Evidence map›Paper›PMID 31511663›Full record

ReviewNature reviews. Cancer2019

Targeting transcription factors in cancer - from undruggable to reality.

John H Bushweller

Open access · greenAbstract readReview
In one paragraph

Review in Nature reviews. Cancer, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 581 papers.

0numbers the graph read from it
0cells of the map it votes in
581citing papers in PubMed
32.4field-weighted citation impact, top 1% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

581 citing papers in PubMed, 917 citations in OpenAlex.

  1. Article
  2. Targeting Microglial Transcriptional Reprogramming as a Therapy Strategy for Alzheimer's Disease.BioEssays : news and reviews in molecular, cellular and developmental biology · 2026
    Review
  3. Review
  4. Review
  5. Article
  6. Article
  7. Article
  8. Article
  9. Exercise inhibits proliferation and induces apoptosis of lung adenocarcinoma cells via the POU2F2-SPOCD1-PI3K/AKT signaling axis.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2026
    Article
  10. Article
  11. Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. A ligandable PNT domain establishes ERG as a directly targetable oncogenic driver in prostate cancer.Proceedings of the National Academy of Sciences of the United States of America · 2026
    Article
  17. Review
  18. Article
  19. Article
  20. Article

521 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

1 author at 1 institution in 1 country.

John H BushwellerDepartment of Molecular Physiology and Biological Physics, University of Virginia, Charlottesville, VA, USA. jhb4v@virginia.edu.ORCID http://orcid.org/0000-0002-5386-1758
University of Virginia · US

Funding

Targeted Small Molecule Inhibitors for Inv(16) LeukemiaR01CA234478 · NCI · UNIVERSITY OF VIRGINIA · PI BUSHWELLER, JOHN HACKETT, CASTILLA, LUCIO H. · 2019 to 2023
$3.4M
Development of Inhibitors of the Leukemia Fusion Protein CBFbeta-SMMHCR01CA140398 · NCI · UNIVERSITY OF VIRGINIA · PI BUSHWELLER, JOHN HACKETT, CASTILLA, LUCIO H. · 2010 to 2013
$2.6M
NCI NIH HHS R01 CA140398NCI NIH HHS R01 CA234478
6 · The paper itself

Abstract

Mutated or dysregulated transcription factors represent a unique class of drug targets that mediate aberrant gene expression, including blockade of differentiation and cell death gene expression programmes, hallmark properties of cancers. Transcription factor activity is altered in numerous cancer types via various direct mechanisms including chromosomal translocations, gene amplification or deletion, point mutations and alteration of expression, as well as indirectly through non-coding DNA mutations that affect transcription factor binding. Multiple approaches to target transcription factor activity have been demonstrated, preclinically and, in some cases, clinically, including inhibition of transcription factor-cofactor protein-protein interactions, inhibition of transcription factor-DNA binding and modulation of levels of transcription factor activity by altering levels of ubiquitylation and subsequent proteasome degradation or by inhibition of regulators of transcription factor expression. In addition, several new approaches to targeting transcription factors have recently emerged including modulation of auto-inhibition, proteolysis targeting chimaeras (PROTACs), use of cysteine reactive inhibitors, targeting intrinsically disordered regions of transcription factors and combinations of transcription factor inhibitors with kinase inhibitors to block the development of resistance. These innovations in drug development hold great promise to yield agents with unique properties that are likely to impact future cancer treatment.

Indexed as

Gene Expression Regulation, NeoplasticAnimalsAntineoplastic AgentsCatalytic DomainCell Line, TumorCell ProliferationDNADrug DesignHumansLigandsMutationNeoplasmsPhosphorylationProteasome Endopeptidase ComplexProtein BindingProtein Interaction MappingAntineoplastic AgentsDNALigandsProteasome Endopeptidase ComplexTranscription Factors

Identifiers

PMID31511663
PMCPMC8820243
OpenAlexW2973216672

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.