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Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes
Published on: January 12, 2024
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Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
Chao Wang1,2, Yujing Zhang3, Lingyu Shi1,2
1The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, China.
Journal of Enzyme Inhibition and Medicinal Chemistry
|May 19, 2022
Summary
Specific and nongenetic IAP-dependent protein erasers (SNIPERs) offer targeted protein degradation for diseases. This review covers SNIPER advances and their therapeutic potential.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Proteolytic targeting chimaeras (PROTACs) are heterobifunctional molecules for targeted protein degradation.
- PROTACs induce polyubiquitination of proteins of interest (POIs) via the ubiquitin-proteasome system.
- Various PROTACs, including CRBN, VHL, IAP, and MDM2-based, have been developed.
Purpose of the Study:
- To review the latest advancements in specific and nongenetic IAP-dependent protein erasers (SNIPERs).
- To discuss the therapeutic opportunities and challenges for SNIPERs in disease treatment.
- To highlight the structure and mechanism of IAP-based PROTACs.
Main Methods:
- Literature review of SNIPER research.
- Analysis of SNIPER structures (target protein ligand, E3 ligase ligand, linker).
- Examination of SNIPER efficacy in various diseases, particularly cancer.
Main Results:
- SNIPERs effectively degrade target proteins implicated in diseases.
- Extensive research demonstrates SNIPERs' success in multiple disease models.
- SNIPERs are a promising therapeutic strategy, especially for cancers.
Conclusions:
- SNIPERs represent a significant advancement in targeted protein degradation technology.
- Further research is needed to overcome challenges for SNIPERs' clinical application.
- SNIPERs hold considerable promise as future therapeutic agents.
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