kinesin-related motor ... "Parkin regulates Eg5 expression by Hsp70 ubiquitination-dependent inactivation of c-Jun NH2-terminal kinase". J Biol Chem. 283 ...
Mir-126
Wang S, Aurora AB, Johnson BA, Qi X, McAnally J, Hill JA, Richardson JA, Bassel-Duby R, Olson EN (2008). "The endothelial- ... suppresses the growth of neoplastic cells by targeting phosphatidylinositol 3-kinase signaling and is frequently lost in colon ...
G2-M DNA damage checkpoint
"Bora and the Kinase Aurora A Cooperatively Activate the Kinase Plk1 and Control Mitotic Entry". Science. 320 (5883): 1655-1658 ... This loop is further amplified indirectly through the coordinated interaction of the Aurora A kinase and the Bora cofactor. ... pathways which activate the Chk2 and Chk1 kinases, respectively. These kinases act upstream of Cdc25 and Wee1, the direct ... The main rad3 effector is the kinase Chk1, which is required for the G2-M arrest in response to DNA-damaging agents. Chk1 is an ...
Cell cycle checkpoint
Seki A, Coppinger JA, Jang CY, Yates JR, Fang G (June 2008). "Bora and the kinase Aurora a cooperatively activate the kinase ... These kinases phosphorylate and activate the effector kinases Chk2 and Chk1, respectively, which in turn phosphorylate the ... The G1 phase cyclin-dependent kinase works together with S phase cyclin-dependent kinase targeting p27 for degradation. In turn ... The cell is once more examined for sites of DNA damage or incomplete replication, and the kinases ATR and ATM are recruited to ...
Rosie Alegado
Alegado, Rosanna A.; Chin, Chui-Yoke; Monack, Denise M.; Tan, Man-Wah (October 2011). "The two-component sensor kinase KdpD is ... Kahanamoku, Sara; Alegado, Rosie 'Anolani; Kagawa-Viviani, Aurora; Kamelamela, Katie Leimomi; Kamai, Brittany; Walkowicz, ...
Centrosome cycle
... and Aurora kinases are responsible for this phosphorylation. [21] The phosphorylation of downstream targets of Plks and Aurora ... "Figure 1". Aurora-A: the maker and breaker of spindle poles. Journal of Cell Science. Archived from the original on 11 May 2012 ... "CDK2 cyclin dependent kinase 2 [Homo sapiens (human)]". Gene - NCBI. Retrieved 1 December 2019. Hinchcliffe EH, Li C, Thompson ... The mis-expression of genes such as p53, BRCA1, Mdm2, Aurora-A and survivin causes an increase in the amount of centrosomes ...
Cytokinesis
The centralspindlin cluster formation is promoted by phosphorylation of MLKP1 by Aurora B, a component of CPC. In short, the ... Petronczki M, Glotzer M, Kraut N, Peters JM (May 2007). "Polo-like kinase 1 triggers the initiation of cytokinesis in human ... Second, RhoA promotes myosin II activation by the kinase ROCK, which activates myosin II directly by phosphorylation of the ...
Survivin
"Survivin enhances Aurora-B kinase activity and localizes Aurora-B in human cells". J. Biol. Chem. 278 (1): 486-90. doi:10.1074/ ... Survivin has been shown to interact with: Aurora B kinase, CDCA8, Caspase 3, Caspase 7, Diablo homolog and INCENP. GRCh38: ...
SU6656
Aurora C, Aurora B, CaMKKβ. The inhibition of these kinases in biochemical reactions in vitro does not necessarily indicate ... SU6656 was initially identified as a Src kinase inhibitor by virtue of its ability to reverse an effect that an activated ... SU6656 has been used primarily as a research tool to investigate the function of Src family kinases in cellular signal ... SU6656 is a Src family kinase inhibitor developed by the biotechnology company SUGEN Inc (a subsidiary of Pharmacia) in 2000. ...
CHEK1
... role in the spindle checkpoint during mitosis thus interacts with spindle assembly proteins Aurora A kinase and Aurora B kinase ... Checkpoint kinases (Chks) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been ... WEE1 kinase and PLK1 are also targeted by Chk1 to induce cell cycle arrest. Phosphorylation of WEE1 kinase inhibits cdk1 which ... Checkpoint kinase 1, commonly referred to as Chk1, is a serine/threonine-specific protein kinase that, in humans, is encoded by ...
Claire E. Eyers
Byrne DP, Vonderach M, Ferries S, Brownridge PJ, Eyers CE, Eyers PA (2016). "cAMP-dependent protein kinase (PKA) complexes ... "Identification of novel phosphorylation sites on Xenopus laevis Aurora A and analysis of phosphopeptide enrichment by ... protein kinase complexes and glycan conformation, and several highly-accessed reviews[citation needed] on the subject of ion ... at the University of Dundee where she was awarded a PhD in 2002 for her work on stress-activated protein kinases with Sir ...
