Small molecule targeting of chromatin writers in cancer

© 2021. Springer Nature America, Inc..

More than a decade after the launch of DNA methyltransferase and histone deacetylase inhibitors for the treatment of cancer, 2020 heralded the approval of the first histone methyltransferase inhibitor, revitalizing the concept that targeted manipulation of the chromatin regulatory landscape can have profound therapeutic impact. Three chromatin regulatory pathways-DNA methylation, histone acetylation and methylation-are frequently implicated in human cancer but hundreds of potentially druggable mechanisms complicate identification of key targets for therapeutic intervention. In addition to human genetics and functional screening, chemical biology approaches have proven critical for the discovery of key nodes in these pathways and in an ever-increasing complexity of molecularly defined human cancer contexts. This review introduces small molecule targeting approaches, showcases chemical probes and drug candidates for epigenetic writer enzymes, illustrates molecular features that may represent epigenetic dependencies and suggests translational strategies to maximize their impact in cancer therapy.

Medienart:

E-Artikel

Erscheinungsjahr:

2022

Erschienen:

2022

Enthalten in:

Zur Gesamtaufnahme - volume:18

Enthalten in:

Nature chemical biology - 18(2022), 2 vom: 24. Feb., Seite 124-133

Sprache:

Englisch

Beteiligte Personen:

Conery, Andrew R [VerfasserIn]
Rocnik, Jennifer L [VerfasserIn]
Trojer, Patrick [VerfasserIn]

Links:

Volltext

Themen:

Antineoplastic Agents
Chromatin
Journal Article
Review

Anmerkungen:

Date Completed 17.02.2022

Date Revised 30.10.2022

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1038/s41589-021-00920-5

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM334888336