Cellular and Molecular Life Sciences

, Volume 69, Issue 11, pp 1745–1753

Targeting transcription factor corepressors in tumor cells

Authors

  • Aristeidis G. Vaiopoulos
    • Department of Biological ChemistryUniversity of Athens Medical School
  • Ioannis D. Kostakis
    • Department of Biological ChemistryUniversity of Athens Medical School
  • Kalliopi Ch. Athanasoula
    • Department of Biological ChemistryUniversity of Athens Medical School
    • Department of Biological ChemistryUniversity of Athens Medical School
Visions and reflections

DOI: 10.1007/s00018-012-0986-5

Cite this article as:
Vaiopoulos, A.G., Kostakis, I.D., Athanasoula, K.C. et al. Cell. Mol. Life Sci. (2012) 69: 1745. doi:10.1007/s00018-012-0986-5

Abstract

By being the “integration” center of transcriptional control as they move and target transcription factors, corepressors fine-tune the epigenetic status of the nucleus. Many of them utilize enzymatic activities to modulate chromatin through histone modification or chromatin remodeling. The clinical and etiological relevance of the corepressors to neoplastic growth is increasingly being recognized. Aberrant expression or function (both loss and gain of) of corepressors has been associated with malignancy and contribute to the generation of transcriptional “inflexibility” manifested as distorted signaling along certain axes. Understanding and predicting the consequences of corepressor alterations in tumor cells has diagnostic and prognostic value, and also have the capacity to be targeted through selective epigenetic regimens. Here, we evaluate corepressors with the most promising therapeutic potential based on their physiological roles and involvement in malignant development, and also highlight areas that can be exploited for molecular targeting of a large proportion of clinical cancers and their complications.

Keywords

CorepressorsHDACInhibitorCancerTherapy

Copyright information

© Springer Basel AG 2012