Telophase
Aurora B kinase, and kinesin-8". The Journal of Cell Biology. 191 (4): 795-808. doi:10.1083/jcb.201006028. PMC 2983061. PMID ... The phosphorylation of the protein targets of M-Cdks (Mitotic Cyclin-dependent Kinases) drives spindle assembly, chromosome ... Telophase is primarily driven by the dephosphorylation of mitotic cyclin-dependent kinase (Cdk) substrates. ... microtubule-stabilizer-specific kinases, and plus-end directed microtubule depolymerases, respectively. These effectors are ...
David Glover
This led to genetic studies that allowed him to discover and name the Polo and Aurora protein kinases, required for the ... In Cambridge he discovered the second main Aurora B kinase required for cells to progress through metaphase and used genetic ... Over the past decade he has uncovered the major steps of centriole duplication by demonstrating that Polo-like-kinase 4 (Plk4) ... Remarkably, the localisation and function of Polo kinase at the centrosome, the kinetochore and the central spindle in ...
Bill Earnshaw
He discovered the "chromosomal passenger complex" of INCENP, Aurora B kinase, Survivin and Borealin - a major regulator of ...
JUB (gene)
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 ...
Bcr-Abl tyrosine-kinase inhibitor
Unlike other T315I targeting inhibitors in development, ponatinib does not target Aurora kinases, which clearly distinguishes ... At first it was believed that bosutinib was a selective Src kinase inhibitor but now it is known that its kinase inhibition ... Since dasatinib is an inhibitor of Src family kinases, it can overcome resistance due to Src family kinase activation. Because ... particularly the Src family kinases. The Src family kinases have been implicated in Bcr-Abl signaling and mediate imatinib ...
IPO8
"Human POGZ modulates dissociation of HP1alpha from mitotic chromosome arms through Aurora B activation". Nature Cell Biology. ... "14-3-3 epsilon dynamically interacts with key components of mitogen-activated protein kinase signal module for selective ...
Aurora Biosciences
... wanted to apply Aurora's assay expertise to its programs in kinase inhibitors and caspase inhibitors, and wanted access to ... which created Aurora Discovery from it. Aurora Discovery eventually changed its name to Aurora Biotechnologies, and in 2009 was ... In 2001, Aurora was acquired by Vertex Pharmaceuticals for $592 million in stock. Vertex wanted access to Aurora's insight into ... Vertex retained Aurora's drug discovery facility and staff in San Diego; ivacaftor was discovered there in 2005. "Aurora ...
Garikapati Narahari Sastry
Badrinarayan, Preethi; Sastry, G. Narahari (2014). "Specificity Rendering 'Hot-Spots' for Aurora Kinase Inhibitor Design: The ... Badrinarayan, Preethi; Sastry, G. Narahari (2011). "Sequence, Structure, and Active Site Analyses of p38 MAP Kinase: Exploiting ...
SEPTIN1
... a new interaction partner for human serine/threonine kinase aurora-B". Biochemical and Biophysical Research Communications. 336 ...
Aurora libraries. Aurora A-B Kinases Targeted Library
Aurora A-B Kinases Library is a set of small-molecule Aurora kinase inhibitors. Overexpression of Aurora kinases has been ... ZIP Aurora libraries. Aurora A-B Kinases Targeted Library 9,342 compounds PDF Aurora libraries. Aurora A-B Kinases Targeted ... Aurora kinases, a family of serine/threonine kinases, consisting of Aurora A (AURKA), Aurora B (AURKB) and Aurora C (AURKC), ... Besides regulating mitosis, Aurora kinases have been implicated in regulating meiosis. The deletion of Aurora kinases could ...
Aurora kinase (Aur) family | Enzymes | IUPHAR/BPS Guide to PHARMACOLOGY
Aurora kinase (Aur) family in the IUPHAR/BPS Guide to PHARMACOLOGY. ... ARK1 , AurA , Aurora 2 , Aurora family kinase 1 , ratAurA , serine/threonine kinase 15 , serine/threonine kinase 6 , STK15 , ... Aurora kinases A and B are widely expressed in dividing cells, whereas Aurora kinase C expression appears to be restricted to ... 2010) Shared and separate functions of polo-like kinases and aurora kinases in cancer. Nat Rev Cancer, 10 (12): 825-41. [PMID: ...
Aurora A kinase activation: Different means to different ends | Journal of Cell Biology | Rockefeller University Press
review the different activation mechanisms of the Aurora A kinase during mitotic entry and progression. ... Aurora B kinase, Polo-like kinase 1 (Plk1), and Cyclin-dependent kinase 1 (Cdk1)/Cyclin A/B complexes. Their precise and ... Aurora A kinase activation: Different means to different ends Nicolas Tavernier, Nicolas Tavernier ... Aurora A is a serine/threonine kinase essential for mitotic entry and spindle assembly. Recent molecular studies have revealed ...
