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Researchers Discover Potential New Treatment for Glioma

Sep 11, 2020

A recent research conducted by LIU Qingsong and LIU Jing, professors of the Institute of Health & Medical Technology, Hefei Institute of Physical Science, reported that small molecule NG52, an inhibitor of yeast cycle regulated kinase, might be useful for glioma.

In this study, the researchers used high-throughput screening approach and identified that NG52 could inhibit PGK1 kinase activity in the micromolar arrange, consequently slow down the progression of glioma.

Further investigation revealed that NG52 could partially promote the aerobic metabolism process of cells by inhibiting the activity of PGK1 kinase, thereby inhibiting the proliferation of cancer cells.

Besides, in vivo animal experiments showed that NG52 had good antitumor effect against glioma. These evidences provided the proof-of-concept that targeting PGK1 kinase activity might be useful for the treatment of glioma.

Glioma is the most common brain tumor, which accounts for about 60% of all brain tumors. PGK1 kinase has been found overexpressed in glioma. However, no small molecule inhibitors targeting its activity have been reported yet and there is no better choice in the clinical treatment of glioma other than surgery.

Therapeutically, the combination of temozolomide (TMZ) chemotherapy and radiotherapy is often used in the clinic. However, most patients relapse within a few years after treatment.

This study points the way for potential treatment for glioma to meet the unfilled clinical needs.

The study was supported by the National Natural Science Foundation of China, the strategic science and technology pilot project of "personalized medicine" of the Chinese Academy of Sciences (CAS), the key research plan of Frontier Science of CAS, and special support of China Postdoctoral fund.

A. NG52 can inhibit the activity of PGK1 kinase; B. NG52 has strong anti-proliferation effect on primary glioma cells; C. NG52 has strong anti-tumor effect on glioma PDX. (Image by WANG Aoli)

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ZHOU Shu

Hefei Institutes of Physical Science

E-mail:

Pharmacologically inhibiting phosphoglycerate kinase 1 for glioma with NG52

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