Drugs targeting Tubulin
Drugs targeting tubulin are important anticancer, antiworm, anti-inflammatory, and antifungals. They all bind to tubulin and change the cytoskeleton of cells.
Tubulin plays a very important role in cytoskeleton formation, α- and β-tubulins polymerize into microtubules, a major component of the eukaryotic cytoskeleton. Microtubules are essential elements for cellular division, neutrophilic movement, and helminthic nutrition.
Following drugs target tubulin
Vinka Alkaloids (Vincristine and Vinblastine)
Vinka alkaloids are M phase-specific cell cycle inhibitors, they cause metaphase (M-phase) arrest and are cytotoxic. Vinka alkaloids bind to protein tubulin and block the ability of tubulin to polymerize to form microtubules. The paracrystalline aggregates consisting of tubulin dimers and the alkaloid drug are formed. Without the formation of microtubules, a cell is frozen in metaphase, chromosomal segregation doesn’t happen and cells undergo apoptosis and dies. This property is very useful in cancer treatment.
Taxanes (Paclitaxel and docetaxel)
These drugs are active in the G2/M-phase of the cell cycle, they promote polymerization and stabilization of the polymer which leads to the accumulation of microtubules. Microtubules formed are overly stable and non-functional, and chromosome desegregation does not occur. A cell doesn’t proceed towards anaphase and undergoes apoptosis. Taxanes are also useful in anticancer drugs.
Mebendazole and Albendazole
They act by binding to parasites β-tubulin and inhibiting microtubule polymerization in the parasite. The parasite’s intestinal cells cannot absorb glucose and necessary nutrient without microtubule activity. Without glucose and nutrient helminths immobilize and die.
Colchicine
Colchicine binds to tubulin, a microtubular protein, causing its depolymerization. This disrupts cellular functions, such as the mobility of neutrophils, thus decreasing their migration into the inflamed joint. Colchicine also blocks cell division by binding to mitotic spindles. The anti-inflammatory activity of colchicine is specific for gout and it relieves pain within 12 hours of treatment.
Griseofulvin
Griseofulvin is an antifungal which enters the dermatophyte through energy-dependent transport and bind to fungal microtubules. Griseofulvin disrupts the mitotic spindle and inhibition of fungal mitosis. It is used for dermatophytosis of the scalp and hair.
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Revision for today Osmotic Diuretics
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