Human AURKB (Aurora Kinase B) ELISA Kit
- AFSBio Inc.
Serine/Threonine Kinase 12; Aurora-1; Aurora-and IPL1-like midbody-associated protein 1; Aurora/IPL1-related kinase 2 Species: ... Aurora-1; Aurora-and IPL1-like midbody-associated protein 1; Aurora/IPL1-related kinase 2 ... The concentration of Aurora Kinase B(AURKB) in the samples is then determined by comparing the OD of the samples to the ... The microtiter plate provided in this kit has been pre-coated with an antibody specific to Aurora Kinase B(AURKB). Standards or ...
High expression of aurora kinase B predicts poor prognosis in hepatocellular carcinoma after curative surgery and its effects...
Aurora B kinase is the downstream target of ATR
- Oregon Health & Science University
Aurora B kinase is thought to be responsible for the phosphorylation of H-3. Recent results from the Thayer lab have shown that ... Aurora B kinase is the downstream target of ATR. *Chang, Bill (PI) ... Therefore, I hypothesize that inhibition of Aurora B, either by inhibition of kinase activity or inhibition of recruitment to ... The objective is to characterize the link between DRT/DMC, the replication checkpoint, and Aurora B kinase. ...
October | 2022 | Aurora kinase B
ProViz - Aurora kinase A - AURKA - O14965
ProViz is an interactive protein exploration tool, which searches several databases
for information about a given query protein. Data relevant to the protein like an
alignment of homologues, linear motifs, post translational modifications, domains,
secondary structure, sequence variations and others are graphically represented
relative to their position in the protein.
Aurora Kinase | Cell Cycle|Epigenetics| CSNpharm
Three Aurora kinases have been identified in mammalian cells to date, Aurora A, Aurora B, Aurora C. Besides being implicated as ... Aurora kinase helps the dividing cell dispense its genetic materials to its daughter cells. Defects in this segregation can ... mitotic regulators, these three kinases have generated significant interest in the cancer research field due to their elevated ... Aurora kinases are serine/threonine kinases that are essential for cell proliferation. ...
Aurora Kinase compound (inhibitors, antagonists)-ProbeChem.com
... potent and selective Aurora A, Aurora B, Aurora C inhibitor. ... Aurora Kinase Request The Product List ofAurora Kinase Aurora ... Aurora Kinase compound (inhibitors, antagonists, inducers) with high quality and purity, chemical tool in various assays for ... F114 is a novel, first-in-class, dual aurora and lim kinase inhibitor with IC50 of 72 nM and 137 nM against Aurora-A and Limk1 ... PF-03814735 is a potent, orally bioavailable, reversible inhibitor of both Aurora A and Aurora B kinases with IC50 values of ...
IMSEAR at SEARO: Haploinsufficient tumor suppressor Tip60 negatively regulates oncogenic Aurora B kinase
The Aurora kinases represent a group of serine/threonine kinases which are crucial regulators of mitosis. DysregulatedAurora ... Haploinsufficient tumor suppressor Tip60 negatively regulates oncogenic Aurora B kinase. Authors: Bose, Arnab. Sudevan, Surabhi ... Haploinsufficient tumor suppressor Tip60 negatively regulates oncogenic Aurora B kinase. Journal of Biosciences. 2019 Dec; 44(6 ... kinase B (AurkB) expression, stemming from genomic amplification, increased gene transcription or overexpressionof its ...
June 2016 - Page 7 - Polo-Like Kinases and Aurora Kinases in Cancer Therapy
Lectin-like oxidized low-density lipoprotein receptor (LOX-1) is really a scavenger receptor that binds oxidized low-density lipoprotein (OxLDL) and has a role in atherosclerosis development. both control and test slides. 2.8 Chaperonin-containing TCP-1 (CCT) complex purification CCT was purified from bovine testes according to previously established procedures and the integrity of the oligomeric CCT complex was confirmed by using single-particle cryoelectron microscopy BCH [32-33]. The final purified protein concentration was determined by using the Bradford assay with BSA standards (Pierce) and substrate folding activity of the CCT complex was assessed with a luciferase refolding assay as previously described [34]. 2.9 Direct binding assay NeutrAvidin agarose beads (100 μl of 50% slurry Thermo Scientific) were washed in CCT lysis buffer which comprised 25 mM HEPES (pH 7.4) 100 mM KCl 5 mM MgCl2 10 glycerol 0.1% Triton X-100 20 mM EDTA 0.1% v/v Tween-20 and protease inhibitors (Roche). Then ...
