Inhibition of Tubulin-Microtubule Polymerization by Drugs of the Vinca Alkaloid Class
RJ Owellen, CA Hartke, RM Dickerson, FO Hains - Cancer Research, 1976 - AACR
RJ Owellen, CA Hartke, RM Dickerson, FO Hains
Cancer Research, 1976•AACRA 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× 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.
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× 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.
Summary
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 × 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.
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