Associate Professor Kenro Usui and his group at the University of Tsukuba have succeeded in developing Gatastatin, a compound that inhibits γ-tubulin, which promotes the nucleation of microtubules that play an important role in cell division.

Microtubules, which are one of the cytoskeletons, are tubular proteins formed by the polymerization of α / β-tubulin, and are the main constituents of the mitotic spindle that evenly separate chromosomes during cell division.For this reason, inhibitors of α / β-tubulin are used as therapeutic agents for cancer cells that are actively undergoing cell division.However, since microtubules play an important role outside the cell division phase, there is a problem that using an inhibitor against α / β-tubulin also damages normal cells that are not undergoing cell division.

γ-Tubulin is a protein that promotes the polymerization of α / β-tubulin, and past studies have revealed that it is activated during cell division and is overexpressed in some cancer cells. It has become.From these facts, the development of an inhibitor against γ-tubulin was expected as a new anticancer drug with few side effects.

This research group consists of Glaziovianin A, a substance isolated from the leaves of legumes native to Brazil, which has the function of inhibiting the polymerization and depolymerization of microtubules, and the anticancer drug, which has the function of inhibiting the polymerization of microtubules. We have developed Gatastatin, a γ-tubulin-specific inhibitor, by synthetically developing the agent Plinabrin.In the future, it is expected that Gatastatin will be used to analyze γ-tubulin function and develop new anticancer drugs.

Source: [University of Tsukuba] Achievements leading to the development of a new type of anticancer drug-Successful development of γ-tubulin-specific inhibitor-

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