June 2022 - Structure-based characterization of novel Aurora Kinase inhibitors
There was marked increased in creatine kinase (11,960?U/L in the beginning and 24,240?U/L after 1 day) and lactate ... There was marked increased in creatine kinase (11,960?U/L initially and 24,240?U/L after 1 day) and lactate dehydrogenase ... There was marked increased in creatine kinase (11,960?U/L initially and 24,240?U/L after 1 day) and lactate dehydrogenase ...
A phase i study of MK-5108, an oral aurora a kinase inhibitor, administered both as monotherapy and in combination with...
Dive into the research topics of A phase i study of MK-5108, an oral aurora a kinase inhibitor, administered both as ... T1 - A phase i study of MK-5108, an oral aurora a kinase inhibitor, administered both as monotherapy and in combination with ... N2 - Background MK-5108 is a potent/highly selective Aurora A kinase inhibitor. Methods A randomized Phase I study of MK-5108, ... AB - Background MK-5108 is a potent/highly selective Aurora A kinase inhibitor. Methods A randomized Phase I study of MK-5108, ...
The Role of Aurora Kinase Inhibitors in hematologic disorders - Aurora Kinase Inhibitor
MedlinePlus: Genes
Urine Tumor Markers in Bladder Cancer Diagnosis: Overview of Urine Tumor Markers, Genetic Aberrations in Bladder Cancer,...
Tension directly stabilizes reconstituted kinetochore-microtubule attachments | Nature
... through a catch bond-like mechanism that does not require Aurora B7,8,9,10. On the basis of these findings, we propose that ... Aurora B4,5. However, a complete mechanistic understanding of the role of tension requires reconstitution of kinetochore- ... by suppressing the destabilizing activity of a kinase, ... Tension can directly suppress Aurora B kinase-triggered release ... Tension can directly suppress Aurora B kinase-triggered release of kinetochore-microtubule attachments *Anna K. de Regt ...
Phosphorylation of Merlin by Aurora A kinase appears necessary for mitotic progression | Institut Curie
Urine Tumor Markers in Bladder Cancer Diagnosis: Overview of Urine Tumor Markers, Genetic Aberrations in Bladder Cancer,...
"Inactivation of Aurora kinases and Cyclin-dependent kinases 4/6 allows" by Vural Tagal, Uttam K. Tambar et al.
AURORA KINASE A and related downstream molecules: A potential network for cancer therapy. | Adv Protein Chem Struct Biol;134:...
Aurora-A kinase (AURKA) belongs to the serine/threonine kinase family specific to cell division. In normal cells, activation of ... AURORA KINASE A and related downstream molecules: A potential network for cancer therapy. ... AURORA KINASE A and related downstream molecules: A potential network for cancer therapy. ... Aurora Quinase A; Carcinogênese; Humanos; Ciclo Celular; Proliferação de Células; Inibidores de Proteínas Quinases ...
MicroRNA let-7b regulates genomic balance by targeting Aurora B kinase - Fingerprint
- VTT's Research Information Portal
Ras-Driven Transcriptome Analysis Identifies Aurora Kinase ......Ras-Driven Transcriptome Analysis Identifies Aurora Kinase A as...
Ras-Driven Transcriptome Analysis Identifies Aurora Kinase A as a Potential Malignant... ... Download Ras-Driven Transcriptome Analysis Identifies Aurora Kinase ...... ... Ras-Driven Transcriptome Analysis Identifies Aurora Kinase ......Ras-Driven Transcriptome Analysis Identifies Aurora Kinase A as ... a serine/threonine kinase, is a member of the mitogen activated protein kinase kinase kinase ...
CHIR-124 405168-58-3 was the first to combine the seen an Aurora kinase inhibition | Microrna Inhibitors
CHIR-124 405168-58-3 was the first to combine the seen an Aurora kinase inhibition. Posted on July 27, 2012. by mirn0190 ... MLN8237 MLN8237 MLN8054 2.1.4 to share structural homology, but has four times the power of the inhibition of Aurora kinase A ... 6 This study was the first to combine the seen an Aurora kinase inhibition, and senescence, a classic effect with antimitotic ... evident that key Drowsiness and liver toxicity escalation t limited to the level necessary to adequately inhibit Aurora kinase ...
Therapeutic Options Against BCR-ABL1 T315I-Positive Chronic Myelogenous Leukemia | Clinical Cancer Research | American...
Dual Aurora/ABL kinase inhibitors. The human Aurora proteins (A, B, and C) are serine/threonine kinases that regulate different ... Other Aurora kinase inhibitors with anti-T315I activity. VE-465 is an Aurora kinase inhibitor structurally related to MK-0457 ... Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680. Cancer ... AT9283, an inhibitor of Aurora A, Aurora B, JAK2, JAK3, and BCR-ABL T315I kinases (IC50 , 5 nmol/L in all case), is undergoing ...
6R4B: Aurora-A in complex with shape-diverse fragment 56
Cell-based screen for altered nuclear phenotypes reveals senescence progression in polyploid cells after Aurora kinase B...
