As the first discovered histone demethylase, LSD1 plays an important
role in maintaining the function of normal and tumor cells. In previous
studies, it has been found that LSD1 is highly expressed in a variety of
tumor cells, such as acute myeloid leukemia, non-small cell lung cancer,
prostate cancer, breast cancer, and gastric cancer, etc. Therefore,
targeting LSD1 is a promising strategy for the treatment of tumors. Cell
stemness refers to the characteristics of self-replication, rapid
proliferation, and multidirectional differentiation potential. Moreover,
cancer stem cells could regulate self-renewal, cell proliferation,
migration and malignant phenotype. Therefore, lowering the tumor cells
stemness could inhibit their growth effectively and inhibition of stem
cell characteristics has a bright prospect in the field of tumor
therapy. Up to now, there exist many studies revealing the significant
role of LSD1 in regulating the stemness characteristics such as
embryonic stem cells differentiation and inhibition of LSD1 decreased
the property of cancer cell stemness. However, there lacks a detailed
review about the relationship of LSD1 and cancer cell stemness. Herein,
in this review, we summarized the mechanisms of LSD1 in regulating cell
stemness comprehensively, in addition, related inhibitors targeting LSD1
to inhibit the proliferation characteristics of cancer stem cells are
also described.