Strategic selection of TPD technologies based on disease pathology: from mechanistic diversity to clinical implementation

Targeted protein degradation (TPD) offersa way to remove disease-associated proteins rather than only inhibit their activity. Its modalities include heterobifunctional degraders, molecular glues, and lysosome-directed strategies, which differ in their mechanisms and accessible substrates. This review examines how disease pathology can guide TPD selection across cancer, neurodegenerative diseases, metabolic syndrome, autoimmune diseases, and infectious diseases. We compare these approaches according to target localization, protein conformation or aggregation state, and the availability of cellular degradation machinery. Representative preclinical studies and clinical programs illustrate both their potential and the limits of current evidence. Clinical translation remains constrained by tissue delivery, pharmacokinetic properties, target and effector selectivity, acquired resistance, and long-term safety. Molecular design and delivery strategies may help address these barriers, but target degradation must be distinguished from demonstrated therapeutic benefit. A pathology-guided framework can therefore support candidate selection and experimental design, while its clinical utility requires validation in specific disease settings.

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Publication Details

Journal
Frontiers in Pharmacology
Published
2026-11-04
DOI
https://doi.org/10.3389/fphar.2026.1999595
Primary Topic
Protein Degradation and Inhibitors
Type
article
Field-Weighted Citation Impact
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article

Strategic selection of TPD technologies based on disease pathology: from mechanistic diversity to clinical implementation

Dongxin Yi, Hong Yuan, Shuai Li, Jingyuan Zhao
Frontiers in Pharmacology
Protein Degradation and Inhibitors
article

Strategic selection of TPD technologies based on disease pathology: from mechanistic diversity to clinical implementation

Dongxin Yi, Hong Yuan, Shuai Li, Jingyuan Zhao
article en

Abstract

Targeted protein degradation (TPD) offersa way to remove disease-associated proteins rather than only inhibit their activity. Its modalities include heterobifunctional degraders, molecular glues, and lysosome-directed strategies, which differ in their mechanisms and accessible substrates. This review examines how disease pathology can guide TPD selection across cancer, neurodegenerative diseases, metabolic syndrome, autoimmune diseases, and infectious diseases. We compare these approaches according to target localization, protein conformation or aggregation state, and the availability of cellular degradation machinery. Representative preclinical studies and clinical programs illustrate both their potential and the limits of current evidence. Clinical translation remains constrained by tissue delivery, pharmacokinetic properties, target and effector selectivity, acquired resistance, and long-term safety. Molecular design and delivery strategies may help address these barriers, but target degradation must be distinguished from demonstrated therapeutic benefit. A pathology-guided framework can therefore support candidate selection and experimental design, while its clinical utility requires validation in specific disease settings.

Frontiers in PharmacologyVol. 17
Dalian University of Technology (CN), First Affiliated Hospital of Dalian Medical University (CN)
Openalex Percentile: Top 24%
Protein Degradation and Inhibitors
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