Target Protein

Summary

PROTAC is a small molecular complex targeting protein degradation. After the PROTAC molecule enters the cell, the target protein (Protein of interest, POI) ligand in its structure can specifically bind to the corresponding target protein, while the other end can recruit E3 ligase to form a POI-Linker-E3 ligase ternary complex, in which E3 ligase can mediate the ubiquitin binding enzyme E2 to ubiquitin-binding POI. 

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Introduction

POI labeled by ubiquitin is recognized and degraded by the proteasome. In this process, there is no need for the target protein-ligand to occupy the binding site for a long time, only the short-term formation of the ternary complex can instantly complete the ubiquitination of the target protein, and PROTAC can be recycled many times in the cell. With the development of the great potential of protein-targeted degradation technology, the most exciting thing is that it has the opportunity to use a variety of proteomes that once could not be treated by drugs.

References

For more information, please see PROTAC Technology.

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