The peptide PROTAC modality: a novel strategy for targeted protein ubiquitination

August 8, 2020

Jin, J., Wu, Y., Chen, J., et al.

Theranostics 2020, vol: 10(22) doi: 10.7150/thno.46985

Abstract

Despite dramatic advances in drug discovery over the decades, effective therapeutic strategies for cancers treatment are still in urgent demands. PROteolysis TArgeting Chimera (PROTAC), a novel therapeutic modality, has been vigorously promoted in preclinical and clinical applications. Unlike small molecule PROTAC, peptide PROTAC (p-PROTAC) with advantages of high specificity and low toxicity, while avoiding the limitations of shallow binding pockets through large interacting surfaces, provides promising substitutions for E3 ubiquitin ligase complex-mediated ubiquitination of “undruggable proteins”. It is worth noting that successful applications of p-PROTAC still have some obstacles, including low stability and poor membrane permeability. Hence, we highlight that p-PROTAC combined with cell-penetrating peptides, constrained conformation technique, and targeted delivery systems could be the future efforts for potential translational research.

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Topics: PROTACs, Monolith – MicroScale Thermophoresis, MST,  Publications

 

 

 

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