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Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review

School of Pharmacy and Pharmaceutical Sciences, Trinity Biomedical Sciences Institute, Trinity College Dublin, D02 Dublin, Ireland
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Pharmaceuticals 2020, 13(1), 8; https://doi.org/10.3390/ph13010008
Received: 29 November 2019 / Revised: 20 December 2019 / Accepted: 23 December 2019 / Published: 3 January 2020
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.
Keywords: anti-cancer; anti-tubulin; tubulin binding; microtubule-targeting agents; colchicine; colchicine binding site; combretastatin; CA-4; tubulin destabilizing anti-cancer; anti-tubulin; tubulin binding; microtubule-targeting agents; colchicine; colchicine binding site; combretastatin; CA-4; tubulin destabilizing
MDPI and ACS Style

McLoughlin, E.C.; O’Boyle, N.M. Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review. Pharmaceuticals 2020, 13, 8.

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