2015) Cell-based screen for altered nuclear phenotypes reveals senescence progression in polyploid cells after Aurora kinase B ... Aurora Kinase B, Cell Aging, Cell Division, Cell Line, Cell Nucleus, Chromosome Segregation, Cytokinesis, HeLa Cells, High- ... Downstream analyses show that all of the compounds that induce tetraploid senescence inhibit Aurora kinase B (AURKB). AURKB is ... Cell-based screen for altered nuclear phenotypes reveals senescence progression in polyploid cells after Aurora kinase B ...
PDB 5DNR | Chain AURORA A KINASE IN COMPLEX WITH ATP IN SPACE GROUP P41212 | 5DNR A | 3D Structure | canSARS
Our new article "Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis" is published in Journal of...
"Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis" is published in Journal of Proteome Research. ... HomeOur new article "Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis" is published in Journal of ... Our new article "Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis" is published in Journal of ... "Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis" is published in Journal of Proteome Research. ...
Inhibitor27
- 2006) 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. (guidetopharmacology.org)
- 2004) VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. (guidetopharmacology.org)
- Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively[1]. (csnpharm.com)
- Tozasertib is the inhibitor of Aurora-A, -B, -C kinases with Ki values of 0.6, 18, 4.6 nM respectively. (csnpharm.com)
- TC-A2317 HCl is an Aurora kinase A inhibitor. (csnpharm.com)
- SU6668 is a cell-permeable indolinone compound that acts as a potent ATP-competitive inhibitor against RTKs (receptor tyrosine kinases) Kit, PDGFR, VEGFR2 (Flk-1KDR), FGFR1 activity in vitro (IC50 0.01, 0.1, 3.9, and 3.8 M, respectively) and PDGFVEGFbFGF-mediated angiogenesis and tumor development. (csnpharm.com)
- SP-96 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)
- NU6140 is a selective CDK2 inhibitor with IC50 value of 0.94μM, as well as potently inhibits Aurora kinase A/B with IC50 values of 0.035 and 0.067μM, respectively. (csnpharm.com)
- Derrone, a natural product isolated and purified from the herbs of Cudrania tricuspidata, may be interesting antimicrobial agents to be used against infectious diseases caused by many pathogens, and is an Aurora kinase inhibitor, it can significantly inhibit the formation and growth of MCF7 tumor spheroids. (csnpharm.com)
- DBPR114 is a potent multi-kinase inhibitor with potent activities against more than 57 oncogenic kinases, including Aurora-A, FLT3, CSF1R, MET, etc. (csnpharm.com)
- Danusertib is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively. (csnpharm.com)
- CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. (csnpharm.com)
- Cenisertib (AS 703569;R763) is a novel potent, orally available inhibitor of Aurora kinases, exhibits signifficant anti-proliferative activity against a wide range of tumor cells both in vitro and in vivo (A549 EC50=9 nM). (probechem.com)
- Tozasertib (MK-0457, VX-680) is a highly potent, selective and reversible Aurora kinase inhibitor with Ki of 0.6, 18 and 4.6 nM for Aurora A, B and C, respectively. (probechem.com)
- PF-03814735 is a potent, orally bioavailable, reversible inhibitor of both Aurora A and Aurora B kinases with IC50 values of 0.8 and 5 nM, respectively. (probechem.com)
- PHA-680626 is a kinase inhibitor exhibiting strong inhibitory activity on both Bcr-Abl and Aurora kinases, also inhibits the formation of the Aurora-A/N-Myc complex. (probechem.com)
- Tinengotinib (TT-00420) is a spectrum-selective multikinase inhibitor that targets cell proliferation, angiogenesis, and immunomodulatory pathways by inhibiting Aurora A/B and JAK involved in cytokine signalling, and RTKs involved in angiogenesis (FGFRs and VEGFRs). (probechem.com)
- F114 is a novel, first-in-class, dual aurora and lim kinase inhibitor with IC50 of 72 nM and 137 nM against Aurora-A and Limk1, respectively, F114 inhibits GBM proliferation and invasion. (probechem.com)
- TAS-119 (TAS119) is a potent, selective, orally active inhibitor of Aurora A with IC50 of 1 nM. (probechem.com)
- Background MK-5108 is a potent/highly selective Aurora A kinase inhibitor. (wustl.edu)
- We characterize the screen using a focused tool compound kinase inhibitor library. (sgul.ac.uk)
- A phase Ib study of investigational pan-RAF kinase inhibitor MLN2480 plus investigational TORC1/2 inhibitor MLN0128, investigational Aurora A kinase inhibitor alisertib (MLN8237), or paclitaxel in patients (pts) with advanced solid tumors. (ox.ac.uk)
