TargetRx Atlas

MRNA basic information

  • mRNA ID:ENST00000236850
  • Gene Name:APOA1
  • mRNA database:Ensembl
  • mRNA expression :up-regulated
  • mRNA Method:RT-PCR
  • mRNA Pathway:NA
  • Evidence:validated
  • (mRNA-drug)

Drug basic information

  • Drug ID:DB12000
  • Drug Name:Apabetalone
  • Drug Method:up-regulated the gene expression

Disease basic infommation

  • Disease:atherosclerosis
  • Tissue:tissues

Other information

  • Title:RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist
  • Journal:Plos One
  • Published:2013
  • PubMed ID:24391744
  • Abstract:Increased synthesis of Apolipoprotein A-I (ApoA-I) and HDL is believed to provide a new approach to treating atherosclerosis through the stimulation of reverse cholesterol transport. RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. Using binding assays and X-ray crystallography, we now show that RVX-208 selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. siRNA experiments further suggest that induction of ApoA-I mRNA is mediated by BET family member BRD4. These data indicate that RVX-208 increases ApoA-I production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis.
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