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Lysine-Specific Demethylase 1 Promises to Be a Novel Target in Cancer Drug Resistance: Therapeutic Implications

Feifei Yang, Xue-Li Xu, Ting Hu, Jian‐Quan Liu, Jin-Zhu Zhou, Liying Ma, Hong‐Min Liu

2023Journal of Medicinal Chemistry21 citationsDOIOpen Access PDF

Abstract

Chemotherapy, targeted therapy, and immunotherapy are effective against most tumors, but drug resistance remains a barrier to successful treatment. Lysine-specific demethylase 1 (LSD1), a member of histone demethylation modifications, can regulate invasion, metastasis, apoptosis, and immune escape of tumor cells, which are associated with tumorigenesis and tumor progression. Recent studies suggest that LSD1 ablation regulates resensitivity of tumor cells to anticarcinogens containing immune checkpoint inhibitors (ICIs) via multiple upstream and downstream pathways. In this review, we describe the recent findings about LSD1 biology and its role in the development and progression of cancer drug resistance. Further, we summarize LSD1 inhibitors that have a reversal or resensitive effect on drug resistance and discuss the possibility of targeting LSD1 in combination with other agents to surmount resistance.

Topics & Concepts

DemethylaseCancer researchDrug resistanceChemistryCancerImmunotherapyCarcinogenesisMetastasisCancer cellDrugImmune systemEpigeneticsPharmacologyBiologyImmunologyBiochemistryGeneMicrobiologyGeneticsEpigenetics and DNA MethylationHistone Deacetylase Inhibitors ResearchCancer Immunotherapy and Biomarkers
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