Inhibition of BRD4 suppresses tumor growth and enhances iodine uptake in thyroid cancer

Biochem Biophys Res Commun. 2016 Jan 15;469(3):679-85. doi: 10.1016/j.bbrc.2015.12.008. Epub 2015 Dec 18.

Abstract

Thyroid cancer is a common malignancy of the endocrine system. Although radioiodine (131)I treatment on differentiated thyroid cancer is widely used, many patients still fail to benefit from (131)I therapy. Therefore, exploration of novel targeted therapies to suppress tumor growth and improve radioiodine uptake remains necessary. Bromodomain-containing protein 4 (BRD4) is an important member of the bromodomain and extra terminal domain family that influences transcription of downstream genes by binding to acetylated histones. In the present study, we found that BRD4 was up-regulated in thyroid cancer tissues and cell lines. Inhibition of BRD4 in thyroid cancer cells by JQ1 resulted in cell cycle arrest at G0/G1 phase and enhanced (131)I uptake in vitro and suppressed tumor growth in vivo. Moreover, JQ1 treatment suppressed C-MYC but enhanced NIS expression. We further demonstrated that BRD4 was enriched in the promoter region of C-MYC, which could be markedly blocked by JQ1 treatment. In conclusion, our findings revealed that the aberrant expression of BRD4 in thyroid cancer is possibly involved in tumor progression, and JQ1 is potentially an effective chemotherapeutic agent against human thyroid cancer.

Keywords: BRD4; C-MYC; JQ1; NIS; Thyroid cancer.

MeSH terms

  • Cell Cycle Proteins
  • Cell Line, Tumor
  • Cell Proliferation / radiation effects
  • Gene Expression Regulation, Neoplastic / radiation effects
  • Humans
  • Iodine Radioisotopes / pharmacokinetics*
  • Iodine Radioisotopes / therapeutic use
  • Metabolic Clearance Rate
  • Nuclear Proteins / metabolism*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / therapeutic use
  • Thyroid Neoplasms / metabolism*
  • Thyroid Neoplasms / pathology*
  • Thyroid Neoplasms / radiotherapy
  • Transcription Factors / metabolism*
  • Up-Regulation

Substances

  • BRD4 protein, human
  • Cell Cycle Proteins
  • Iodine Radioisotopes
  • Nuclear Proteins
  • Radiopharmaceuticals
  • Transcription Factors