Lysine-specific demethylase 7A (KDM7A) : A potential target for disease therapy

Copyright © 2023 Elsevier Inc. All rights reserved..

Histone demethylation is a kind of epigenetic modification mediated by a variety of enzymes and participates in regulating multiple physiological and pathological events. Lysine-specific demethylase 7A is a kind of α-ketoglutarate- and Fe(II)-dependent demethylase belonging to the PHF2/8 subfamily of the JmjC demethylases. KDM7A is mainly localized in the nucleus and contributes to transcriptional activation via removing mono- and di-methyl groups from the lysine residues 9 and 27 of Histone H3. Mounting studies support that KDM7A is not only necessary for normal embryonic, neural, and skeletal development, but also associated with cancer, inflammation, osteoporosis, and other diseases. Herein, the structure of KDM7A is described by comparing the similarities and differences of its amino acid sequences of KDM7A and other Histone demethylases; the functions of KDM7A in homeostasis and dyshomeostasis are summarized via documenting its content and related signaling; the currently known KDM7A-specific inhibitors and their structural relationship are listed based on their structure optimization and pharmacological activities; and the challenges and opportunities in exploring functions and developing targeted agents of KDM7A are also prospected via presenting encountered problems and potential solutions, which will provide an insight in functional exploration and drug discovery for KDM7A-related diseases.

Medienart:

E-Artikel

Erscheinungsjahr:

2023

Erschienen:

2023

Enthalten in:

Zur Gesamtaufnahme - volume:216

Enthalten in:

Biochemical pharmacology - 216(2023) vom: 02. Okt., Seite 115799

Sprache:

Englisch

Beteiligte Personen:

Li, Chang-Yun [VerfasserIn]
Liu, Yan-Jun [VerfasserIn]
Tao, Fan [VerfasserIn]
Chen, Ru-Yi [VerfasserIn]
Shi, Jin-Jin [VerfasserIn]
Lu, Jian-Fei [VerfasserIn]
Yang, Guan-Jun [VerfasserIn]
Chen, Jiong [VerfasserIn]

Links:

Volltext

Themen:

Cancer
Diseases
Histone demethylation
Inhibitor
Journal Article
KDM7A
Review
Targeted therapy

Anmerkungen:

Date Revised 28.09.2023

published: Print-Electronic

Citation Status Publisher

doi:

10.1016/j.bcp.2023.115799

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM361938802