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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Видео Proteins as Drug Targets: Microtubule Inhibitors - Medicinal Chemistry 1.9 канала Daniel S.