4.6 Review

Promising natural lysine specific demethylase 1 inhibitors for cancer treatment: advances and outlooks

期刊

CHINESE JOURNAL OF NATURAL MEDICINES
卷 20, 期 4, 页码 241-257

出版社

CHINESE JOURNAL NATURAL MEDICINES
DOI: 10.1016/S1875-5364(22)60141-9

关键词

Histone lysine demethylase; LSD1 inhibitor; Natural product; Anticancer

资金

  1. National Natural Science Foundation of China [81803695, 82104359]
  2. Natural Science Fund in Jiangsu Province [BK20180568]
  3. China Postdoctoral Science Foundation [2021M691647]
  4. Fundamental Research Funds for the Central Universities [2632021ZD24]
  5. Open Project of State Key Laboratory of Natural Medicines [SKLNMKF202207]

向作者/读者索取更多资源

This review highlights recent advances in natural LSD1 inhibitors, including their discovery and identification process, natural sources, chemical structures, anticancer effects, and structure-activity relationships. Natural products play an important role in drug discovery, particularly in cancer therapy.
Lysine specific demethylase 1 (LSD1), a transcriptional corepressor or coactivator that serves as a demethylase of his tone 3 lysine 4 and 9, has become a potential therapeutic target for cancer therapy. LSD1 mediates many cellular signaling pathways and regulates cancer cell proliferation, invasion, migration, and differentiation. Recent research has focused on the exploration of its pharmacological inhibitors. Natural products are a major source of compounds with abundant scaffold diversity and structural complexity, which have made a major contribution to drug discovery, particularly anticancer agents. In this review, we briefly highlight recent advances in natural LSD1 inhibitors over the past decade. We present a comprehensive review on their discovery and identification process, natural plant sources, chemical structures, anticancer effects, and structure???activity relationships, and finally provide our perspective on the development of novel natural LSD1 inhibitors for cancer therapy.

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