Abstract

The wide application of benzimidazoles in agriculture and veterinary medi­ cine as fungicides and anthelminthic drugs, and their experimental use in cancer chemotherapy, has led to intensive research to elucidate their mode of action in detail. These studies show that bioactive benzimidazoles are specific inhibitors of microtubule assembly that act by binding to their heterodimeric subunit, the tubulin molecule. Most of the original literature on antifungal benzimidazoles has already been discussed in a number of reviews (4, 10, 1 3, 14, 19, 52). This chapter, therefore, does not give an extensive review of the complete literature but rather discusses those experiments that made essential contributions to the development of the research area. Much of our knowledge stems from research in fungal cell biology and molecular genetics that uses benzimidazoles as tools to study tubulin structure and the organization and function of microtubules. Rapid progress is being made in the latter areas, which ultimately will lead to a complete characterization of the benzimidazole binding site at the tubulin molecule and its role in microtubule assembly.

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