LSD1 plays a pivotal role in numerous biological functions. The overexpression of LSD1 is reported to be associated with different malignancies. Over the last decade, LSD1 has emerged as an interesting target for the treatment of acute myeloid leukaemia (AML). Numerous researchers have designed, synthesized, and evaluated various LSD1 inhibitors with diverse chemical architectures. Some of these inhibitors have entered clinical trials and are currently at different phases of clinical evaluation. This comprehensive review enlists recent research developments in LSD1 targeting pharmacophores reported over the last few years.
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