Signal transducer and activator of transcription 6 (STAT6), a key mediator of IL-4/IL-13 signaling, regulates Th2 differentiation, making it an attractive target for atopic dermatitis (AD). The reported phosphopeptide-based STAT6 proteolysis-targeting chimera (PROTAC) established proof of concept for targeted STAT6 d...
Wen-Tao Wang, Meng-Yu Zhao, Liu-Zhi Hu et al.· Journal of Medicinal Chemist...· 0 citations
Bromodomain-containing protein 9 (BRD9) has emerged as an epigenetic target in hematologic malignancies. However, previous studies on BRD9 PROTACs reported MYC upregulation following chronic administration. Here, we describe bifunctional BRD9 PROTAC/immunomodulatory drug (IMiD) degraders engineered to simultaneously el...
Hai-Ting Duan, Ruo-Xin Chen, Jing-Yu Zhang et al.· Journal of Medicinal Chemist...· 0 citations
The AI-guided development of a first-in-class proteolysis-targeting chimera (PROTAC) designed to selectively degrade the CLIP1-LTK fusion protein is reported, providing a promising therapeutic strategy for overcoming acquired resistance in kinase-driven cancers.
Shi-Cheng Chen, Hai-Ting Duan, S. Zhong et al.· Proceedings of the National...· 0 citations
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