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Updated: Jan 4, 2026

Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes

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Triazol: a privileged scaffold for proteolysis targeting chimeras.

Li-Wen Xia^1,2, Meng-Yu Ba^1,2, Wei Liu³

¹School of Pharmaceutical Science, Zhengzhou University, Zhengzhou, Henan 450001, China.

Future Medicinal Chemistry

|November 9, 2019

Summary

Proteolysis targeting chimeras (PROTACs) offer a novel therapeutic strategy by degrading target proteins. Triazole-based PROTACs show significant anticancer potential, highlighting their structure-activity relationship for drug development.

Keywords:

PROTACs SAR drug development protein degradation triazole

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Area of Science:

Medicinal Chemistry
Drug Discovery
Molecular Biology

Background:

Traditional drugs face limitations due to occupancy-driven pharmacology.
Proteolysis targeting chimeras (PROTACs) offer an event-driven mechanism for targeted protein knockdown.
The linker component of PROTACs is critical for their efficacy.

Purpose of the Study:

To review PROTACs incorporating a triazole scaffold.
To discuss the structure-activity relationship of triazole-based PROTACs.
To analyze the milestones and critical aspects of PROTAC drug discovery.

Main Methods:

Literature review of PROTACs with triazole linkers.
Analysis of structure-activity relationships.
Discussion of key developments and challenges in PROTAC technology.

Main Results:

Triazole linkers have been successfully incorporated into PROTACs.
Certain triazole-based PROTACs exhibit promising anticancer activities.
The structural features of the triazole linker influence PROTAC performance.

Conclusions:

PROTACs represent a promising therapeutic modality.
Triazole scaffolds are valuable components in PROTAC design.
Further research into triazole-based PROTACs could lead to novel cancer treatments.