Protein Lysine Methyltransferases Inhibitors.

Humans Histone-Lysine N-Methyltransferase / chemistry Lysine / chemistry Epigenesis, Genetic Histones / metabolism Neoplasms / drug therapy Methyltransferases / metabolism Protein Processing, Post-Translational
Epigenetics cancer inhibitors methylation methyltransferases protein lysine small molecular

Journal

Current medicinal chemistry
ISSN: 1875-533X
Titre abrégé: Curr Med Chem
Pays: United Arab Emirates
ID NLM: 9440157

Informations de publication

Date de publication:
2023
Historique:
received: 11 03 2022
revised: 31 05 2022
accepted: 20 06 2022
medline: 1 6 2023
pubmed: 1 9 2022
entrez: 31 8 2022
Statut: ppublish

Résumé

Protein lysine methylation is a significant protein post-translational modification (PTMs) and has a key function in epigenetic regulation. Protein lysine methyltransferase (PKMTs) mainly catalyzes the lysine methylation of various core histones and a few non-histone proteins. It has been observed that aberrant activity of PKMTs has been found in many cancers and other diseases, and some PKMT inhibitors have been discovered and progressed to clinical trials. This field developed rapidly and has aroused great interest. In this paper, we reviewed the biochemical and biological activities of PKMTs and their association with various cancers. Selective small-molecule inhibitors, including their chemical structure, structure-activity relationship, and in vitro/vivo studies, are also described to provide ideas for the discovery of highly potent, selective PKMT inhibitors.

Identifiants

DOI: 10.2174/0929867329666220829151257 PMID: 36043747
pubmed: 36043747
pii: CMC-EPUB-125988
doi: 10.2174/0929867329666220829151257
doi:

Substances chimiques

Histone-Lysine N-Methyltransferase EC 2.1.1.43
Lysine K3Z4F929H6
Histones 0
Methyltransferases EC 2.1.1.-

Types de publication

Review Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

3060-3089

Informations de copyright

Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Auteurs

Ying Li (Y)

College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, P.R. China.

Lei Ding (L)

College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, P.R. China.

Shuang Ren (S)

College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, P.R. China.

Wen Zhang (W)

College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, P.R. China.

Guo-Wu Rao (GW)

College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, P.R. China.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › One-carbon group transferases › Methyltransferases › Protein Methyltransferases › Histone méthyltransférases › Histone-lysine N-methyltransferase › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › Acides aminés essentiels › Lysine › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Phénomènes génétiques › Régulation de l'expression des gènes › Épigenèse génétique › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Nucléoprotéines › Histone › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Tumeurs › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › One-carbon group transferases › Methyltransferases › Protein Lysine Methyltransferases Inhibitors.
questionsmedicales.fr › Phénomènes génétiques › Régulation de l'expression des gènes › Modification traductionnelle des protéines › Maturation post-traductionnelle des protéines › Protein Lysine Methyltransferases Inhibitors.