• We show here that multiple phosphorylation sites within Rec8 as well as two different kinases, casein kinase 1delta/epsilon (CK1delta/epsilon) and Dbf4-dependent Cdc7 kinase (DDK), are required for Rec8 cleavage and meiosis I nuclear division. (nih.gov)
  • Based on in silico and in vitro data, casein kinase 1 (CK1) was predicted as a candidate for MR phosphorylation. (nih.gov)
  • Imetelstat treatment (2 weeks at 3uM) resulted in decreased expression of casein kinase 2 (CK2) subunits alpha and beta, and a reduction in phosphorylation of downstream CK2 substrates such as the DNA repair protein XRCC1. (aacrjournals.org)
  • Phosphorylation of glycogen synthase by cyclic AMP-independent casein kinase-2 from rabbit skeletal muscle. (uab.cat)
  • Phosphorylation of DARPP-32, a dopamine- and cAMP-regulated phosphoprotein, by casein kinase II. (cornell.edu)
  • The phosphorylated residues are located NH2-terminal to acidic amino acid residues, a characteristic of casein kinase II phosphorylation sites. (cornell.edu)
  • Phosphorylation by casein kinase II did not affect the potency of DARPP-32 as an inhibitor of protein phosphatase-1, which depended only on phosphorylation of Thr34 by cAMP-dependent protein kinase. (cornell.edu)
  • However, phosphorylation of DARPP-32 by casein kinase II facilitated phosphorylation of Thr34 by cAMP-dependent protein kinase with a 2.2-fold increase in the Vmax and a 1.4-fold increase in the apparent Km. (cornell.edu)
  • Phosphorylation of DARPP-32 by casein kinase II in intact cells may therefore modulate its phosphorylation in response to increased levels of cAMP. (cornell.edu)
  • Interestingly, activity of the NMDAR and Ca 2+ /calmodulin-dependent protein kinase II regulates CK2 phosphorylation of Ser1480. (jneurosci.org)
  • Tyrosine kinase signaling has emerged as a central regulator of the inflammatory response, partly through direct phosphorylation and dephosphorylation of the adherens junction components. (hindawi.com)
  • Phosphorylation of DNA topoisomerase II by casein kinase II: modulation of eukaryotic topoisomerase II activity in vitro. (nih.gov)
  • The phosphorylation of Drosophila melanogaster DNA topoisomerase II by purified casein kinase II was characterized in vitro. (nih.gov)
  • Apparent Km and Vmax values for the phosphorylation reaction were 0.4 microM topoisomerase II and 3.3 mumol of phosphate incorporated per min per mg of kinase, respectively. (nih.gov)
  • 13. Gene expression levels of Casein kinase 1 (CK1) isoforms are correlated to adiponectin levels in adipose tissue of morbid obese patients and site-specific phosphorylation mediated by CK1 influences multimerization of adiponectin. (nih.gov)
  • Phosphorylation of Nrf2 in the transcription activation domain by casein kinase 2 (CK2) is critical for the nuclear translocation and transcription activation function of Nrf2. (cdc.gov)
  • Caption: Casein kinase 1 (CK1) regulates PERIOD, a core protein in the biological clock of people. (nih.gov)
  • This gene encodes the beta subunit of casein kinase II, a ubiquitous protein kinase which regulates metabolic pathways, signal transduction, transcription, translation, and replication. (nih.gov)
  • Abstract A56: The telomerase inhibitor imetelstat exhibits antitumor and anticancer stem cell effects through perturbation of casein kinase-2 signaling. (aacrjournals.org)
  • A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfiler TM service. (guidetopharmacology.org)
  • 1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. (guidetopharmacology.org)
  • TMCB is a dual-kinase inhibitor of both casein kinase 2 (CK2) and extracellular-signal-regulated kinase 8 (ERK8) with IC50s of 0.50 μM. (csnpharm.com)
  • PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively. (csnpharm.com)
  • H 89 2HCl is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM. (csnpharm.com)
  • Ellagic acid is a potent and cell permeable casein kinase 2 (CK2) inhibitor with Ki of 20 nM, acts as a potent antioxidant and anti-mutagenic. (csnpharm.com)
  • CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively[1]. (csnpharm.com)
  • BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. (csnpharm.com)
  • Overall a collection of twenty diverse analogues of a casein kinase I inhibitor has been synthesised by changing three principle binding vectors. (vapourtec.com)
  • Purified bovine DARPP-32 was phosphorylated in vitro by casein kinase II to a stoichiometry greater than 2 mol of phosphate/mol of protein whereas two structurally and functionally related proteins, protein phosphatase inhibitor-1 and G-substrate, were poor substrates for this enzyme. (cornell.edu)
  • A screen of 72 inhibitors against 456 human kinases. (guidetopharmacology.org)
  • A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase Hotspot SM platform. (guidetopharmacology.org)
  • 2011) 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. (guidetopharmacology.org)
  • 1. Recent Advances in the Development of Casein Kinase 1 Inhibitors. (nih.gov)
  • 2. Casein Kinase 1δ Inhibitors as Promising Therapeutic Agents for Neurodegenerative Disorders. (nih.gov)
  • 3. Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK. (nih.gov)
  • 7. 1-(Benzo[d]thiazol-2-yl)-3-phenylureas as dual inhibitors of casein kinase 1 and ABAD enzymes for treatment of neurodegenerative disorders. (nih.gov)
  • 8. Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity. (nih.gov)
  • 15. Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening. (nih.gov)
  • Because these kinases exhibit constitutive activity in biochemical assays, it is likely that their activity in cells is controlled by subcellular localization, interactions with inhibitory proteins, targeted degradation, or combinations of these mechanisms. (figshare.com)
