Citation: Keliang Li, Guoqiang Dong, Shanchao Wu, Chunquan Sheng. Discovery of an activatable near-infrared fluorescent and theranostic PROTAC for tumor-targeted detecting and degrading of BRD4[J]. Chinese Chemical Letters, ;2025, 36(6): 110280. doi: 10.1016/j.cclet.2024.110280 shu

Discovery of an activatable near-infrared fluorescent and theranostic PROTAC for tumor-targeted detecting and degrading of BRD4

The Center for Basic Research and Innovation of Medicine and Pharmacy (MOE), School of Pharmacy, Second Military Medical University (Naval Medical University), Shanghai 200433, China

wushanchao07_2@126.com

shengcq@smmu.edu.cn

Received Date: 7 May 2024
Revised Date: 12 July 2024
Accepted Date: 17 July 2024
Available Online: 18 July 2024

Figures(5)

Proteolysis-targeting chimera (PROTAC) has emerged as an efficient strategy to accurately control intracellular protein levels. However, conventional PROTACs are generally limited by nonspecific protein degradation and off-tissue side effects. Particularly, there is a lack of effective chemical tools for visualizing protein degradation. Herein, a near-infrared fluorescent and theranostic PROTAC (PRO-S-DCM) was designed for imaging the degradation of bromodomain-containing protein 4 (BRD4). PRO-S-DCM could be tumor-specifically activated and exhibited favorable imaging effects both in vitro and in vivo. PRO-S-DCM was proven to be a theranostic probe, which potently inhibited growth, invasion and migration of HeLa cells and induced cell apoptosis.
- PROTAC,
- Near-infrared,
- Theranostic,
- BRD4,
- Tumor-targeted
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