Inhibition of tubulin-microtubule polymerization by drugs of the Vinca alkaloid class.
A series of Vinca alkaloids were found to block polymerization of crude tubulin extracts of porcine brain in a dose-dependent manner. This appears to be a specific effect occurring at low concentrations of drug. The concentration of vinblastine that prevents polymerization by 50% was 4.3 x 10(-7) mole/liter for a tubulin concentration of 3.0 mg/ml, and this concentration is consistent with levels achieved in vivo following routine pharmacological doses in humans.
D000818:Animals; D003078:Colchicine / Q000378:metabolism / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006023:Glycoproteins / Q000378:metabolism*; D066298:In Vitro Techniques; D008870:Microtubules / Q000187:drug effects* / Q000378:metabolism; D011108:Polymers; D013552:Swine; D014404:Tubulin / Q000378:metabolism*; D014747:Vinblastine / Q000378:metabolism / Q000494:pharmacology; D014748:Vinca Alkaloids / Q000378:metabolism / Q000494:pharmacology*; D014750:Vincristine / Q000378:metabolism / Q000494:pharmacology; D014783:Viscosity
D006023:Glycoproteins; D011108:Polymers; D014404:Tubulin; D014748:Vinca Alkaloids; D014750:Vincristine; D014747:Vinblastine; D003078:Colchicine