Bioactive pre-tubulysins and use thereof
Pretubulysins were already claimed as a
hypothetically common preliminary stage of tubulysins in 2004. Scientists of Saarland University provided evidence for the existence of this biosynthesis intermediate and made it available by synthesis. Compared to tubulysins the pretubulysins are easier to synthesize and can be obtained in higher quantity. The scientists show that the simplified precursor is nearly equally potent compared to the parent compound. Pretubulysin induces apoptosis and inhibits cancer cell migration and tubulin assembly in vitro. Consequently, pretubulysin appears to be an ideal candidate for future development in preclinical trials and is a very promising early lead structure in cancer therapy.
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