Controlled bioorthogonal activation of Bromodomain-containing protein 4 degrader by co-delivery of PROTAC and Pd-catalyst for tumor-specific therapy

Li, Zhiyao; Jiang, Taibai; Yuan, Xu; Li, Bowen; Wu, Chongzhi; Li, Yecheng; Huang, Yong; Xie, Xin; Pan, Weidong; Ping, Yuan

doi:10.1016/j.jconrel.2024.08.032

Journal of Controlled Release

2024

DOI: 10.1016/j.jconrel.2024.08.032

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Controlled bioorthogonal activation of Bromodomain-containing protein 4 degrader by co-delivery of PROTAC and Pd-catalyst for tumor-specific therapy

Zhiyao Li,

Taibai Jiang,

Xu Yuan

et al.

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Precision-engineered PROTACs minimize off-tissue effects in cancer therapy

Shi,

Wang,

Zeng

et al. 2024

Front. Mol. Biosci.

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Proteolysis-targeting chimeras (PROTACs) offer a groundbreaking approach to selectively degrade disease-related proteins by utilizing the ubiquitin-proteasome system. While this strategy shows great potential in preclinical and clinical settings, off-tissue effects remain a major challenge, leading to toxicity in healthy tissues. This review explores recent advancements aimed at improving PROTAC specificity, including tumor-specific ligand-directed PROTACs, pro-PROTACs activated in tumor environments, and E3 ligase overexpression strategies. Innovations such as PEGylation and nanotechnology also play a role in optimizing PROTAC efficacy. These developments hold promise for safer, more effective cancer therapies, though challenges remain for clinical translation.

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Precision-engineered PROTACs minimize off-tissue effects in cancer therapy

Shi,

Wang,

Zeng

et al. 2024

Front. Mol. Biosci.

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show abstract

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Controlled bioorthogonal activation of Bromodomain-containing protein 4 degrader by co-delivery of PROTAC and Pd-catalyst for tumor-specific therapy

Cited by 1 publication

References 39 publications

Precision-engineered PROTACs minimize off-tissue effects in cancer therapy

Precision-engineered PROTACs minimize off-tissue effects in cancer therapy

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