J. Med. Chem. | new BTK - PROTACs: blood system lymphoma treatment of new ideas

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Recently, Dong Xiaobu/Che Jinxin from the Department of Pharmacy of Zhejiang University, Zhou Yubo and Li Jia from the Shanghai Institute of Materia Medica of the Chinese Academy of Sciences (CAS) have jointly reported a novel Medicinal medicinal medicine BGK-Protacs (C13), a novel glucose-tyrosine kinase (BTK) depressant. Compared with ibrutinib and other drugs, the compound showed inhibitory effects on different blood cancer cells and decreased BTK-related signaling pathways, improved oral bioavailability, effectively reduced BTK protein levels and inhibited tumor growth, and could be used in the treatment of lymphoma.

1. Represents the molecule

2. Targets and indications
◆ Target: Bruton tyrosine kinase
◆ Potential indication: hematologic lymphoma

3. Synthesis path

4. Biological activity
The results showed that C13 could effectively reduce the level of BTK protein and inhibit tumor growth.