Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity,

Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity,

Simultaneous targeting of BCL-xL and BCL-2 is an attractive approach for cancer treatment. Based on information gained by computational structure modelling, the authors develop a PROTAC that induces degradation of both BCL-xL and BCL-2 and effectively targets BCL-xL/2-dependent leukaemia cells.

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Auteurs principaux: Dongwen Lv, Pratik Pal, Xingui Liu, Yannan Jia, Dinesh Thummuri, Peiyi Zhang, Wanyi Hu, Jing Pei, Qi Zhang, Shuo Zhou, Sajid Khan, Xuan Zhang, Nan Hua, Qingping Yang, Sebastian Arango, Weizhou Zhang, Digant Nayak, Shaun K. Olsen, Susan T. Weintraub, Robert Hromas, Marina Konopleva, Yaxia Yuan, Guangrong Zheng, Daohong Zhou
Format: article
Langue:EN
Publié: Nature Portfolio 2021
Sujets:
Science
Q
Accès en ligne:https://doaj.org/article/38d97353bbbf41e4aa6eb4a5907c3bd4
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Résumé:Simultaneous targeting of BCL-xL and BCL-2 is an attractive approach for cancer treatment. Based on information gained by computational structure modelling, the authors develop a PROTAC that induces degradation of both BCL-xL and BCL-2 and effectively targets BCL-xL/2-dependent leukaemia cells.

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