Chemical tools targeting readers of lysine methylation.
Chemical probes
Lysine methylation
Peptidomimetic ligands
Post-translational modifications
Reader domains
Small-molecule antagonists
Journal
Current opinion in chemical biology
ISSN: 1879-0402
Titre abrégé: Curr Opin Chem Biol
Pays: England
ID NLM: 9811312
Informations de publication
Date de publication:
06 2023
06 2023
Historique:
received:
07
09
2022
revised:
01
02
2023
accepted:
20
02
2023
medline:
30
5
2023
pubmed:
23
3
2023
entrez:
22
3
2023
Statut:
ppublish
Résumé
Reader domains that recognize methylated lysine and arginine residues on histones play a role in the recruitment, stabilization, and regulation of chromatin regulatory proteins. Targeting reader proteins with small molecule and peptidomimetic inhibitors has enabled the elucidation of the structure and function of specific domains and uncovered their role in diseases. Recent progress towards chemical probes that target readers of lysine methylation, including the Royal family and plant homeodomains (PHD), is discussed here. We highlight recently developed covalent cyclic peptide inhibitors of a plant homeodomain. Additionally, inhibitors targeting previously untargeted Tudor domains and chromodomains are discussed.
Identifiants
pubmed: 36948085
pii: S1367-5931(23)00024-8
doi: 10.1016/j.cbpa.2023.102286
pmc: PMC10264141
mid: NIHMS1897578
pii:
doi:
Substances chimiques
Chromatin
0
Histones
0
Lysine
K3Z4F929H6
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
102286Subventions
Organisme : NCI NIH HHS
ID : R01 CA250459
Pays : United States
Informations de copyright
Copyright © 2023 The Authors. Published by Elsevier Ltd.. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Danica Fujimori reports financial support was provided by University of California, San Francisco. Danica Fujimori reports a relationship with National Institutes of Health that includes: funding grants.
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