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  • RPD3
  • The report provides comprehensive information on the Histone Deacetylase 2 (Transcriptional Regulator Homolog RPD3 or YY1-Associated Factor 1 or EC 3.5.1.98), targeted therapeutics, complete with analysis by indications, stage of development, mechanism of action (MoA), route of administration (RoA) and molecule type. (reportsnreports.com)
  • Additionally, the report provides an overview of key players involved in Histone Deacetylase 2 (Transcriptional Regulator Homolog RPD3 or YY1-Associated Factor 1 or EC 3.5.1.98) targeted therapeutics development and features dormant and discontinued projects. (reportsnreports.com)
  • antibody
  • Indeed, a recombinant, humanized, monoclonal anti-Her-2 antibody, trastuzumab (Herceptin), has been shown to dephosphorylate and down-regulate Her-2 levels and signaling as well as to exhibit clinical efficacy against breast cancer ( 11 ). (aacrjournals.org)
  • Inhibition
  • The fact that the incidence of cytomegalic inclusion disease (CID) is intimately related to viral burden suggests that the inhibition of viral production by the specific repression of viral gene expression will reduce the occurrence of CID [ 2 ]. (pubmedcentralcanada.ca)
  • Depletion of c-Raf-1 and inhibition of Erk1/2 phosphorylation as well as attenuation of pAKT by GA or 17-AAG leads to disruption of the Raf-mitogen-activated protein kinase (MAPK)/Erk kinase-MAPK (Erk1/2) and PI3K/AKT signaling, resulting in cytostasis and apoptosis of cancer cells ( 27 ). (aacrjournals.org)
  • endothelial
  • Objective- Arginase 2 (Arg2) is a critical target in atherosclerosis because it controls endothelial nitric oxide, proliferation, fibrosis, and inflammation. (ahajournals.org)
  • Tsukahara T, Haniu H, Matsuda Y. Cyclic Phosphatidic Acid Inhibits Alkyl-Glycerophosphate-Induced Downregulation of Histone Deacetylase 2 Expression and Suppresses the Inflammatory Response in Human Coronary Artery Endothelial Cells. (medsci.org)
  • phosphorylation
  • Following LAQ824 treatment, the cell membrane association, autotyrosine phosphorylation, and colocalization of Her-2 with HER-3 also declined. (aacrjournals.org)
  • human
  • These findings suggest that LAQ824 is active against human breast cancer cells and has the potential to improve the efficacy of trastuzumab, taxotere, gemcitabine, and epothilone B against breast cancer with Her-2/ neu amplification. (aacrjournals.org)
  • activity
  • Epigenetic silencing can be reversed in vitro using agents with hypomethylating or histone deacetylase inhibitory (HDI) activity. (aacrjournals.org)
  • The combination of 5-aza-2'-deoxycytidine (DAC), a potent hypomethylating agent, and valproic acid (VPA), an antiepileptic drug with HDI activity, has synergistic antileukemia activity in vitro. (aacrjournals.org)
  • Activation
  • Dimerization of Her-2 with HER-3 results in activation and signaling through the phosphatidylinositol 3-kinase (PI3K)/AKT and Ras-Raf-extracellular signal-regulated kinase (Erk) pathways, promoting cell proliferation and survival, and is associated with poor prognosis in breast cancer ( 4 , 5 ). (aacrjournals.org)
  • However, resistance to trastuzumab, given alone or in combination with chemotherapeutic agents, is common, involving mechanisms that involve the activation of PI3K/AKT and/or Erk1/2 signaling ( 16 -18 ). (aacrjournals.org)
  • potent
  • Lovastatin was found to be 2 times more potent than its predecessor, mevastatin, the first discovered statin. (drugbank.ca)