Evidence map›Paper›PMID 35363464›Full record

ReviewACS chemical biology2022

Exploring Methods of Targeting Histone Methyltransferases and Their Applications in Cancer Therapeutics.

Michelle Y Wang, Priscilla Liow, Maria I Tarazona Guzman, Jun Qi

Open access · greenAbstract readReview
In one paragraph

Review in ACS chemical biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
2.4field-weighted citation impact, top 10% 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

18 citing papers in PubMed, 30 citations in OpenAlex.

  1. Epidrugs in cancer: mechanisms, applications, and future direction.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2026
    Review
  2. Review
  3. Review
  4. Review
  5. Article
  6. Review
  7. Article
  8. Review
  9. Review
  10. Review
  11. Review
  12. Review
  13. Promiscuous Enzymes for Residue-Specific Peptide and Protein Late-Stage Functionalization.Chembiochem : a European journal of chemical biology · 2023
    Review
  14. Review
  15. Review
  16. Virtual Special Issue: Epigenetics 2022.ACS pharmacology & translational science · 2022
    Article
  17. Virtual Special Issue: Epigenetics 2022.ACS medicinal chemistry letters · 2022
    Article
  18. Article
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

4 authors at 2 institutions in 1 country.

Michelle Y WangDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.ORCID 0000-0002-7294-0339
Priscilla LiowDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.
Maria I Tarazona GuzmanDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.
Jun QiDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.
Dana-Farber Cancer Institute · USHarvard University · US

Funding

Project 3: Humoral Targets and B Cell Biology in Chronic Graft-vs.-Host DiseaseP01CA142106 · NCI · DANA-FARBER CANCER INST · PI RITZ, JEROME · 2009 to 2019
$17.5M
Targeting to Epigenetic Modications in ALLR01CA176745 · NCI · SLOAN-KETTERING INST CAN RESEARCH · PI ARMSTRONG, SCOTT A, QI, JUN · 2012 to 2022
$4.2M
EZH2 in cancer biology and novel inhibitorsR01CA222218 · NCI · DANA-FARBER CANCER INST · PI QI, JUN · 2018 to 2022
$2.6M
Transcriptional and Epigenetic Adaptation as Novel Therapeutic Vulnerabilities for Mantle Cell LymphomaR01CA233601 · NCI · H. LEE MOFFITT CANCER CTR & RES INST · PI DUCKETT, DEREK RONALD, QI, JUN · 2020 to 2024
$2.5M
NCI NIH HHS P01 CA142106NCI NIH HHS R01 CA176745NCI NIH HHS R01 CA222218NCI NIH HHS R01 CA233601
6 · The paper itself

Abstract

Histone methyltransferases (HMTs) are enzymes that catalyze the methylation of lysine or arginine residues of histone proteins, a key post-translational modification (PTM). Aberrant expression or activity of these enzymes can lead to abnormal histone methylation of cancer-related genes and thus promote tumorigenesis. Histone methyltransferases have been implicated in chemotherapeutic resistance and immune stimulation, making these enzymes potential therapeutic targets of interest, and chemically targeting these proteins provides an avenue for novel drug development in cancer therapy. This Review aims to discuss the evolution of chemical approaches that have emerged in the past five years to design probes targeting these enzymes, including inhibition through noncovalent inhibitors, covalent inhibitors, and targeted protein degradation through proteolysis targeting chimeras (PROTACs). This Review also highlights how these compounds have been used to study the myriad of HMT functions in cancer progression and treatment response. The recent advancement of some of these drugs into human clinical investigation and even to regulatory approval highlights HMTs as a promising class of targets for chemical intervention and novel therapy development.

Indexed as

HistonesNeoplasmsHistone-Lysine N-MethyltransferaseHistone MethyltransferasesHumansMethylationMethyltransferasesHistone-Lysine N-MethyltransferaseHistone MethyltransferasesHistonesMethyltransferases

Identifiers

PMID35363464
PMCPMC9336197
OpenAlexW4221109095

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.