喜树碱
拓扑异构酶
拓扑异构酶抑制剂
药品
化学
抗体-药物偶联物
抗癌药
癌细胞
癌症
药理学
计算生物学
DNA
单克隆抗体
生物
生物化学
抗体
免疫学
遗传学
作者
Seungmin Han,Kyutae Lim,Brody J. Blackburn,Jina Yun,Charles W. Putnam,David A. Bull,Young‐Wook Won
出处
期刊:Pharmaceutics
[MDPI AG]
日期:2022-08-16
卷期号:14 (8): 1707-1707
被引量:4
标识
DOI:10.3390/pharmaceutics14081707
摘要
DNA topoisomerases are essential enzymes that stabilize DNA supercoiling and resolve entanglements. Topoisomerase inhibitors have been widely used as anti-cancer drugs for the past 20 years. Due to their selectivity as topoisomerase I (TOP1) inhibitors that trap TOP1 cleavage complexes, camptothecin and its derivatives are promising anti-cancer drugs. To increase accumulation of TOP1 inhibitors in cancer cells through the targeting of tumors, TOP1 inhibitor antibody-drug conjugates (TOP1-ADC) have been developed and marketed. Some TOP1-ADCs have shown enhanced therapeutic efficacy compared to prototypical anti-cancer ADCs, such as T-DM1. Here, we review various types of camptothecin-based TOP1 inhibitors and recent developments in TOP1-ADCs. We then propose key points for the design and construction of TOP1-ADCs. Finally, we discuss promising combinatorial strategies, including newly developed approaches to maximizing the therapeutic potential of TOP1-ADCs.
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