- Seliciclib (CYC202 or R-roscovitine), a CDK (cyclin dependent kinase) inhibitor, is in Phase 2 studies for the treatment of lung cancer and nasopharyngeal cancer and in a Phase 1 trial in combination with sapacitabine. (nbcnews.com)
- CYC116, an Aurora kinase and VEGFR2 inhibitor, is in a Phase 1 trial in patients with solid tumors. (nbcnews.com)
- mTOR kinase inhibitor AZD2014 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. (biochempartner.com)
- CHIR-99021 is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo. (dcchemicals.com)
- CHIR-99021 is a GSK-3α/β inhibitor with an IC50 of 10 and 6.7 nM,showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases. (dcchemicals.com)
Inhibition10
- And a growing number of studies have demonstrated that inhibition of Aurora kinases could potentiate the effect of chemotherapies. (chemdiv.com)
- Therefore, I hypothesize that inhibition of Aurora B, either by inhibition of kinase activity or inhibition of recruitment to the chromosome, plays a direct role in the DMC phenotype. (elsevier.com)
- 6 This study was the first to combine the seen an Aurora kinase inhibition, and senescence, a classic effect with antimitotic agents. (mirnainhibitors.com)
- MLN8237 MLN8237 MLN8054 2.1.4 to share structural homology, but has four times the power of the inhibition of Aurora kinase A and reduced tendency for the key Can cause drowsiness. (mirnainhibitors.com)
- Cell-based screen for altered nuclear phenotypes reveals senescence progression in polyploid cells after Aurora kinase B inhibition. (sgul.ac.uk)
- Our new article "Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis" is published in Journal of Proteome Research. (ku.edu.tr)
- Here, we investigated the effects of glycogen synthase kinase 3 (GSK3) inhibition via lithium chloride (LiCl) treatment on SERCA uncoupling in skeletal muscle and UCP1 expression in adipose. (jbc.org)
- ALS concentration-dependently induced autophagy in PANC-1 and BxPC-3 cells, which may be attributed to the inhibition of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR), p38 mitogen-activated protein kinase (p38 MAPK), and extracellular signal-regulated kinases 1 and 2 (Erk1/2) but activation of 5'-AMP-dependent kinase signaling pathways. (dovepress.com)
- Schubert A, Koziol U, Cailliau K, Vanderstraete M, Dissous C, Brehm K (2014) Targeting Echinococcus multilocularis Stem Cells by Inhibition of the Polo-Like Kinase EmPlk1. (plos.org)
- no significant inhibition on 26 other kinases. (dcchemicals.com)
Serine7
- Aurora kinases, a family of serine/threonine kinases, consisting of Aurora A (AURKA), Aurora B (AURKB) and Aurora C (AURKC), are essential kinases for cell division via regulating mitosis especially the process of chromosomal segregation. (chemdiv.com)
- Aurora A is a serine/threonine kinase essential for mitotic entry and spindle assembly. (rupress.org)
- The Aurora kinases represent a group of serine/threonine kinases which are crucial regulators of mitosis. (who.int)
- Aurora-A kinase ( AURKA ) belongs to the serine / threonine kinase family specific to cell division . (bvsalud.org)
- Aurora A is a cytoplasmic serine/threonine kinase that is critical in transitioning cells through mitosis and meiosis. (novusbio.com)
- A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS . (bvsalud.org)
- mTOR, a serine/threonine kinase that is upregulated in a variety of tumors, plays an important role downstream in the PI3K/Akt/mTOR signaling pathway. (biochempartner.com)
Inhibitors9
- For the past decades, a series of Aurora kinases inhibitors (AKIs) developed effectively repress the progression and growth of many cancers both in vivo and in vitro, suggesting that Aurora kinases could be a novel therapeutic target. (chemdiv.com)
- Currently, more than 100 crystallographic complexes obtained for various small-molecule Aurora kinase inhibitors are available within PDB databank. (chemdiv.com)
- Representative compounds from ChemDiv's library have demonstrated similar binding mode compared to reported Aurora kinase inhibitors. (chemdiv.com)
- Their importance in the mitotic cycle has driven the development of Aurora kinase inhibitors as therapeutic antimitotic agents for both adult and childhood malignancies. (guidetopharmacology.org)
- 2009) A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J Med Chem , 52 (10): 3300-7. (guidetopharmacology.org)
- 2010) Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. (guidetopharmacology.org)
- Mutations within the kinase domain of BCR-ABL1 constitute the most frequent mechanism of resistance in patients with chronic myelogenous leukemia treated with imatinib or the second generation tyrosine kinase inhibitors nilotinib and dasatinib. (aacrjournals.org)
- Of note, different mutations confer varying degrees of insensitivity to imatinib and other tyrosine kinase inhibitors (TKI). (aacrjournals.org)
