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  • inhibitor
  • Pretreatment with Triton X-100, a detergent that damages the endocardial endothelium (EE), or with 1H-(1,2,4)oxadiazolo-(4,3-a)quinoxalin-1-one (ODQ), a specific inhibitor of soluble guanylate cyclase, or with the cGMP-activated protein kinase (PKG) inhibitor KT5328, abolished ANG II-mediated inotropism. (biologists.org)
  • This selectivity is definitely impressive, as no medically authorized kinase inhibitor is definitely selective for Src over additional SFKs or Abl kinase (Davis et al. (brain-tumor-cancer-information.com)
  • Our study on the detergent-reconstituted enzyme shows that chlorophyllide a and phytol, the products of chlorophyll a hydrolysis, affect the activity, but their effects are antagonistic: chlorophyllide a activates chlorophyllase while phytol acts as the inhibitor. (docplayer.net)
  • substrates
  • In contrast to polyisoprenoid phosphates serving as cofactors in the biosynthesis of glycoproteins, glucosyl phosphatidyl inositol (GPI) anchor or bacterial peptidoglycan, the biological importance of polyprenols and dolichols still remains a question of debate besides their function of reservoir of substrates for kinase. (docplayer.net)
  • receptor
  • Extracellular hormones such as glucagon and epinephrine begin an intracellular signalling cascade that triggers protein kinase A activation by first binding to a G protein-coupled receptor (GPCR) on the target cell. (wikipedia.org)
  • Incubation of rat brain frontal cortical slices with 6-chloro-7,8-dihydroxy-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1 H -3-benzazepine (SKF83959), a recently identified selective agonist of the PI-linked D 1 -like dopamine receptor, elicited transient time- and dose-dependent stimulations of cyclin-dependent kinase 5 (cdk5) and calcium/calmodulin-dependent protein kinase II (CaMK II) activities. (aspetjournals.org)
  • 12 Capsaicin, by binding to the ligand-gated vanilloid-sensitive transient receptor potential channel, TRPV1, on presynaptic terminals, directly catalyzes Ca +2 entry and also effects a depolarization that activates presynaptic calcium channels, as well as releasing Ca +2 from intracellular reticuli whose membranes contain TRPV1 channels, 13 all of which result in the release of glutamate and SP from primary nociceptor terminals. (asahq.org)
  • subtypes
  • Also, different mGluR subtypes are found predominantly in different parts of the body. (wikipedia.org)
  • The molecular identification of individual NTPDase subtypes, genetic engineering, mutational analyses, and the generation of subtype-specific antibodies have resulted in considerable insights into enzyme structure and function. (springer.com)
  • presynaptic
  • For example, one study found that Group I mGluRs are located mostly on postsynaptic parts of cells, while groups II and III are mostly located on presynaptic elements, though they have been found on both pre- and postsynaptic membranes. (wikipedia.org)
  • genome
  • Normal cellular homologs of v-Raf and v-Mil were soon found in both the mouse and chicken genome (hence the name c-Raf for the normal cellular Raf gene), and it became clear that these too had a role in regulating growth and cell division. (wikipedia.org)
  • calcium
  • In comparison to calcium (Ca), the most abundant cation in the human body, Mg 2+ displays higher affinity for oxygen donor ligands, that is negatively charged carboxylates and phosphates or enolate moieties (WOLF, CITTADINI 2003). (docplayer.net)
  • negatively
  • The close proximity of these two domains as well as several lines of experimental data suggest that they act as a single unit to negatively regulate the activity of the protein kinase domain, by direct physical interaction. (wikipedia.org)
  • subfamily
  • Human T-lymphotropic virus type 1 (HTLV1), a member of the delta-retroviridae subfamily, was the first human pathogenic retrovirus discovered and found to contribute to cancer development , . (pubmedcentralcanada.ca)
  • family
