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Author

Zheng-Yu Jiang

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Oct 2026

Discovery of Tricyclic Oxazinoquinolinone-Based BCL6 PROTAC Degraders with Potent Activity Against Diffuse Large B-Cell Lymphoma

B-cell lymphoma 6 (BCL6) is a key transcriptional repressor involved in the pathogenesis of diffuse large B-cell lymphoma (DLBCL). In this study, scaffold hopping of BI-3802 led to compound 1, a new tricyclic BCL6-targeting ligand. Further optimization of linker architecture and CRBN-recruiting motifs led to compound...

Xue-Tao Chen, Ru-Ju Xu, Xiao-Ran Wang et al. · 0 citations
Open access Sep 2026

Allosteric modulation of YTHDFs by ellagic acid suppresses triple-negative breast cancer via non-canonical activation of the HIF-1α pathway.

Triple-negative breast cancer (TNBC) lacks effective targeted therapies, and YTHDF proteins are frequently overexpressed in this malignancy, which correlates with adverse prognosis. Through high-throughput drug screening, we identify ellagic acid (EA) as a compound that binds to YTHDF proteins and disrupts their intera...

Jian-Heng Zhou, Yu-Yuan Li, Xue-Tao Chen et al. · 0 citations
Open access Aug 2026

Harnessing the E3 Ligase KLHL12 for Tumor-Selective Protein Degradation.

KLHL12 is identified as a potentially tumor-selective E3 ligase and the development of the first-in-class KLHL12-recruiting PROTACs are reported, which established KLHL12 as a promising tumor‑selective E3 ligase and provided a KLHL12-recruiting PROTAC platform for cancer therapy.

Shicheng Xu, Xian Zhang, Shun-Bo Hu et al. · 0 citations

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