Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 226, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113855
Keywords
Lysine-specific demethylase 5A; Cancer therapy; Histone methylation; Screening methods; Drug resistance
Categories
Funding
- Natural Science Foundation of Zhejiang Province [LZ18C190001]
- National Natural Science Foundation of China [31972821]
- State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products [2010DS700124-ZZ2008]
- Science and Technology Development Fund, Macau SAR [0072/2018/A2, 0007/2020/A1]
- SKL-QRCM(UM)
- University of Macau [MYRG2019-00002-ICMS]
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KDM5A, a demethylase that is aberrantly expressed in many cancers, plays a role in promoting cancer cell proliferation, metastasis, invasiveness, drug resistance, and poor prognosis. Pharmacological inhibition of KDM5A has been shown to significantly attenuate tumor progression and may serve as a potential drug target in cancer therapy.
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. (C) 2021 Elsevier Masson SAS. All rights reserved.
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