平方毫米
化学
癌症研究
髓系白血病
调节器
耐火材料(行星科学)
降级(电信)
细胞凋亡
医学
生物化学
生物
计算机科学
电信
天体生物学
基因
作者
Ryan P. Wurz,Victor J. Cee
标识
DOI:10.1021/acs.jmedchem.8b01945
摘要
MDM2 is a key oncogenic protein that serves as a negative regulator of the tumor suppressor p53. While a number of inhibitors of the MDM2-p53 interaction have progressed to clinical testing as treatments for a variety of hematologic and solid tumor cancers, the results thus far have been mixed, with perhaps the strongest responses observed in relapsed/refractory acute myeloid leukemia (AML). In an effort to improve the efficacy for this class of compounds, researchers have turned to targeted degradation of MDM2. IMiD-based MDM2 PROTAC 8, which potently reduces MDM2 protein levels through targeted degradation, exhibits enhanced efficacy in the RS4;11 xenograft model relative to a nondegrading MDM2-p53 inhibitor MI-1061.
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