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Updated: Aug 6, 2026
05:33
High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
Leveraging peptides for targeted protein degradation
Yuyang Li1, Xiaowei Wang2, Xinyu Wang1
1Department of Clinical Pathobiology and Immunological Testing, School of Medical Laboratory, Qilu Medical University, Zibo 255300, China.
The Journal of Pharmacy and Pharmacology
|July 23, 2026
Summary
Peptide-based targeted protein degradation (TPD) offers a promising solution to drug discovery challenges. By engineering selective peptides and advanced delivery systems, TPD enhances therapeutic precision and efficacy for previously undruggable targets.
Area of Science:
- Drug Discovery and Development
- Molecular Biology
- Biotechnology
Background:
- Targeted protein degradation (TPD) and proteolysis-targeting chimeras (PROTACs) represent significant advancements in drug discovery.
- Clinical translation of TPD is hindered by challenges such as identifying ligands for undruggable proteins, poor solubility/permeability, biodistribution issues, and off-target toxicity.
- Peptides offer potential as ligands for TPD due to their broad molecular recognition capabilities.
Purpose of the Study:
- To review recent advancements in peptide-based PROTAC development.
- To highlight innovative delivery strategies and methods for enhancing TPD efficiency.
- To provide insights into future prospects for optimizing therapeutic precision and efficacy in peptide-mediated TPD.
Main Methods:
- Comprehensive literature search conducted across multiple online scientific databases including Google Scholar, Web of Science, PubMed, CNKI, Baidu Scholar, and X-mol.
- Collection and synthesis of information on recent developments in peptide-mediated TPD.
Main Results:
- Peptide-mediated TPD shows promise in overcoming current limitations.
- Engineering of highly selective peptides enhances binding affinity for undruggable proteins and improves solubility/permeability.
- Next-generation delivery systems are being developed to reduce nonspecific biodistribution and off-target toxicity, enhancing therapeutic potential.
Conclusions:
- Peptide-based PROTAC development is advancing rapidly.
- Innovative delivery strategies are crucial for enhancing the efficiency and therapeutic precision of peptide-mediated TPD.
- Future research will focus on optimizing peptide-based TPD for improved efficacy and safety.
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