• In biochemistry, a dual-specificity kinase (EC 2.7.12.1) is a kinase that can act as both tyrosine kinase and serine/threonine kinase. (wikipedia.org)
  • HIPKs belong to the CMGC group of serine/threonine kinases and are part of the dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) family. (nature.com)
  • DYRKs are named after their characteristic dual-specificity, as they auto-phosphorylate a conserved tyrosine in their activation loop, but phosphorylate substrates on serine and threonine residues 2 . (nature.com)
  • C-terminally adjacent to the HID follows a proline, glutamate, serine, and threonine (PEST)-rich domain, mediating proteasomal degradation of these kinases. (nature.com)
  • The receptor complex consists of two type II and two type I transmembrane serine/threonine kinases. (nih.gov)
  • The dual-specificity tyrosine phosphorylation-regulated kinase DYRK1A is a serine/threonine kinase involved in neuronal differentiation and synaptic plasticity and a major candidate of Down syndrome brain alterations and cognitive deficits. (jneurosci.org)
  • The anti-inflammatory agent pyridinylimidazole and its analogs (SB [SmithKline Beecham] compounds) are highly potent and selective inhibitors of p38, but not of the closely-related ERK2, or other serine/threonine kinases. (rcsb.org)
  • Its lipid transfer activity is negatively regulated by casein kinase, a serine/threonine-protein kinase which phosphorylates STARD10 on a serine residue at position 284 (Olayioye et al. (reactome.org)
  • Violin plots show distribution of expression levels for Dual specificity tyrosine-phosphorylation-regulated kinase 2 (SMED30002728) in cells (dots) of each of the 12 neoblast clusters. (stowers.org)
  • Expression of Dual specificity tyrosine-phosphorylation-regulated kinase 2 (SMED30002728) in the t-SNE clustered sub-lethally irradiated X1 and X2 cells. (stowers.org)
  • Violin plots show distribution of expression levels for Dual specificity tyrosine-phosphorylation-regulated kinase 2 (SMED30002728) in cells (dots) of each of the 10 clusters of sub-leathally irradiated X1 and X2 cells. (stowers.org)
  • Global Dual Specificity Tyrosine Phosphorylation Regulated Kinase 1A market will reach xxx Million USD in 2020 with CAGR xx% 2020-2025. (courant.biz)
  • Homeodomain-interacting protein kinases (HIPKs) belong to the CMGC kinase family and are closely related to dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs). (nature.com)
  • Upon phosphorylation by the receptors, Smad complexes translocate into the nucleus, where they cooperate with sequence-specific transcription factors to regulate gene expression. (nih.gov)
  • hPTTG phosphorylation is mediated by cyclin-dependent kinase 2 (CDC2) and expression is regulated by specificity protein 1 (SP1). (endocrine-abstracts.org)
  • This has led to the development of a range of ERK1/2 inhibitors (ERKi) that either inhibit kinase catalytic activity (catERKi) or additionally prevent the activating pT-E-pY dual phosphorylation of ERK1/2 by MEK1/2 (dual-mechanism or dmERKi). (babraham.ac.uk)
  • However, the mechanism through which phosphorylation regulates the activity of PIF7 is unclear. (elifesciences.org)
  • Phosphoenrichment-coupled mass spectrometry analysis revealed specific subsynaptic- and trisomy-associated iGluR phosphorylation signature, concomitant with differential subsynaptic kinase and phosphatase composition of Ts65Dn hippocampal subsynaptic compartments. (logic2010.org)
  • dual-specificity tyrosine phosphorylation-regulated kinase 1) also influences NMDAR surface manifestation and function much like NMDAR rules by Hsa21 gene products (Grau et al. (logic2010.org)
  • A prominent example for the decisive impact of lipid rafts on signaling is LRP6, whose localization to the same lipid rafts domain as the kinase CK1γ is crucial for its successful phosphorylation and the subsequent activation of the signalosome, hence WNT/β-catenin signaling. (frontiersin.org)
  • OMIM:615812]) is a rare autosomal dominant disorder caused by pathogenic variants in the dual-specificity tyrosine phosphorylation-regulated kinase 1B gene ( DYRK1B ) located on chromosome 19q13.2 [ 1 ]. (biomedcentral.com)
