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Issue 98, 2019
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Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL

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Abstract

BCL-XL, an anti-apoptotic BCL-2 family protein, plays a key role in cancer cell survival. However, the potential of BCL-XL as an anti-cancer target has been hampered by the on-target platelet toxicity because platelets depend on BCL-XL to maintain their viability. Here we report the development of a PROTAC BCL-XL degrader, XZ424, which has increased selectivity for BCL-XL-dependent MOLT-4 cells over human platelets compared with conventional BCL-XL inhibitors. This proof-of-concept study demonstrates the potential of utilizing a PROTAC approach to achieve tissue selectivity.

Graphical abstract: Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL

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Publication details

The article was received on 14 Sep 2019, accepted on 12 Nov 2019 and first published on 19 Nov 2019


Article type: Communication
DOI: 10.1039/C9CC07217A
Chem. Commun., 2019,55, 14765-14768

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    Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL

    X. Zhang, D. Thummuri, Y. He, X. Liu, P. Zhang, D. Zhou and G. Zheng, Chem. Commun., 2019, 55, 14765
    DOI: 10.1039/C9CC07217A

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