Advantages of PROTACs in achieving selective degradation of homologous protein families

Proteolysis-targeting chimeras (PROTACs) have emerged as a promising therapeutic modality and now represent an important addition to the toolkit of medicinal chemists. Compared with conventional small-molecule inhibitors, PROTACs exhibit notable advantages, particularly in achieving selectivity within highly homologous proteins. The ability to discriminate among members of such families holds broad implications for future disease treatment. In this review, we primarily summarize the advantages of PROTACs in conferring selectivity toward highly homologous proteins. This focus will provide a feasible strategy for developing PROTACs that selectively target highly homologous proteins and will ultimately support future therapeutic applications.

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Publication Details

Journal
Beilstein Journal of Organic Chemistry
Published
2026-04-27
DOI
https://doi.org/10.3762/bjoc.22.49
Primary Topic
Protein Degradation and Inhibitors
Type
article
Field-Weighted Citation Impact
0.00

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article

Advantages of PROTACs in achieving selective degradation of homologous protein families

Xinfei Mao, Mingfei Wu, Wenhai Huang, Xiaowu Dong et al.
Beilstein Journal of Organic Chemistry
Protein Degradation and Inhibitors
article

Advantages of PROTACs in achieving selective degradation of homologous protein families

Xinfei Mao, Mingfei Wu, Wenhai Huang, Xiaowu Dong, Yinqiao Chen, Jingyi Zhang, Jing Shu, Luxi Yang
article en

Abstract

Proteolysis-targeting chimeras (PROTACs) have emerged as a promising therapeutic modality and now represent an important addition to the toolkit of medicinal chemists. Compared with conventional small-molecule inhibitors, PROTACs exhibit notable advantages, particularly in achieving selectivity within highly homologous proteins. The ability to discriminate among members of such families holds broad implications for future disease treatment. In this review, we primarily summarize the advantages of PROTACs in conferring selectivity toward highly homologous proteins. This focus will provide a feasible strategy for developing PROTACs that selectively target highly homologous proteins and will ultimately support future therapeutic applications.

Beilstein Journal of Organic ChemistryVol. 22
National Natural Science Foundation of China
Reduced inequalities
Openalex Percentile: Top 15%
Protein Degradation and Inhibitors
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