  • Protein phosphorylation is the most common post-translation modification of proteins and regulates many biological processes. (lu.se)
  • Phosphoinositide 3-kinase (PI3K) as a key regulator of lipid signal has been reported to be involved in autophagy. (frontiersin.org)
  • STARD10 is thought to function as a dual specificity lipid transfer protein capable of shuttling phosphatidylcholine and phosphatidylethanolamine between membranes. (reactome.org)
  • Our findings bring a new perspective on how lipid metabolism is regulated and may help understand why some people may be more resistant to metabolic problems while others are more vulnerable," said Wang. (neurosciencenews.com)
  • The protein encoded by this gene is a member of the dual specificity protein phosphatase subfamily. (nih.gov)
  • In mammalian cells, there are three types of PI3K with distinct substrate specificities. (frontiersin.org)
  • Different members of the family of dual specificity phosphatases show distinct substrate specificities for various MAP kinases, different tissue distribution and subcellular localization, and different modes of inducibility of their expression by extracellular stimuli. (nih.gov)
  • Here we demonstrate that p38 MAPK gamma (p38γ) acts as a CDK-like kinase and thus cooperates with CDKs, regulating entry into the cell cycle. (nature.com)
  • They negatively regulate members of the mitogen-activated protein (MAP) kinase superfamily (MAPK/ERK, SAPK/JNK, p38), which is associated with cellular proliferation and differentiation. (nih.gov)
  • Mitogen-activated protein kinase (MAPK) cascades transmit environmental signals and induce stress and defence responses in plants. (biorxiv.org)
  • The genetic changes abnormally activate the protein, which disrupts the tightly regulated RAS/MAPK signaling pathway in many types of cells. (medlineplus.gov)
  • DUSP9, a Dual-Specificity Phosphatase with a Key Role in Cell Biology and Human Diseases. (nih.gov)
  • Expression of Dual-Specificity Phosphatase 9 in Placenta and Its Relationship with Gestational Diabetes Mellitus. (nih.gov)
  • The alteration of iGluR phosphoresidues in Ts65Dn hippocampi, together with the kinase/phosphatase signature, identifies potential novel restorative targets for the treatment of glutamatergic dysfunctions in DS. (logic2010.org)
  • This phosphopattern is in agreement with the concomitant subsynaptic-specific increase of kinase manifestation and phosphatase downregulation in Ts65Dn mice hippocampi. (logic2010.org)
  • Overall, our results demonstrate an modified phosphopattern in CB2R-IN-1 the glutamatergic synapse, together with the identification of a protein kinase/phosphatase biochemical signature in the Ts65Dn murine model, which may represent novel restorative focuses on for DS synaptopathy. (logic2010.org)
  • Specificity and mechanism of action of some commonly used protein kinase inhibitors. (rndsystems.com)
  • Many kinases in these pathways are validated drug targets and kinase inhibitors are first-line treatment for several advanced cancers. (escholarship.org)
  • The first generation of kinase inhibitors were intended to target single proteins. (escholarship.org)
  • However, the highly conserved active sites of protein kinases prohibited the design of perfectly selective inhibitors. (escholarship.org)
  • Unexpectedly, this specificity problem led to the development of clinically useful, multi-targeted kinase inhibitors. (escholarship.org)
  • The design of dual PI3K/PTK inhibitors is chemically challenging because PI3Ks and PTKs are members of significantly divergent kinase families. (escholarship.org)
  • Anderson, B.D. Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties. (eurekaselect.com)
  • The recent identification of associations between protein kinases and AD pathology has spurred interest in tyrosine kinase inhibitors (TKIs) as potential strategic therapeutic agents for AD. (biomedcentral.com)
  • These findings suggest that tyrosine kinase inhibitors (TKIs) could be leveraged as therapeutic agents for AD. (biomedcentral.com)
