Proteins as Drug Targets: Microtubule Inhibitors - Medicinal Chemistry 1.9

Microtubule is an attractive target for anticancer drugs because of its important role in mitosis. In fact, it has been one of the most successful chemotherapeutic targets. Mitotic or microtubule inhibitors would disrupt microtubules and inhibit mitosis of cancer cells because cancer cells are able to grow and eventually spread through the body through non-stop mitosis. Cancer cells tend to divide a lot more frequently than normal cells, so are more sensitive to inhibition of mitosis.
Two main classes of mitotic inhibitors or microtubule inhibitors are microtubule stabilizer/stabilizing agent and microtubule destabilizer/destabilizing agent. Microtubule stabilizer would either promote the polymerization or inhibit the depolymerization of microtubules into tubulin heterodimer. One example would be Vinca alkaloids, which were first extracted from periwinkle plants. Microtubule destabilizer would disrupt microtubule polymerization. One example is taxanes, which were first extracted from the barks of Yew trees. But despite the difference between the microtubule stabilizer and destabilizer, the final result is the same, which is disrupting mitosis, stopping cell proliferation and causing cell death.
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[@gdkim0217]

Thank you!

[@molemanchem4385]

You're welcome!

[@hoangvan1991]

This video is so helpful for me, thank you so much.

[@Rahma_ASafar]

Perfect 👌🏻 ❤

[@andrewwee7458]

Thank you, it was very informative!

[@molemanchem4385]

Glad you like it!

[@killianpapail9324]

very nice vidéo!

[@molemanchem4385]

Thanks!!

[@mytrueserenity5666]

Interesting! Any idea why the yew or trees from the Pacific Northwest were selected for initial study? Were scientists prompted by the traditional use of the yew's bark? Any idea?

[@molemanchem4385]

Thanks for your question! Based on a literature, National Cancer Institute has conducted a research on natural compounds from 15000+ species of plants and the Pacific yew tree was among them. But they could certainly included it in the study because of its traditional use, like you said:)
Feel free to look up this paper if you are interested:
Mol Biol Cell. 2014 Sep 15; 25(18): 2677-2681.

[@mytrueserenity5666]

@@molemanchem4385 Thanks!