Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation.

Haixia LiuChaowei RenRenhong SunHuihui WangYuexiong ZhanXiaobao YangBiao JiangHongli Chen

Published in: Chemical communications (Cambridge, England) (2022)

By introducing a reactive oxygen species (ROS) triggered leaving group (arylboronic acid) to the parent PROTACs, ROS-responsive Pre-PROTACs were designed and evaluated. Pre-PROTAC (7) efficiently degraded the target protein BRD3 according to ROS levels. Our research provides an effective approach to control PROTAC activation by the endogenous ROS-related microenvironment.

Keyphrases

reactive oxygen species
cell death
dna damage
stem cells
cancer therapy
protein protein
amino acid
binding protein
oxidative stress
small molecule
drug delivery
drug induced