  • Selective compounds have been developed that target either the extracellular ligand-binding region of the EGFR (including a number of monoclonal antibodies [MAbs], immunotoxins, and ligand-binding cytotoxic agents) or the intracellular tyrosine kinase region (including various small-molecule inhibitors). (medscape.com)
  • Bithiazole Inhibitors of Phosphatidylinositol 4-Kinase (PI4KIIIβ) as Broad-Spectrum Antivirals Blocking the Replication of SARS-CoV-2, Zika Virus and Human Rhinoviruses. (cdc.gov)
  • Hematopoietic progenitor kinase 1 (HPK1) regulates stress responses, proliferation, and apoptosis in hematopoietic cells. (aacrjournals.org)
  • In contrast, the activation of the MAP kinase ERK2 (extracellular-signal-regulated kinase 2) leads to cellular differentiation or proliferation. (rcsb.org)
  • Long noncoding RNA (lncRNAs) are vital noncoding RNAs (ncRNAs) that regulate fat accumulation, including the processes of proliferation, differentiation, and hypertrophy of adipocytes [ 6 , 7 ]. (animbiosci.org)
  • Casein kinase II (CK II) has been implicated in regulating multiple processes related to cell growth, proliferation, and differentiation. (rupress.org)
  • WNT signaling regulates central developmental processes of the cell, including cell fate, cell proliferation, cell migration and adult homeostasis. (frontiersin.org)
  • VEGF-induced pMF was attenuated by the MEK/ERK inhibitor U0126 [1,4-diamino-2,3-dicyano-1,4-bis( o -aminophenylmercapto)butadiene] and was abolished by the phosphotidinositol 3 kinase/Akt inhibitor LY294002 [2-(4-morpholinyl)-8-phenyl-1(4 H )-benzopyran-4-one hydrochloride], demonstrating that ERK mitogen-activated protein kinases and Akt are both required for full expression of VEGF-induced pMF. (jneurosci.org)
  • Identification of a novel inhibitor of mitogen-activated protein kinase kinase. (rndsystems.com)
  • The mitogen-activated protein (MAP) kinases are important signaling molecules that participate in diverse cellular events and are potential targets for intervention in inflammation, cancer, and other diseases. (rcsb.org)
  • In the poster section, Joanna Shisler (University of Illinois at Urbana-Champaign [UIUC], Urbana) reported that the modified virus, Ankara, activates nuclear factor κB through the mitogen-activated protein kinase, extracellular signal-regulated kinase (MEK)/extracellular signal-regulated kinase (ERK) pathway, possibly facilitating the host immune response. (cdc.gov)
  • In the poster section, Joanna Shisler (University of Illinois at Urbana-Champaign [UIUC], Urbana) reported that the modified virus, Ankara, activates nuclear factor κB through the mitogen-activated protein kinase, extracellular signal–regulated kinase (MEK)/extracellular signal–regulated kinase (ERK) pathway, possibly facilitating the host immune response. (cdc.gov)
  • In recent years, the search for intracellular signaling integrator downstream of receptor tyrosine kinases provided valuable novel substrates. (springer.com)
  • The HER (erbB) family of transmembrane receptor tyrosine kinases is one of the cytostatic targets in tumor cell growth and survival. (medscape.com)
  • Collectively, these results unraveled a novel and broad role of PI3K in plant immunity which promoted stomatal closure and PR gene expression possibly via regulating ROS production. (frontiersin.org)
  • This gene product shows selectivity for members of the ERK family of MAP kinases and is localized to the cytoplasm and nucleus. (nih.gov)
  • The MAP2K1 gene provides instructions for making a protein known as MEK1 protein kinase. (medlineplus.gov)
  • The identified MAP2K1 gene mutation is a germline mutation that replaces the amino acid glutamic acid with the amino acid glycine at position 102 (written as Glu102Gly or E102G) in MEK1 protein kinase. (medlineplus.gov)
  • Casein kinase II is a predominantly nuclear enzyme. (rupress.org)
  • VEGFA-165 signals by activating its receptor tyrosine kinase VEGF receptor-2 (VEGFR-2). (jneurosci.org)
  • Because another growth/trophic factor that signals via a receptor tyrosine kinase (brain derived neurotrophic factor) elicits a long-lasting facilitation of respiratory motor activity in the phrenic nerve, we tested the hypothesis that VEGFA-165 elicits similar phrenic motor facilitation (pMF). (jneurosci.org)
