Mitotic inhibitors and camptothecins in chemotherapy


Mitotic Inhibitors

Mitotic inhibitors hinder the development of the mitotic spindle, causing metaphase arrest. They're primarily referred to as M-phase active, however they could also have activity in G 2 and S. These medicine is the vinca alkaloids, the epipodophyllo-toxins, and also the taxanes.

Vinca alkaloids, also known as plant alkaloids, are extracts of the periwinkle plant. They bind to microtubular proteins, that are answer to forming the mitotic spindle of the dividing cells. This binding arrests mitosis, which eventually causes cell death. The vincas act mainly in the M phase; however, high doses may also disrupt RNA and protein synthesis.

Epipodophyllotoxins were isolated in the mandrake plant. They act in the premitotic phase, G 2 and S, and hinder topoisomerase II enzyme reaction. Taxanes cause mitotic arrest by forming abnormal spindle fibers and mitotic asters.

Camptothecins

Camptothecins really are a new subcategory of cell cycle-specific drugs. They act in the S phase and inhibit topoisomerase I, a nuclear enzyme essential for maintaining DNA structure. Inhibition of the enzyme results in single-stranded DNA breaks and subsequently cell death.

Antineoplastic agents that work through all phases of the cell cycle and therefore are not restricted to a particular phase are calledcell cycle-nonspecific drugs. These drugs have an effect on the DNA molecule and display no specificity for cells that are dividing.

They're considered more toxic than their cell cycle-specific counterparts as their destructive action doesn't differentiate between normal and malignant cycling cells. Their toxicities are felt through the cell cycle. Non-specific agents receive in bolus doses simply because they cause death independently of the proliferative state of the cell. These agents also lessen the quantity of cells that make up a tumor, which is called the tumor burden.

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Note: This article was sent to us by: Alan Reed at 07252011

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