epothilone-b and taxane

epothilone-b has been researched along with taxane* in 2 studies

Other Studies

2 other study(ies) available for epothilone-b and taxane

Article	Year
Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites. Journal of natural products, 2018, 03-23, Volume: 81, Issue:3 The marine natural product zampanolide and analogues thereof constitute a new chemotype of taxoid site microtubule-stabilizing agents with a covalent mechanism of action. Zampanolide-ligated tubulin has the switch-activation loop (M-loop) in the assembly prone form and, thus, represents an assembly activated state of the protein. In this study, we have characterized the biochemical properties of the covalently modified, activated tubulin dimer, and we have determined the effect of zampanolide on tubulin association and the binding of tubulin ligands at other binding sites. Tubulin activation by zampanolide does not affect its longitudinal oligomerization but does alter its lateral association properties. The covalent binding of zampanolide to β-tubulin affects both the colchicine site, causing a change of the quantum yield of the bound ligand, and the exchangeable nucleotide binding site, reducing the affinity for the nucleotide. While these global effects do not change the binding affinity of 2-methoxy-5-(2,3,4-trimethoxyphenyl)-2,4,6-cycloheptatrien-1-one (MTC) (a reversible binder of the colchicine site), the binding affinity of a fluorescent analogue of GTP (Mant-GTP) at the nucleotide E-site is reduced from 12 ± 2 × 10 Topics: Animals; Binding Sites; Biological Products; Bridged-Ring Compounds; Cattle; Colchicine; Humans; Ligands; Macrolides; Microtubules; Nucleotides; Taxoids; Tubulin	2018
Synthesis and biological activities of high affinity taxane-based fluorescent probes. Bioorganic & medicinal chemistry letters, 2009, Feb-01, Volume: 19, Issue:3 Three fluorescent probes 3a,3b, and 4 have been synthesized through conjugation of fluorescein and difluorescein groups to the 7-OH of C-2 modified paclitaxel and cephalomannine derivatives with very high affinity to microtubules. All these probes exhibited potent tubulin assembly promotion and tumor cell killing activities, thus may be useful as tools for the determination of thermodynamic parameters and exploration of ligand-microtubule interactions. Topics: Anisotropy; Bridged-Ring Compounds; Chemistry, Pharmaceutical; Dose-Response Relationship, Drug; Drug Design; Fluorescein; Fluorescent Dyes; Ligands; Microtubules; Models, Chemical; Plant Extracts; Taxoids; Temperature; Thermodynamics; Tubulin	2009

Article

Year

Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites.

Journal of natural products, 2018, 03-23, Volume: 81, Issue:3

The marine natural product zampanolide and analogues thereof constitute a new chemotype of taxoid site microtubule-stabilizing agents with a covalent mechanism of action. Zampanolide-ligated tubulin has the switch-activation loop (M-loop) in the assembly prone form and, thus, represents an assembly activated state of the protein. In this study, we have characterized the biochemical properties of the covalently modified, activated tubulin dimer, and we have determined the effect of zampanolide on tubulin association and the binding of tubulin ligands at other binding sites. Tubulin activation by zampanolide does not affect its longitudinal oligomerization but does alter its lateral association properties. The covalent binding of zampanolide to β-tubulin affects both the colchicine site, causing a change of the quantum yield of the bound ligand, and the exchangeable nucleotide binding site, reducing the affinity for the nucleotide. While these global effects do not change the binding affinity of 2-methoxy-5-(2,3,4-trimethoxyphenyl)-2,4,6-cycloheptatrien-1-one (MTC) (a reversible binder of the colchicine site), the binding affinity of a fluorescent analogue of GTP (Mant-GTP) at the nucleotide E-site is reduced from 12 ± 2 × 10

Topics: Animals; Binding Sites; Biological Products; Bridged-Ring Compounds; Cattle; Colchicine; Humans; Ligands; Macrolides; Microtubules; Nucleotides; Taxoids; Tubulin

2018

Synthesis and biological activities of high affinity taxane-based fluorescent probes.

Bioorganic & medicinal chemistry letters, 2009, Feb-01, Volume: 19, Issue:3

Three fluorescent probes 3a,3b, and 4 have been synthesized through conjugation of fluorescein and difluorescein groups to the 7-OH of C-2 modified paclitaxel and cephalomannine derivatives with very high affinity to microtubules. All these probes exhibited potent tubulin assembly promotion and tumor cell killing activities, thus may be useful as tools for the determination of thermodynamic parameters and exploration of ligand-microtubule interactions.

Topics: Anisotropy; Bridged-Ring Compounds; Chemistry, Pharmaceutical; Dose-Response Relationship, Drug; Drug Design; Fluorescein; Fluorescent Dyes; Ligands; Microtubules; Models, Chemical; Plant Extracts; Taxoids; Temperature; Thermodynamics; Tubulin

2009