Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review
| Autor: | Eavan McLoughlin, Niamh M. O’Boyle |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Drug media_common.quotation_subject lcsh:Medicine lcsh:RS1-441 Pharmaceutical Science Computational biology Review 01 natural sciences colchicine Tubulin binding lcsh:Pharmacy and materia medica 03 medical and health sciences Microtubule Colchicine binding Drug Discovery Binding site colchicine binding site anti-cancer media_common biology 010405 organic chemistry lcsh:R Rational design Correction microtubule-targeting agents tubulin destabilizing 0104 chemical sciences anti-tubulin 030104 developmental biology Tubulin Drug development biology.protein Molecular Medicine tubulin binding combretastatin CA-4 |
| Zdroj: | Pharmaceuticals Pharmaceuticals, Vol 13, Iss 1, p 8 (2020) |
| ISSN: | 1424-8247 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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