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Pharmacological Modulation of Transcriptional Coregulators in Cancer

Timothy R Bishop1, Yuxiang Zhang1, Michael A Erb1

  • 1Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

Trends in Pharmacological Sciences
|May 13, 2019
PubMed

Insights

Transcriptional coregulators regulate gene expression and are key in cancer development. Recent advances in cancer pharmacology are making these proteins viable targets for new small-molecule cancer drugs.

Area of Science:

  • Molecular Biology
  • Cancer Biology
  • Pharmacology

Background:

  • Transcriptional coregulators are essential for gene regulation by transcription factors.
  • These proteins play critical roles in oncogenesis through aberrant control of gene transcription.
  • Coregulators are a rapidly expanding target class in small-molecule drug discovery for cancer.

Purpose of the Study:

  • To review challenges and recent trends in targeting transcriptional coregulators in cancer therapy.
  • To highlight the potential of coregulators as tractable targets for novel cancer drug development.

Main Methods:

  • Review of recent trends in cancer pharmacology.
  • Discussion of challenges in targeting transcriptional coregulators.
  • Analysis of the role of coregulators in cancer-specific genetic dependencies and disease pathology.

Main Results:

  • Identifying cancer-specific genetic dependencies for coregulator targeting remains a challenge.
  • Matching pharmacologically relevant protein folds to disease pathology is crucial.
  • Achieving selectivity is necessary to exploit genetic dependencies.

Conclusions:

  • Recent trends in cancer pharmacology are addressing challenges in targeting transcriptional coregulators.
  • Coregulators are increasingly recognized as tractable targets for developing new cancer therapies.
  • Small-molecule drug discovery targeting coregulators shows promise for future cancer treatments.
Keywords:
cancerchromatintherapeuticstranscription

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