蛋白水解靶向嵌合体（PROTACs）在药物发现中的进展和展望。
Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery.
机构信息
Department of Pharmaceutical Chemistry and Analysis, Fourth Military Medical University, Xi'an, Shaanxi 710032, China.
Department of Pharmaceutical Chemistry and Analysis, Fourth Military Medical University, Xi'an, Shaanxi 710032, China.
出版信息
Bioorg Chem. 2022 Aug;125:105848. doi: 10.1016/j.bioorg.2022.105848. Epub 2022 May 5.
Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin-proteasome system (UPS) to induce different POIs degradation. Currently, the first oral PROTACs (ARV-110 and ARV-471) have shown encouraging efficacy in clinical trials of prostate and breast cancer treatment, which turns a new avenue for the development of PROTAC research. In this review, we focus on a detailed summary of the latest progress of PROTACs and elucidate the advantages of PROTACs technology. In addition, potential challenges and perspectives of PRTOACs are discussed.
蛋白水解靶向嵌合体（PROTACs）是一种由靶蛋白（POI）配体、E3 连接酶配体和连接子组成的双功能分子，已被开发用于劫持泛素-蛋白酶体系统（UPS）以诱导不同 POI 的降解。目前，首个口服 PROTACs（ARV-110 和 ARV-471）在前列腺癌和乳腺癌治疗的临床试验中显示出令人鼓舞的疗效，为 PROTAC 研究的发展开辟了新途径。在这篇综述中，我们重点详细总结 PROTACs 的最新进展，并阐明 PROTACs 技术的优势。此外，还讨论了 PRTOACs 的潜在挑战和前景。
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