  • C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases, from the TKL (Tyrosine-kinase-like) group of kinases. (wikipedia.org)
  • Several infants with severe forms of long-QT syndrome (LQTS) who displayed life-threatening ventricular arrhythmias together with delayed neurodevelopment and epilepsy were found to have mutations in either this gene or another member of the calmodulin gene family (PMID:23388215). (nih.gov)
  • Nevertheless, selective pharmacologic inhibition of Src kinase is definitely challenging, as the eight users from the Src kinase family members are extremely conserved, and few small-molecule kinase inhibitors can distinguish between them (Anastassiadis et al. (brain-tumor-cancer-information.com)
  • Users of these family members inhibit Src kinase with nanomolar strength and a lot more than 80-fold selectivity on the carefully related Hck and Abl kinase (Kleiner et al. (brain-tumor-cancer-information.com)
  • Included in spinal responses to peripheral nerve input are the mitogen-activated protein kinases (MAPKs), a family of serine-threonine protein kinases that are activated in spinal cord by noxious peripheral stimuli and play important roles in modulating signal transduction, both acutely by protein phosphorylation and chronically by affecting gene transcription. (asahq.org)
  • known
  • RAF proto-oncogene serine/threonine-protein kinase, also known as proto-oncogene c-RAF or simply c-Raf or even Raf-1, is an enzyme that in humans is encoded by the RAF1 gene. (wikipedia.org)
  • several
  • Several years later after the discovery of c-Raf, two further related kinases were described: A-Raf and B-Raf. (wikipedia.org)
  • Within the past decade, ectonucleotidases belonging to several enzyme families have been discovered, cloned and characterized. (springer.com)
  • gene
  • The first Raf gene, v-Raf was found in 1983. (wikipedia.org)
  • A year later, another transforming gene was found in the avian retrovirus MH2, named v-Mil - that turned out to be highly similar to v-Raf. (wikipedia.org)
  • Pseudogenes of this gene are found on chromosomes 10, 13, and 17. (nih.gov)
  • activation
  • Moreover, we found that cdk5 phosphorylates dopamine and cAMP-regulated phosphoprotein at Thr75, whereas CaMK II is responsible for the activation of cAMP response element-binding protein in response to SKF83959 stimulation. (aspetjournals.org)
  • 12 Activation of the inotropic receptors causes a postsynaptic membrane depolarization and Ca +2 entry, whereas metabotropic receptors activate various kinases and also indirectly increase [Ca +2 ] in dorsal horn neurons of the spinal cord. (asahq.org)
  • demonstrate
  • Our results demonstrate, for the first time, that the expression of enzymes involved in chlorophyll catabolism is light-controlled. (docplayer.net)
  • group
  • The chemicals 2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV) and eglumegad activate only group II mGluRs, while 2-amino-4-phosphonobutyrate (L-AP4) activates only group III mGluRs. (wikipedia.org)
  • 7 Note Set 11 7 enol phosphates (like PEP) have a high Phosphate Group-Transfer Potential PGTP of PEP is 14.8 kcal/mol G ' = kcal/mol G' = reversible 10. (docplayer.net)
  • cell
  • We found virus type-specific (HTLV1 vs. HTLV3), expression-specific (Tax1 vs. Tax3) and cell-type-specific (T lymphocytes vs. kidney epithelial cells) changes in the metabolite profiles. (pubmedcentralcanada.ca)
  • high
  • Many small-molecule kinase inhibitors had been found out in high-throughput displays and their marketing was led by Lipinskis rule-of-five (RO5) that explain top features of some orally bioavailable medicines (Lipinski et al. (brain-tumor-cancer-information.com)
  • interest
  • 2001). Recently, compounds such as for example macrocycles that explore chemical substance space beyond RO5-compliant substances have received interest as selective enzyme inhibitors (Driggers et al. (brain-tumor-cancer-information.com)
  • function
  • All cells function to maintain the resting condition adenylate metabolite concentrations as best as possible in the face of increasing ATP demand. (hindawi.com)