2010
DOI: 10.1007/s12575-010-9029-5
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Quick and Simple Detection Technique to Assess the Binding of Antimicrotubule Agents to the Colchicine-Binding Site

Abstract: Development of antimitotic binding to the colchicine-binding site for the treatment of cancer is rapidly expanding. Numerous antimicrotubule agents are prepared every year, and the determination of their binding affinity to tubulin requires the use of purified tubulins and radiolabeled ligands. Such a procedure is costly and time-consuming and therefore is limited to the most promising candidates. Here, we report a quick and inexpensive method that requires only usual laboratory resources to assess the binding… Show more

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Cited by 63 publications
(68 citation statements)
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“…(46) Control cells treated with 0.5% DMSO followed by EBI show an intense β-tubulin–EBI adduct band. With the exception of compound 11 , all PIB-SO inhibited the EBI binding to the C-BS.…”
Section: Discussionmentioning
confidence: 99%
“…(46) Control cells treated with 0.5% DMSO followed by EBI show an intense β-tubulin–EBI adduct band. With the exception of compound 11 , all PIB-SO inhibited the EBI binding to the C-BS.…”
Section: Discussionmentioning
confidence: 99%
“…Microtubule-destabilising agents that bind at the colchicine-site, such as 2, prevent the formation of the β-tubulin-EBI adduct [33]. MCF-7 cells were treated with vehicle control, 2 (10 μM) or 1 (40 μM) for 2 h, followed by EBI for an additional 1.5 h (Figure 10).…”
mentioning
confidence: 99%
“…EBI binds to the colchicine site of β-tubulin and forms a cross-link between the Cys239 and the Cys354 residues [24]. The EBI-β-tubulin adduct can be easily separated from normal β-tubulin by western blot using β-tubulin antibody because the EBI-β-tubulin adduct band migrates faster than the normal β-tubulin band.…”
Section: Sklb060 Binds To Colchicine Binding Site On β-Tubulinmentioning
confidence: 99%
“…The EBI-β-tubulin adduct can be easily separated from normal β-tubulin by western blot using β-tubulin antibody because the EBI-β-tubulin adduct band migrates faster than the normal β-tubulin band. Tubulin inhibitors binding to the colchicine-binding site can inhibit the formation of the EBI-β-tubulin adduct, which makes the assay an easy approach to identify whether inhibitors bind to colchicine-binding site [24]. As shown in Fig.…”
Section: Sklb060 Binds To Colchicine Binding Site On β-Tubulinmentioning
confidence: 99%