A selective BCL-X(L) PROTAC degrader achieves safe and potent antitumor activity

BCL-X(L) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-X(L) inhibitors such as ABT263 as safe and effective anticancer agents. To reduce the toxicity of ABT263, we converted it into DT2216, a BCL-X(L) proteolysis targeting chimera...

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Udgivet i:Nat Med
Main Authors: Khan, Sajid, Zhang, Xuan, Lv, Dongwen, Zhang, Qi, He, Yonghan, Zhang, Peiyi, Liu, Xingui, Thummuri, Dinesh, Yuan, Yaxia, Wiegand, Janet S., Pei, Jing, Zhang, Weizhou, Sharma, Abhisheak, McCurdy, Christopher R., Kuruvilla, Vinitha M., Baran, Natalia, Ferrando, Adolfo A., Kim, Yong-mi, Rogojina, Anna, Houghton, Peter J., Huang, Guangcun, Hromas, Robert, Konopleva, Marina, Zheng, Guangrong, Zhou, Daohong
Format: Artigo
Sprog:Inglês
Udgivet: 2019
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6898785/
https://ncbi.nlm.nih.gov/pubmed/31792461
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41591-019-0668-z
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