Fms-like tyrosine kinase 3 (FLT3), a member of the type III receptor tyrosine kinase family, is identified as a promising drug target for treatment of acute myeloid leukemia (AML). Here, we designed and synthesized a series of new FLT3 PROTAC degraders by incorporating rigid linkers between gilteritinib and CRBN ligand...
Li-Cheng Zhou, Ying-Long Chen, Jia-He Li et al.· Bioorganic & Medicinal Chemi...· 0 citations
Transcription factor EB (TFEB) is a promising target for autophagy regulation and cancer therapy, yet it has long been regarded as an undruggable protein. Starting from eltrombopag, an FDA-approved agent that exhibits both thrombopoietin receptor (Tpo-R) agonistic activity and TFEB inhibitory potency, we performed syst...
Chang-Le Du, Ya-Ping Rong, Zi-Lu Wang et al.· Journal of Medicinal Chemist...· 0 citations
These findings demonstrate that minimal structural alteration permits precision control over degrader target selectivity, while furnishing selective chemical probes for NSD2 and GSPT1.
Wei-Zhong Shen, Yi-Han Liu, Lian-Chao Liu et al.· bioRxiv· 0 citations
Molecular editing, rooted in synthetic chemistry, has emerged as a powerful tool for structure optimization in medicinal chemistry but remains underutilized in targeted protein degradation. Here, we demonstrate the utility of molecular editing by repurposing the NSD2 degrader LLC0424 with GSPT1 neosubstrate engagement...
Wei-Zhong Shen, Yi-Han Liu, Lian-Chao Liu et al.· bioRxiv· 0 citations
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