Fu Xiaoli, Zhang Peng, Yu Bin
College of Public Heath, Zhengzhou University, Zhengzhou 450001, China.
Department of Neurosurgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China.
Future Med Chem. 2017 Jul;9(11):1227-1242. doi: 10.4155/fmc-2017-0068. Epub 2017 Jul 19.
LSD1 has become an important biologically validated epigenetic target for cancer therapy since its identification in 2004. LSD1 mediates many cellular signaling pathways and is involved in the initiation and development of cancers. Aberrant overexpression of LSD1 has been observed in different types of cancers, and inactivation by small molecules suppresses cancer cell differentiation, proliferation, invasion and migration. To date, a large number of LSD1 inhibitors have been reported, RG6016, GSK-2879552, INCB059872, IMG-7289 and CC-90011 are currently undergoing clinical assessment for the treatment of acute myeloid leukemia, small-cell lung cancer, etc. In this review, we briefly highlight recent advances of LSD1 inhibitors mainly covering the literatures from 2015 to 2017 and tentatively propose our perspectives on the design of new LSD1 inhibitors for cancer therapy.
自2004年被发现以来，赖氨酸特异性去甲基化酶1（LSD1）已成为癌症治疗中一个重要的经生物学验证的表观遗传靶点。LSD1介导许多细胞信号通路，并参与癌症的发生和发展。在不同类型的癌症中均观察到LSD1的异常过表达，小分子使其失活可抑制癌细胞的分化、增殖、侵袭和迁移。迄今为止，已报道了大量的LSD1抑制剂，RG6016、GSK - 2879552、INCB059872、IMG - 7289和CC - 90011目前正在接受治疗急性髓系白血病、小细胞肺癌等的临床评估。在本综述中，我们简要突出LSD1抑制剂的最新进展，主要涵盖2015年至2017年的文献，并初步提出我们对设计用于癌症治疗的新型LSD1抑制剂的观点。
