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Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and

Sylwia Wasiak1, Dean Gilham1, Laura M Tsujikawa1

  • 1Resverlogix Corp., Calgary, Canada.

Data in Brief
|August 30, 2016
PubMed

Insights

Apabetalone (RVX-208), a bromodomain and extraterminal (BET) inhibitor, increases apolipoprotein A-I (ApoA-I) production. This suggests potential for treating atherosclerotic cardiovascular disease by modulating HDL levels.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Atherosclerotic cardiovascular disease (ASCVD) is a leading cause of mortality.
  • Bromodomain and extraterminal (BET) proteins are epigenetic regulators involved in gene expression.
  • Targeting BET proteins offers a potential therapeutic strategy for ASCVD.

Purpose of the Study:

  • To investigate the effects of apabetalone (RVX-208), a BET inhibitor, on apolipoprotein A-I (ApoA-I) expression and production.
  • To analyze gene expression changes induced by RVX-208 in relevant cellular models.

Main Methods:

  • Treatment of primary human and African green monkey hepatocytes with RVX-208 and JQ1 (a comparator BET inhibitor).
  • Measurement of apolipoprotein A-I (ApoA-I) mRNA expression and protein production.
  • Microarray-based gene expression analysis of human whole blood and primary human hepatocytes.

Main Results:

  • RVX-208 and JQ1 significantly increased ApoA-I mRNA expression and production in hepatocytes.
  • Gene expression profiling revealed distinct patterns of transcriptional changes in response to RVX-208 treatment.
  • Apabetalone demonstrated its capacity to modulate pathways implicated in cardiovascular disease.

Conclusions:

  • Apabetalone (RVX-208) effectively increases ApoA-I production, a key component of high-density lipoprotein (HDL).
  • The findings support the therapeutic potential of apabetalone for atherosclerotic cardiovascular disease.
  • RVX-208's mechanism involves the inhibition of BET proteins, impacting cardiovascular disease-related pathways.
Keywords:
African green monkeyApoA-IApolipoprotein A-IBET inhibitorBET proteinsBromodomainGene expressionJQ1MicroarraysPrimary human hepatocytesRVX-208Vascular inflammation

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