When are the BET factors the most sensitive to bromodomain inhibitors?

Transcription. 2013 Mar-Apr;4(2):54-7. doi: 10.4161/trns.23191. Epub 2013 Feb 14.

Abstract

The recent publication of two detailed studies of mouse spermatogenesis, either after chemical inhibition of the BET bromodomains, or in the context of genetic alterations of one specific BET member, Brdt, provides the unique opportunity to assess the functional impact of BET bromodomain inhibitors.

Keywords: Brd2; Brd3; Brd4; Brdt; acetylation; cancer; chromatin; histone; infertility; pTEFb; spermatogenesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azepines / pharmacology
  • Chromosomal Proteins, Non-Histone
  • Gene Expression Regulation / drug effects
  • Male
  • Mice
  • Nerve Tissue Proteins / antagonists & inhibitors
  • Nerve Tissue Proteins / metabolism*
  • Nuclear Proteins / antagonists & inhibitors*
  • Nuclear Proteins / genetics
  • Nuclear Proteins / metabolism
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / metabolism
  • Receptors, Cell Surface / antagonists & inhibitors
  • Receptors, Cell Surface / metabolism*
  • Spermatogenesis / drug effects
  • Transcription Factors / antagonists & inhibitors*
  • Transcription Factors / metabolism
  • Triazoles / pharmacology

Substances

  • (+)-JQ1 compound
  • Azepines
  • BRDT protein, mouse
  • Brd2 protein, mouse
  • Brd3 protein, mouse
  • Brd4 protein, mouse
  • Chromosomal Proteins, Non-Histone
  • Dner protein, mouse
  • Nerve Tissue Proteins
  • Nuclear Proteins
  • Receptors, Cell Surface
  • Transcription Factors
  • Triazoles
  • Protein Serine-Threonine Kinases