  • A survey of different adult chicken tissues revealed substantial tissue-specific differences in the levels of CK II protein, but no evidence was obtained for pronounced tissue specificity in the expression of individual CK II subunits. (rupress.org)
  • The protein interaction landscape of the human CMGC kinase group. (nature.com)
  • U0126 is a potent and selective non-competitive inhibitor of MAP kinase kinase. (rndsystems.com)
  • The most distal of these cadherins is thought to beresponsible for binding specificity, transmembrane domains and carboxy-terminal intracellulardomains. (logic2010.org)
  • MEKs, involved in MAP pathways, are principal examples of dual-specificity kinases. (wikipedia.org)
  • Cancer cells survive by co-opting intracellular growth pathways regulated through kinase signaling. (escholarship.org)
  • In addition, the peroxisome proliferator-activated receptor, phosphatidylinositol-3-kinase-protein kinase B, and mammalian target of rapamycin pathways were enriched in the pathway analysis. (animbiosci.org)
  • Other common examples include: ADK1 (Arabidopsis dual specificity kinase 1) CLK1, CLK2, CLK3, CLK4 DSTYK DYRK1A, DYRK1B, DYRK2, DYRK3, DYRK4 Mps1p TESK1, TESK2 TTK The systematic name of this enzyme class is ATP:protein phosphotransferase (Ser/Thr- and Tyr-phosphorylating). (wikipedia.org)
  • The relatively short intracellular domains interact with a variety of cytoplasmic proteins,such as b-catenin, to regulate cadherin function. (logic2010.org)
  • We determined the crystal structures of HIPK3 and DYRK1A bound to abemaciclib, showing a similar binding mode to the hinge region of the kinase as observed for Cdk6. (nature.com)
  • These phosphatases inactivate their target kinases by dephosphorylating both the phosphoserine/threonine and phosphotyrosine residues. (nih.gov)
  • This raises the question of how the specificity of the ligand-induced signaling is achieved. (nih.gov)
  • We review the molecular basis for the specificity and versatility of signaling by the many ligands through this conceptually simple signal transduction mechanism. (nih.gov)
  • Her seminal early papers on GPCR signaling demonstrated that dopamine receptors are the target of antipsychotic drugs, that muscarinic receptors inhibit adenylate cyclase and that phospholipase C and CaM kinase II activation mediate cardiac hypertrophy. (aspet.org)
  • Integrin CD11b negatively regulates Mincle-induced signaling via the Lyn-SIRPα-SHP1 complex. (rndsystems.com)
  • At a molecular level, this translated into simultaneous inhibition of critical nodes in a signaling network regulated by multiple inputs and levels of feedback. (escholarship.org)
  • Extrapolating/Translating these values to the membrane of a "normal sized" cell yields a raft abundance, that, by far, outnumbers the membrane-associated pathway components of most individual signaling pathway, such as receptor and kinases. (frontiersin.org)
  • For most individual signaling pathway, this quantitative point of view would imply, that rafts clearly outnumber the membrane-associated pathway components, such as receptor and kinases. (frontiersin.org)
  • As a biologically important example we have studied the complex formed by cyclins and cyclin-dependent kinases (CDKs), which play an essential role in the control of the eukaryotic cell cycle. (lu.se)
  • A subset of these compounds potently, and sometimes selectively, inhibit the mammalian target of rapamycin (mTOR), a Ser/Thr kinase in the PI3K family, placing mTOR in kinase space at the intersection of PI3Ks and PTKs. (escholarship.org)
  • Evidence has shown that lncIMF4 regulates porcine intramuscular preadipocytes by attenuating autophagy to inhibit lipolysis [ 8 ]. (animbiosci.org)
  • Recognizes endogenous levels of total p44/p42 MAP kinase (Erk1,2) protein. (reageno.com)
  • This may be relevant to the suggestion of kinase-independent effects of ERK1/2 and the therapeutic use of ERKi. (babraham.ac.uk)
