The development of small-molecule inhibitors targeting CD47

•The small-molecule inhibitors targeting CD47/SIRPα axis, a promising phagocytosis checkpoint in cancer therapy, are reviewed for the first time.•In addition to targeting the interaction of CD47/SIRPα, compounds regulating CD47 at transcriptional, translational and posttranslational levels are summa...

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Veröffentlicht in:Drug discovery today 2021-02, Vol.26 (2), p.561-568
Hauptverfasser: Yu, Wei-Bang, Ye, Zi-Han, Chen, Xiuping, Shi, Jia-Jie, Lu, Jin-Jian
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Sprache:eng
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Zusammenfassung:•The small-molecule inhibitors targeting CD47/SIRPα axis, a promising phagocytosis checkpoint in cancer therapy, are reviewed for the first time.•In addition to targeting the interaction of CD47/SIRPα, compounds regulating CD47 at transcriptional, translational and posttranslational levels are summarized.•Challenges followed by the corresponding strategies are proposed for further development of small-molecule inhibitors targeting CD47/SIRPα axis. Immunotherapy has become an indispensable part of cancer treatment. A pivotal phagocytosis checkpoint, named cluster of differentiation 47 (CD47), which functions as ‘don’t eat me’ signal to protect cells from phagocytosis upon interaction with signal regulatory protein alpha (SIRPα) on macrophages, has recently attracted much attention. Numerous antibodies targeting the CD47/SIRPα axis have shown encouraging efficacy in clinical trials. Meanwhile, studies on small-molecule inhibitors that interfere with CD47/SIRPα interaction or regulate CD47 expression are also in full swing. In this review, we summarize the small-molecule inhibitors interrupting the binding of CD47/SIRPα and regulating CD47 at the transcriptional, translational, and post-translational modification (PTM) levels. We provide perspectives and strategies for targeting the CD47/SIRPα phagocytosis checkpoint.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2020.11.003