- Phthalazinone Pyrazoles as Potent, Selective, and Orally Bioavailable Inhibitors of Aurora-A Kinase. (mpg.de)
AURKA2
- Pivotal protein kinases responsible for the massive increase in protein phosphorylation as cells transit into mitosis include Aurora A kinase (AURKA), Aurora B kinase, Polo-like kinase 1 (Plk1), and Cyclin-dependent kinase 1 (Cdk1)/Cyclin A/B complexes. (rupress.org)
- AURKA phosphorylates its substrates , including oncoproteins , transcriptional factors, tumor suppressor proteins , or other kinases central to various oncogenic signaling pathways critical to cancer . (bvsalud.org)
Mitosis6
- Besides regulating mitosis, Aurora kinases have been implicated in regulating meiosis. (chemdiv.com)
- The three mammalian Aurora kinases (A, B and C) play essential roles cell division, by regulating mitosis and the cell cycle. (guidetopharmacology.org)
- 6. Fu J, Bian M, Jiang Q, Zhang C. (2007) Roles of Aurora kinases in mitosis and tumorigenesis. (guidetopharmacology.org)
- We herein describe the characterization of EmPlk1, encoded by the gene emplk1 , which displays significant homologies to members of the Plk1 sub-family of Polo-like kinases that regulate mitosis in eukaryotic cells. (plos.org)
- Familia de serina-treonina cinasas implicadas en la regulación de la MITOSIS. (bvsalud.org)
- CDK11p58 kinase activity is required to protect sister chromatid cohesion at centromeres in mitosis. (univ-rennes.fr)
Protein kinase1
- Protein kinase C epsilon is important in modulating organic-dust-induced airway inflammation. (cdc.gov)
Mammalian2
- Unanchored dendrogram of mammalian protein kinases. (kinase.com)
- Anchored dendrogram of mammalian protein kinases. (kinase.com)
AURKB7
- The microtiter plate provided in this kit has been pre-coated with an antibody specific to Aurora Kinase B(AURKB). (afsbio.com)
- Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Aurora Kinase B(AURKB). (afsbio.com)
- After TMB substrate solution is added, only those wells that contain Aurora Kinase B(AURKB), biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. (afsbio.com)
- The concentration of Aurora Kinase B(AURKB) in the samples is then determined by comparing the OD of the samples to the standard curve. (afsbio.com)
- DysregulatedAurora kinase B (AurkB) expression, stemming from genomic amplification, increased gene transcription or overexpressionof its allosteric activators, is capable of initiating and sustaining malignant phenotypes. (who.int)
- The haploinsufficient tumor suppressor Tip60 acetylates two highly conserved lysine residues within the kinasedomain of AurkB which not only impinges the protein stability but also its kinase activity. (who.int)
- Downstream analyses show that all of the compounds that induce tetraploid senescence inhibit Aurora kinase B (AURKB). (sgul.ac.uk)
Vitro3
- CTX-0294885 is a bisanilino pyrimidine and exhibits inhibitory activity against a broad range of kinases in vitro, further developed into a Sepharose-supported kinase capture reagent. (csnpharm.com)
- Next, Mid1p "N-term" and "Middle" domains were mapped to yield six potential phospho-sites (S167, S328, S331, S332, S523 and S531), which were utilized to confirm the in vitro phosphorylation by the aurora kinase Ark1p. (bl.uk)
- CHIR 99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR 99021 specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[2]. (dcchemicals.com)
Phosphatidylinositol 3-kina1
- Many well-characterized mitogens [e.g. insulin-like growth factor (IGF),platelet-derived growth factor] signal through receptor tyrosine kinases(RTKs) that lead to activation of the Ras-MAPK and phosphatidylinositol-3-kinase (PI3K) pathways( Marshall, 1995 ). (biologists.com)
Mitotic kinase2
- Here, we report a novel interaction between the mitotic kinase, Aurora A, and the glycolytic enzyme, pyruvate kinase M2 (PKM2), in the interphase of the cell cycle. (jbc.org)
- A GFP fusion with the mitotic kinase Aurora-A labels centrosomes during the division of an SOP cell. (oeaw.ac.at)
Phosphorylation4
- Recent molecular studies have revealed the existence of multiple, distinct mechanisms of Aurora A activation, each occurring at specific subcellular locations, optimized for cellular context, and primed by signaling events including phosphorylation and oxidation. (rupress.org)
- Aurora B kinase is thought to be responsible for the phosphorylation of H-3. (elsevier.com)
- We found Aurora A-mediated phosphorylation of PKM2 at threonine 45. (jbc.org)
- Aurora A-dependent CENP-A phosphorylation at inner centromeres protects bioriented chromosomes against cohesion fatigue. (univ-rennes.fr)
Oncogenic1
