Journal
PHARMACEUTICALS
Volume 13, Issue 1, Pages -Publisher
MDPI
DOI: 10.3390/ph13010008
Keywords
anti-cancer; anti-tubulin; tubulin binding; microtubule-targeting agents; colchicine; colchicine binding site; combretastatin; CA-4; tubulin destabilizing
Categories
Funding
- Trinity College Dublin's Provost's PhD Project Award
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It is over 50 years since the discovery of microtubules, and they have become one of the most important drug targets for anti-cancer therapies. Microtubules are predominantly composed of the protein tubulin, which contains a number of different binding sites for small-molecule drugs. There is continued interest in drug development for compounds targeting the colchicine-binding site of tubulin, termed colchicine-binding site inhibitors (CBSIs). This review highlights CBSIs discovered through diverse sources: from natural compounds, rational design, serendipitously and via high-throughput screening. We provide an update on CBSIs reported in the past three years and discuss the clinical status of CBSIs. It is likely that efforts will continue to develop CBSIs for a diverse set of cancers, and this review provides a timely update on recent developments.
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