Protein-Based Degraders: From Chemical Biology Tools to Neo-Therapeutics.

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Tác giả: Laura M K Dassama, Jeandele Elliot, Lisha Ou, Mekedlawit T Setegne, Fangfang Shen

Ngôn ngữ: eng

Ký hiệu phân loại: 734 *Sculpture from ca. 500 to 1399

Thông tin xuất bản: United States : Chemical reviews , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 678855

The nascent field of targeted protein degradation (TPD) could revolutionize biomedicine due to the ability of degrader molecules to selectively modulate disease-relevant proteins. A key limitation to the broad application of TPD is its dependence on small-molecule ligands to target proteins of interest. This leaves unstructured proteins or those lacking defined cavities for small-molecule binding out of the scope of many TPD technologies. The use of proteins, peptides, and nucleic acids (otherwise known as "biologics") as the protein-targeting moieties in degraders addresses this limitation. In the following sections, we provide a comprehensive and critical review of studies that have used proteins and peptides to mediate the degradation and hence the functional control of otherwise challenging disease-relevant protein targets. We describe existing platforms for protein/peptide-based ligand identification and the drug delivery systems that might be exploited for the delivery of biologic-based degraders. Throughout the Review, we underscore the successes, challenges, and opportunities of using protein-based degraders as chemical biology tools to spur discoveries, elucidate mechanisms, and act as a new therapeutic modality.
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