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KDM5 family as therapeutic targets in breast cancer: Pathogenesis and therapeutic opportunities and challenges
Li, Chang Yun1,2; Wang, Wanhe3; Leung, Chung Hang4,5,6,7; Yang, Guan Jun1,2; Chen, Jiong1,2
Source PublicationMolecular Cancer
ISSN1476-4598
2024-12-01
Abstract

Breast cancer (BC) is the most frequent malignant cancer diagnosis and is a primary factor for cancer deaths in women. The clinical subtypes of BC include estrogen receptor (ER) positive, progesterone receptor (PR) positive, human epidermal growth factor receptor 2 (HER2) positive, and triple-negative BC (TNBC). Based on the stages and subtypes of BC, various treatment methods are available with variations in the rates of progression-free disease and overall survival of patients. However, the treatment of BC still faces challenges, particularly in terms of drug resistance and recurrence. The study of epigenetics has provided new ideas for treating BC. Targeting aberrant epigenetic factors with inhibitors represents a promising anticancer strategy. The KDM5 family includes four members, KDM5A, KDM5B, KDM5C, and KDMD, all of which are Jumonji C domain-containing histone H3K4me2/3 demethylases. KDM5 proteins have been extensively studied in BC, where they are involved in suppressing or promoting BC depending on their specific upstream and downstream pathways. Several KDM5 inhibitors have shown potent BC inhibitory activity in vitro and in vivo, but challenges still exist in developing KDM5 inhibitors. In this review, we introduce the subtypes of BC and their current therapeutic options, summarize KDM5 family context-specific functions in the pathobiology of BC, and discuss the outlook and pitfalls of KDM5 inhibitors in this disease.

KeywordBreast Cancer Histone Demethylation Kdm5 Kdm5 Inhibitors Therapeutic Target
Language英語English
DOI10.1186/s12943-024-02011-0
URLView the original
Volume23
Issue1
Pages109
WOS IDWOS:001255494500001
WOS SubjectBiochemistry & Molecular Biology ; Oncology
WOS Research AreaBiochemistry & Molecular Biology ; Oncology
Indexed BySCIE
Scopus ID2-s2.0-85193620745
Fulltext Access
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Document TypeReview article
CollectionTHE STATE KEY LABORATORY OF QUALITY RESEARCH IN CHINESE MEDICINE (UNIVERSITY OF MACAU)
Institute of Chinese Medical Sciences
Corresponding AuthorLeung, Chung Hang
Affiliation1.State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, Zhejiang, 315211, China
2.Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, 315211, China
3.Institute of Medical Research, Northwestern Polytechnical University, Xi’an, Shaanxi, 710072, China
4.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao
5.Department of Biomedical Sciences, Faculty of Health Sciences, University of Macau, Macao
6.Macao Centre for Research and Development in Chinese Medicine, University of Macau, Macao
7.MoE Frontiers Science Centre for Precision Oncology, University of Macau, Macao
Corresponding Author AffilicationInstitute of Chinese Medical Sciences;  Faculty of Health Sciences;  University of Macau
Recommended Citation
GB/T 7714
Li, Chang Yun,Wang, Wanhe,Leung, Chung Hang,et al. KDM5 family as therapeutic targets in breast cancer: Pathogenesis and therapeutic opportunities and challenges[J]. Molecular Cancer, 2024, 23(1), 109.
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