Glioblastoma, or GBM, is among the most common and malignant types of primary brain tumors in adults, and one with a poor prognosis. The tendency of this type of tumor to aggressively and widely spread through the brain makes it nearly impossible to completely remove the cancer through surgery. Although a limited number of chemotherapy drugs have been approved to treat glioblastoma, the first-line treatments like the drug temozolomide often cause chemo-resistance, meaning the drug becomes ineffective against the tumor and any recurrences.

Recently, Professor Li Minyong's group at the School of Pharmaceutical Sciences published an effective compound called YZ129 in treating glioblastoma, which has become resistant to other drugs, as a cover article in the 2019 March issue of Cell Chemical Biology. Their findings discovered a class of HSP90 inhibitors with strong therapeutic potential against glioblastoma. YZ129 directly interacted with HSP90 to antagonize its chaperoning effect on calcineurin to abrogate NFAT nuclear translocation, and also suppressed other proto-oncogenic pathways including hypoxia, glycolysis, and the PI3K/AKT/mTOR axis. When YZ129 was injected in an animal model of brain tumors, the compound effectively curtailed glioblastoma growth and promoted cancer cell death.

Professor Li Minyong's group has been working on visualization analysis-based drug discovery. IN recent years, his team has published a series of papers on various prestigious journals such as Chem. Soc. Rev., Anal. Chem., J. Med. Chem., Chem. Commun., etc., which have been highlighted by various journals and internet media. The current work is supported by the National Natural Science Foundation of China, the Taishan Scholar Program, and the Qilu Young Scholar Program of Shandong University.

Related reading:

https://www.cell.com/cell-chemical-biology/fulltext/S2451-9456(18)30431-8

Written by: Li Linwei

Edited by: Che Huiqing