E3 ligase Ligand-Linker Conjugates 51 包含用于 E3 泛素连接酶的 VHL 配体和 linker。E3 ligase Ligand-Linker Conjugates 51 可通过 PROTAC 技术合成 BCR-ABL1 降解剂 GMB-475。GMB-475 作用于 Ba/F3 细胞，诱导 BCR-ABL1 降解， IC50 为 1.11 μM。
E3 ligase Ligand-Linker Conjugates 51 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 51 can be used to design BCR-ABL1 PROTAC degrader GMB-475. GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells[1]. VHL
[1]. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. Cancer Res. 2019 Jul 16. pii: canres.1236.2019.
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