Article
Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor.
European journal of medicinal chemistry - 15 Dec 2022
Liu Haixia, Mi Qianglong, Ding Xinyu, Lin Chencen, Liu Linyi, Ren Chaowei, Shen ShuTing, Shao YuBao, Chen Jinju, Zhou Yongqi, Ji Liting, Zhang Heqiao, Bai Fang, Yang Xiaobao, Yin Qianqian, Jiang Biao
Abstract excerpt
The oncogenic fusion protein BCR-ABL is the driving force of leukemogenesis in chronic myeloid leukemia (CML). Despite the great advance in CML treatment through the application of tyrosine kinase inhibitors (TKIs) against BCR-ABL, disease recurrence after TKI discontinuation and clinical resistance mainly due to BCR-ABL mutations continue to be an issue. Herein we report our efforts to synthesize a novel series...
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