4.7 Review

ETS transcription factors as emerging drug targets in cancer

Journal

MEDICINAL RESEARCH REVIEWS
Volume 40, Issue 1, Pages 413-430

Publisher

WILEY
DOI: 10.1002/med.21575

Keywords

breast cancer; ERG; ETS; Ewing sarcoma; leukemia; prostate cancer; small molecule inhibitor

Funding

  1. Terry Fox Research Institute
  2. Terry Fox New Frontiers Program Project Grant

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The ETS family of proteins consists of 28 transcription factors, many of which have been implicated in development and progression of a variety of cancers. While one family member, ERG, has been rigorously studied in the context of prostate cancer where it plays a critical role, other ETS factors keep emerging as potential hallmark oncodrivers. In recent years, numerous studies have reported initial discoveries of small molecule inhibitors of ETS proteins and opened novel avenues for ETS-directed cancer therapies. This review summarizes the state of the art data on therapeutic targeting of ETS family members and highlights the corresponding drug discovery strategies.

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