Enhanced protein degradation by intracellular delivery of pre-fused PROTACs using lipid-like nanoparticles

• Published in: Journal of controlled release Vol. 330; pp. 1244 - 1249
• Main Authors: Chen, Jinjin, Qiu, Min, Ma, Feihe, Yang, Liu, Glass, Zachary, Xu, Qiaobing
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 10.02.2021
• Subjects: Drug delivery; heat-shock protein 70; hydrophobicity; Intercellular Signaling Peptides and Proteins; Lipid-like nanoparticle (LNP); Lipids; molecular weight; Nanoparticles; permeability; PROTAC; Protein degradation; Proteolysis; surface area; Protein degradation; Drug delivery; PROTAC; Lipid-like nanoparticle (LNP)

Proteolysis-targeting chimaera (PROTAC) technology is an emerging approach for achieving targeted degradation of a protein of interest (POI) intracellularly. However, the cell permeability of PROTACs is limited by their high molecular weight and total polar surface area. Moreover, the activation of...