  • Casein kinases are characterized by their preferential utilization of acidic proteins such as caseins as substrates. (nih.gov)
  • Members of the casein kinase I protein family have been implicated in the control of cytoplasmic and nuclear processes, including DNA replication and repair, and have been shown to phosphorylate a variety of proteins, including itself. (nih.gov)
  • CD324 binds to the αEβ7 integrin to mediate cell adhesion and also interacts with a number of intracellular proteins including including erbin, ezrin, caspase-3, caspase-8, β-catenin, presenilin 1, and casein kinase II as well as other extracellular proteins including the EGF receptor. (biolegend.com)
  • Casein kinase I isoform alpha is an enzyme that in humans is encoded by the CSNK1A1 gene. (wikipedia.org)
  • Localisation of eight additional genes in the human major histocompatibility complex, including the gene encoding the casein kinase II beta subunit, and DNA sequence analysis of the class III region. (ox.ac.uk)
  • In the absence of Wnt signaling, β-catenin is targeted for degradation by a destruction complex that consists of the scaffold protein Axin, the tumor suppressor gene product APC, and the kinases CK1 and GSK3β. (wormbook.org)
  • Ror is a transmembrane tyrosine-kinase that contains a cysteine-rich Wnt binding domain that is similar to the extracellular domain of Frizzled ( Xu and Nusse, 1998 ). (wormbook.org)
  • In vitro, DARPP-32 phosphorylated by casein kinase II was dephosphorylated by protein phosphatases-1 and -2A. (cornell.edu)
  • Here we show that casein kinase II (CK2) phosphorylates the serine residue (Ser1480) within the C-terminal PDZ ligand (IESDV) of the NR2B subunit of NMDAR in vitro and in vivo . (jneurosci.org)
  • Members of the casein kinase 1 (CK1) family of serine-threonine protein kinases are implicated in the regulation of many cellular processes, including the cell cycle, circadian rhythms, and Wnt and Hedgehog signaling. (figshare.com)
  • 10. Functions and regulation of the serine/threonine protein kinase CK1 family: moving beyond promiscuity. (nih.gov)
  • CSNK1E is a serine/threonine protein kinase and a member of the casein kinase I protein family. (nih.gov)
  • Numerous serine/threonine kinases phosphorylate Tau, including GSK-3beta, protein kinase A (PKA), cyclin-dependent kinase 5 (cdk5) and casein kinase II. (thermofisher.com)
  • Protein kinase CK2 (formerly known as casein kinase 2) is a serine/threonine protein kinase whose functions have been under investigation for over three decades, leading to the recognition that it interacts with several signaling pathways. (umn.edu)
  • 2. Bischoff N, Olsen B, Raaf J, Bretner M, Issinger OG, Niefind K. (2011) Structure of the human protein kinase CK2 catalytic subunit CK2α' and interaction thermodynamics with the regulatory subunit CK2β. (guidetomalariapharmacology.org)
  • Three-dimensional structure of mammalian casein kinase I: molecular basis for phosphate recognition. (expasy.org)
  • Regulation of LEF-1 and c-Jun N-terminal kinase in mammalian cells. (nature.com)
  • 14. Casein kinase 1 (α, δ and ε) localize at the spindle poles, but may not be essential for mammalian oocyte meiotic progression. (nih.gov)
  • [ 67 , 68 ] In the absence of Wnt ligand, cytoplasmic β-catenin is degraded by a destruction complex that includes Axin, adenomatosis polyposis coli, glycogen synthase kinase 3 (GSK3) and casein kinase 1α (CK1α). (medscape.com)
  • In the latest paper, Partch and her colleagues focused on two core clock components: an enzyme known as casein kinase 1 (CK1) and a protein called PERIOD. (nih.gov)
  • Nearly a decade ago, Ptácek's team showed that affected family members had mutations in an enzyme called casein kinase Iδ (CKIδ). (nih.gov)
  • 6. The role of the casein kinase 1 (CK1) family in different signaling pathways linked to cancer development. (nih.gov)
  • 11. The casein kinase 1 family: participation in multiple cellular processes in eukaryotes. (nih.gov)
  • Caseine Kinase 1 alpha belongs is a member of the protein kinase superfamily, CK1 Ser/Thr protein kinase family, Casein kinase I subfamily. (prospecbio.com)
  • Bdbt has previously been shown to regulate activity of the kinase Discs Overgrown (Dco, also known as Doubletime or Casein Kinase Iε), and Dco itself has been implicated in regulating planar polarity by phosphorylating Dsh as well as the core protein Strabismus. (humanbioscience.org)
  • Casein kinase 1, alpha 1 has been shown to interact with Centaurin, alpha 1 and AXIN1. (wikipedia.org)
  • Under the conditions used, the kinase incorporated a maximum of 2-3 molecules of phosphate per homodimer of topoisomerase II. (nih.gov)
  • Recent findings indicate a complex interaction between kinases, phosphatases, and the adherens junction components that allow a fine regulation of the endothelial permeability to small molecules, leukocyte migration, and barrier resealing. (hindawi.com)
  • 17. Regulation of Alzheimer's disease amyloid-beta formation by casein kinase I. (nih.gov)
  • 2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. (guidetopharmacology.org)
  • Recent demonstrations of signal-mediated dynamic localization of CK2 and the identification of new signaling targets for it have converged to indicate an unexpected function for this protein kinase: cell survival. (umn.edu)
  • 16. Casein kinases as potential therapeutic targets. (nih.gov)
  • 19. Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases. (nih.gov)
  • CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders[1]. (csnpharm.com)