New microtubule/tubulin-targeted anticancer drugs and novel chemotherapeutic strategies.
Wilson, L and Jordan, M A
J Chemother, 16 Suppl 4: 83-5 (2004)
2004
Mostrar resumen
The clinical success of the taxanes and the vinca alkaloids has sparked a major search for new drugs that perturb mitotic spindle microtubule dynamics and function, yielding a large number of promising compounds. A potential valuable strategy would be to use core microtubule-targeted drugs along with novel targeted drug therapies as they are developed, where the antitumor activity of a targeted drug can be combined with the power of low dose microtubule-targeted therapy. The goal of such combination therapy is to achieve high efficacy, reduced toxicity, and reduced emergence of drug resistance. | 15688618
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Crystallographic structure of tubulin: implications for dynamics and drug binding.
Downing, K H and Nogales, E
Cell Struct. Funct., 24: 269-75 (1999)
1998
Mostrar resumen
The structure of tubulin, recently solved by electron crystallography, has given a first look at the molecular basis for some of the properties of tubulin and microtubules that have been observed over the last decades. We discuss how the structure relates to some of these properties, and how inferences about drug binding sites can explain some of the effects of the drugs on tubulin. Microtubules can form a highly dynamic system that requires careful tuning of the stability and properties of tubulin and its interactions with its many ligands. Understanding these interactions can provide fundamental information on the regulation of the microtubule system. | 15216882
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