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DOI 10.1016/j.bmc.2024.117967

Медицинская библиотека · Bioorganic & medicinal chemistry · 2024

The application of PROTACs in immune-inflammation diseases.

Zhang Chao, Sun Xiuyun, Song Peilu, Rao Yu

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Аннотация

Immune-inflammatory diseases are a class of conditions with high prevalence that severely impact the quality of life. Current treatment strategies include immunosuppressants, glucocorticoids, and monoclonal antibodies. However, these approaches have certain limitations, such as poor membrane permeability, immunogenicity, and the requirement for injection in large molecule drugs. Small molecule compounds, on the other hand, suffer from issues like poor selectivity, inability to inhibit non-enzymatic functions, and biological compensation. These factors constrain the effectiveness of current therapeutic strategies in immune-inflammatory diseases. As a novel small molecule drug development technology, proteolysis-targeting chimeras (PROTACs) regulate protein levels by inducing interactions between target proteins and E3 ubiquitin ligases, leading to the selective degradation of target proteins. This technology has already shown promising therapeutic effects in the treatment of immune-inflammatory diseases. This review aims to comprehensively summarize the application of PROTAC technology in the field of immune inflammation and provide insights into its potential in treating immune-inflammatory diseases.

Для цитирования: Zhang Chao, Sun Xiuyun, Song Peilu, Rao Yu. The application of PROTACs in immune-inflammation diseases.. Bioorganic & medicinal chemistry. 2024. DOI: 10.1016/j.bmc.2024.117967.

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