Antimicrotubular drugs binding to vinca domain of tubulin

Gupta, Suvroma ; Bhattacharyya, Bhabatarak (2003) Antimicrotubular drugs binding to vinca domain of tubulin Molecular and Cellular Biochemistry, 253 (1-2). pp. 41-47. ISSN 0300-8177

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Studies on vinca domain binding drugs were done in great details by a number of workers as it is recognized as a potential target for anticancer drug development. Their structures, properties, mode of action, success and failures as potential anticancer drug have been discussed in short details in this review. Among these drugs rhizoxin and maytansine are competitive inhibitors, and bind at the vinblastine binding site of tubulin where as others are non-competitive inhibitors. Besides binding, these drugs also differ in the extent of GTP hydrolysis, GTP exchange and in the stabilization of colchicine binding site. The toxicity level of these drugs towards the host cells and the extent of efflux of drugs by the P-glycoprotein mediated pump are also discussed.

Item Type:Article
Source:Copyright of this article belongs to Springer-Verlag.
Keywords:Tubulin; Microtubules; Spindle; Anticancer Drugs; Vinblastine
ID Code:26136
Deposited On:06 Dec 2010 13:02
Last Modified:21 Jan 2011 06:09

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