- Bose Arnab, Sudevan Surabhi, Rao Vinay J, Shima Hiroki, Trivedi Arun Kumar, Igarashi Kazuhiko, Kundu Tapas K. Haploinsufficient tumor suppressor Tip60 negatively regulates oncogenic Aurora B kinase. (who.int)
Pathways3
- To expedite the identification of strategies to override the resistance imposed by the T315I mutation, several strategies have been pursued, including the exploitation of BCR-ABL1 kinase sites distant from the ATP-binding pocket to cripple the kinase activity of the enzyme and inhibiting signaling pathways downstream from BCR-ABL1. (aacrjournals.org)
- The marked dependence of BCR-ABL1 -positive cells on BCR-ABL1 kinase spurred the design of agents aiming at blocking the activity of this enzyme and its downstream signaling pathways. (aacrjournals.org)
- Neuronal precursor cells in the developing cerebellum require activity of the sonic hedgehog (Shh) and phosphoinositide-3-kinase (PI3K) pathways for growth and survival. (biologists.com)
AURKC1
- Function of aurora kinase C (AURKC) in human reproduction]. (cdc.gov)
Cyclin3
- Inactivation of Aurora kinases and Cyclin-dependent kinases 4/6 allows" by Vural Tagal, Uttam K. Tambar et al. (mdanderson.org)
- ALS remarkably arrested PANC-1 and BxPC-3 cells in G 2 /M phase via regulating the expression of cyclin-dependent kinases 1 and 2, cyclin B1, cyclin D1, p21 Waf1/Cip1, p27 Kip1, and p53. (dovepress.com)
- The potential genes underlying the differential effects of G‑SCs and P‑SCs on bone invasion in OSCC were evaluated using a microarray, which indicated that cyclin‑dependent kinase 1, insulin, aurora kinase A, cyclin B1 and DNA topoisomerase II alpha underlaid these differential effects. (spandidos-publications.com)
Inhibit1
- It was evident that key Drowsiness and liver toxicity escalation t limited to the level necessary to adequately inhibit Aurora kinase A. Based on these results, the development of MLN8054 MLN8237 abandoned in favor. (mirnainhibitors.com)
Apoptosis3
- DUOXA1 knockdown (using a DUOXA1 shRNA construct) resulted in enhanced differentiation compared to cells subjected to a control shRNA and subjecting DUOXA1 overexpressing cells to siRNAs targeting DUOX1 or apoptosis signal-regulating kinase 1 (ASK1) rescued the PRKCA phenotype. (researchensemble.com)
- We further show that a common regulator of apoptosis apoptosis signal-regulating kinase 1 (ASK1) is usually a downstream target of Balaglitazone DUOXA1-mediated H2O2 production and that knockdown of either DUOX1 or ASK1 rescues the DUOXA1 overexpression phenotype. (researchensemble.com)
- An intracellular-signaling kinase that plays a role in regulating APOPTOSIS . (nih.gov)
Vivo1
- BCR-ABL1 kinase has been shown to play a pivotal role in vivo in the development and maintenance of BCR-ABL1 -mediated leukemogenesis in several experimental models ( 1 - 3 ). (aacrjournals.org)
Spindle assembly1
- 4. Ducat D, Zheng Y. (2004) Aurora kinases in spindle assembly and chromosome segregation. (guidetopharmacology.org)
Kinetochore1
- The aurora B kinase promotes inner and outer kinetochore interactions in budding yeast. (ox.ac.uk)
Therapeutic1
- Journal Article] A novel therapeutic combination targeting sequentially Aurora B and Bcl-xL in hepatocellular carcinoma. (nii.ac.jp)
Complexes1
- Crystal structures of active Src kinase domain complexes. (mpg.de)
Mutations3
- These results notwithstanding, a subset of patients receiving imatinib therapy develop resistance to imatinib, which are frequently associated with single-point mutations within the kinase domain of BCR-ABL1 . (aacrjournals.org)
- More than 100 different ABL kinase point mutations have been reported in patients with imatinib-resistant CML ( 8 - 13 ). (aacrjournals.org)
- These mutations impair imatinib binding either by changing the identity of residues with which imatinib makes direct contact within the kinase domain (e.g. (aacrjournals.org)
Recombinant1
- A recombinant protein made to an N-terminal region of the human Aurora A protein (within residues 50-200). (novusbio.com)
Gene2
- Overexpression or gene amplification of Aurora kinases has been clarified in a number of cancers. (chemdiv.com)
- Dec 07): An updated table (Excel) includes Gene IDs, refseq accessions, HGNC names and improved sequences for some kinases. (kinase.com)
Compounds1
- ChemDiv's Aurora A-B Kinases Targeted Library contains 10,000 compounds. (chemdiv.com)
Yeast2
- The classification, annotation and sequences of human, fly, worm and yeast kinases may now be explored through our KinBase database. (kinase.com)
- In the fission yeast Schizosaccharomyces pombe (S. pombe) the anillin Mid1p, aurora Ark1p and the ESCRT family of proteins are involved in regulating specification of division site, mitotic entry and establishment of the final separation, respectively. (bl.uk)