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Pharmacological inhibition of KDM5A for cancer treatment
Yang, Guan Jun1,2,6; Wu, Jia3,5; Miao, Liang1,2,6; Zhu, Ming Hui1,2,6; Zhou, Qian Jin1,2,6; Lu, Xin Jiang1,2,6; Lu, Jian Fei1,2,6; Leung, Chung Hang3,5; Ma, Dik Lung4; Chen, Jiong1,2,6
Source PublicationEuropean Journal of Medicinal Chemistry

Lysine-specific demethylase 5A (KDM5A, also named RBP2 or JARID1A) is a demethylase that can remove methyl groups from histones H3K4me1/2/3. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, drug resistance, and is associated with poor prognosis. Pharmacological inhibition of KDM5A has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of KDM5A, its role in carcinogenesis, a comparison of currently available approaches for screening KDM5A inhibitors, a classification of KDM5A inhibitors, and its potential as a drug target in cancer therapy.

KeywordCancer Therapy Drug Resistance Histone Methylation Lysine-specific Demethylase 5a Screening Methods
URLView the original
Indexed BySCIE
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000703119000036
Scopus ID2-s2.0-85115293669
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Cited Times [WOS]:10   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorLeung, Chung Hang; Ma, Dik Lung; Chen, Jiong
Affiliation1.State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, 315211, China
2.Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, 315211, China
3.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, 999078, China
4.Department of Chemistry, Hong Kong Baptist University, Kowloon, Hong Kong, 999077, China
5.Department of Biomedical Sciences, Faculty of Health Sciences, University of Macau, 999078, China
6.Key Laboratory of Applied Marine Biotechnology of Ministry of Education, Ningbo University, Ningbo, 315211, China
Corresponding Author AffilicationInstitute of Chinese Medical Sciences;  Faculty of Health Sciences
Recommended Citation
GB/T 7714
Yang, Guan Jun,Wu, Jia,Miao, Liang,et al. Pharmacological inhibition of KDM5A for cancer treatment[J]. European Journal of Medicinal Chemistry,2021,226.
APA Yang, Guan Jun,Wu, Jia,Miao, Liang,Zhu, Ming Hui,Zhou, Qian Jin,Lu, Xin Jiang,Lu, Jian Fei,Leung, Chung Hang,Ma, Dik Lung,&Chen, Jiong.(2021).Pharmacological inhibition of KDM5A for cancer treatment.European Journal of Medicinal Chemistry,226.
MLA Yang, Guan Jun,et al."Pharmacological inhibition of KDM5A for cancer treatment".European Journal of Medicinal Chemistry 226(2021).
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