Rational Design of a Novel Tubulin Inhibitor with a Unique Mechanism of Action

A smaller molecule to attack cancer with

31 August 2022

New anti-cancer drugs could come from the discovery of a small molecule that destroys cells by disabling a key protein in the cell skeleton.

Several widely used chemotherapy drugs work by disrupting the construction of microtubules in cells, which prevents cell division from occurring in tumours. But these drugs tend to be toxic and tumours develop resistance to them.

Now, by adopting a rational-design approach, a team led by researchers from the Paul Scherrer Institute in Switzerland has found a new inhibitor of tubulin, the building block of microtubules.

Unlike other tubulin inhibitors, which are usually derived from natural products and thus have large, complex structures, the new inhibitor is small and can be easily made in a two-step process.

The small molecule is a promising starting point for developing new anti-tubulin drugs, the researchers say.

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References

1. Angewandte Chemie International Edition 61, e202204052 (2022). doi: 10.1002/anie.202204052