Pharmaceuticals (May 2022)

HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer

  • Cristina Maccallini,
  • Alessandra Ammazzalorso,
  • Barbara De Filippis,
  • Marialuigia Fantacuzzi,
  • Letizia Giampietro,
  • Rosa Amoroso

DOI
https://doi.org/10.3390/ph15060667
Journal volume & issue
Vol. 15, no. 6
p. 667

Abstract

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Triple negative breast cancer (TNBC) is an urgent as well as huge medical challenge, which is associated with poor prognosis and responsiveness to chemotherapies. Since epigenetic changes are highly implicated in TNBC tumorigenesis and development, inhibitors of histone deacetylases (HDACIs) could represent a promising therapeutic strategy. Although clinical trials involving single HDACIs showed disappointing results against TNBC, recent studies emphasize the high potential impact of HDACIs in controlling TNBC. In addition, encouraging results stem from new compounds designed to obtain isoform selectivity and/or polypharmacological HDAC approach. The present review provides a discussion of the HDACIs pharmacophoric models and of the structural modifications, leading to compounds with a potent activity against TNBC progression.

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