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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
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Polycomb repressive complex 2 inhibitors: emerging epigenetic modulators.

Danishuddin1, Naidu Subbarao1, Mohammad Faheem1

  • 1School of Computational and Integrative Sciences, Jawaharlal Nehru University, New Delhi, India.

Drug Discovery Today
|July 23, 2018
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Summary
This summary is machine-generated.

Polycomb repressive complex 2 (PRC2) inhibitors show promise for cancer treatment by targeting gene silencing. This review details current drug development, focusing on chemical structures, effectiveness, and how they bind, aiding future drug design.

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Area of Science:

  • Epigenetics
  • Molecular Biology
  • Drug Discovery

Background:

  • Polycomb repressive complex 2 (PRC2) is crucial for histone methylation and gene silencing.
  • PRC2 inhibition is a potential cancer therapy strategy.
  • Several PRC2 inhibitors are in clinical trials.

Purpose of the Study:

  • To summarize advances in PRC2 inhibitor drug discovery and development.
  • To analyze chemotypes, activity, selectivity, and binding modes of PRC2 inhibitors.
  • To provide insights for designing next-generation PRC2 inhibitors.

Main Methods:

  • Review of current literature on PRC2 inhibitors.
  • Analysis of inhibitor chemotypes, activity, selectivity, and binding modes.
  • Focus on structure-based drug design principles.

Main Results:

  • Detailed summary of various PRC2 inhibitor classes.
  • Understanding of inhibitor binding modes.
  • Identification of key features for PRC2 inhibition.

Conclusions:

  • PRC2 inhibitors represent a promising therapeutic avenue for cancer.
  • Structure-based drug design can guide the development of novel PRC2 inhibitors.
  • Further research can optimize existing inhibitors and discover new ones.