Cited by 288Epigenetics and DNA MethylationChromatin Remodeling and CancerHistone Deacetylase Inhibitors Research

Marked for death: Targeting epigenetic changes in cancer

Pfister, Sophia Xiao, Ashworth, Alan·2017·Nature Reviews Drug Discovery

Abstract

In the past few years, it has become clear that mutations in epigenetic regulatory genes are common in human cancers. Therapeutic strategies are now being developed to target cancers with mutations in these genes using specific chemical inhibitors. In addition, a complementary approach based on the concept of synthetic lethality, which allows exploitation of loss-of-function mutations in cancers that are not targetable by conventional methods, has gained traction. Both of these approaches are now being tested in several clinical trials. In this Review, we present recent advances in epigenetic drug discovery and development, and suggest possible future avenues of investigation to drive progress in this area.

Integrity signals

Registry

Crossref · 10.1038/nrd.2016.256

Cites

322 of 322 references verified0 citation errors · 0 not checkable

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  • Epigenetic reprogramming may be of central importance when drug-resistant states are functionally heterogeneous, evolving, and transient.

    “Epigenetic reprogramming may be of central importance when drug-resistant states are functionally heterogeneous, evolving, and transient [69], in contrast to more stable drug resistance resulting from genetic alterations.”

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Authors
Pfister, S. X., & Ashworth, A.
Affiliations
University of California, San Francisco (US)
Corresponding author
Ashworth, Alan
Venue
Nature Reviews Drug Discovery
Published
2017-03-10
Volume
16
Issue
4
Pages
241-263
ISSN
  • 1474-1776 (ISSN-L)
  • 1474-1784
OpenAlex
W2593741942
Cited by
288
References
323
Citations by year
2026: 5 · 2025: 11 · 2024: 23 · 2023: 37 · 2022: 26 · 2021: 48 · 2020: 38 · 2019: 43 · 2018: 36 · 2017: 21
FWCI
3.61
Type
journal article
Language
en
Open access
closed
Locations
  • Nature Reviews Drug Discovery (publishedVersion)
  • PubMed (publishedVersion)
Funders
Breast Cancer Research Foundation
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
Keywords
epigenetic regulation, cancer epigenetics, epigenetic inhibitors, gain-of-function mutations, loss-of-function mutations, synthetic lethality, epigenetic drug discovery, epigenetic drug development, clinical trials
MeSH terms
Enzyme Inhibitors, Humans, Models, Genetic, Mutation, Neoplasms, Epigenesis, Genetic, Drug Discovery, Molecular Targeted Therapy

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