  • The RAS-regulated RAF-MEK1/2-ERK1/2 signalling pathway is frequently de-regulated in human cancer. (babraham.ac.uk)
  • However, recent studies have suggested that BRAFi/MEKi and ERK1/2i resistance can arise through activation of a parallel signalling pathway leading to activation of ERK5, an unusual protein kinase that contains both a kinase domain and a transcriptional transactivation domain. (babraham.ac.uk)
  • Phosphoinositide 3-kinase (PI3K) plays a vital role in plant response to abiotic stress. (frontiersin.org)
  • At the International Centre for Kinase Profiling (ICKP) we understand that ascertaining how your compound behaves in relation to the multitude of related enzymes is critical. (mrc.ac.uk)
  • The cell cycle is a tightly regulated process that is controlled by the conserved cyclin-dependent kinase (CDK)-cyclin protein complex 1 . (nature.com)
  • Olfactory perception in C. elegans is simpler than in larger organisms, such as humans, which helps researchers like Mutlu and her colleagues to study how olfaction regulates bodily processes. (neurosciencenews.com)
  • It does not crossreact with either JNK/ SAPK or p38 MAP kinase. (reageno.com)
  • Two kinase families, phosphoinositide-3-kinases (PI3Ks) and protein tyrosine kinases (PTKs), are activated by mutations and amplifications in a disproportionate number of human cancers. (escholarship.org)
  • The known mutations change single amino acids in MEK1 protein kinase. (medlineplus.gov)
  • Mutations in the Methyltransferase Motifs of L Protein Attenuate Newcastle Disease Virus by Regulating Viral Translation and Cell-to-Cell Spread. (cdc.gov)
  • The family is defined by structural similarity of their kinase domains and their capability to autophosphorylate on tyrosine residues. (antibodies-online.com)
  • In the present study, we investigated whether the TKIs ibrutinib, PD180970, and cabozantinib, which have different on-targets, selectively regulate AD pathology in 3.5- to 4-month-old 5xFAD mice (a model of the early phase of AD). (biomedcentral.com)
  • Within the HIPK family, HIPK1 and HIPK2 are the most closely related members, sharing about 93% sequence identity in their kinase domains, while HIPK3 is slightly less conserved with 87% identity. (nature.com)
  • Like the endogenous HPK1, both wild-type HPK1 and its kinase-dead mutant, HPK1-M46, overexpressed in Panc-1 cells, were also targeted by proteasome-mediated degradation. (aacrjournals.org)
  • To better understand the function(s) and regulation of this ubiquitous kinase, it is important to know its subcellular distribution. (rupress.org)
  • These results strongly suggest that CK II functions primarily in regulating nuclear activities, and that the two catalytic subunits, alpha and alpha', may carry out overlapping functions. (rupress.org)
  • They also determined that the neurons act through a selective neural circuit and a neuroendocrine pathway to directly regulate fat metabolism. (neurosciencenews.com)
  • Here, we report that specific but not all olfactory neurons actively regulate fat metabolism without affecting eating behaviors in Caenorhabditis elegans, and identified specific odors that reduce fat mobilization via inhibiting these neurons. (neurosciencenews.com)
  • The metabolism of 2,3,7,8-TCDD and related compounds is required for urinary and biliary excretion, and the rate of metabolism is thought to play a major role in regulating the rate of elimination (and detoxification) of these compounds (Van den Berg et al. (cdc.gov)
  • yet how mechanistically olfaction regulates metabolic homeostasis remains unclear. (neurosciencenews.com)
  • Label-free SARS-CoV-2 detection and classification using phase imaging with computational specificity. (cdc.gov)
  • Our results suggest that ERKi, including current clinical candidates, act as 'kinase degraders', driving the proteasome-dependent turnover of their major target, ERK2. (babraham.ac.uk)
  • Necessary for the normal dephosphorylation of the long-lasting phosphorylated forms of spinal MAPK1/3 and MAP kinase p38 induced by peripheral surgery, which drives the resolution of acute postoperative allodynia (By similarity). (nih.gov)