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Inhibition of angiogenesis and breast cancer in mice by the microtubule inhibitors 2-methoxyestradiol and taxol.
TLDR
Recognition of the antiangiogenic and antitumor properties of 2-ME and Taxol may be crucial in planning clinical applications to angiogenesis-dependent diseases.
2-Methoxyestradiol, an endogenous mammalian metabolite, inhibits tubulin polymerization by interacting at the colchicine site.
TLDR
A mammalian metabolite of estradiol binds to the colchicine site of tubulin and, depending on reaction conditions, either inhibits assembly or seems to be incorporated into a polymer with altered stability properties.
Activities of the Microtubule-stabilizing Agents Epothilones A and B with Purified Tubulin and in Cells Resistant to Paclitaxel (Taxol®)*
TLDR
The epothilones are competitive inhibitors of the binding of [3H]paclitaxel to tubulin polymers, and there were different proportions of various mitotic aberrations following treatment with different drugs.
A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.
TLDR
Using the recently determined X-ray structure of the tubulin:colchicinoid complex as the template, docking studies were employed to determine the binding modes of a set of structurally diverse colchicine site inhibitors and this work constructed a comprehensive, structure-based pharmacophore that in combination with molecular dynamics simulations confirms and extends the understanding of binding interactions at the colchichine site.
Synthesis, antitubulin and antimitotic activity, and cytotoxicity of analogs of 2-methoxyestradiol, an endogenous mammalian metabolite of estradiol that inhibits tubulin polymerization by binding to
TLDR
The potencies of the analogs as cytotoxic and antimitotic agents in cancer cell cultures correlated with their potencies as inhibitors of tubulin polymerization, supporting the hypothesis that inhibition of tubul polymerization is the mechanism of the cytotoxicity action of 2-methoxyestradiol and its congeners.
Structure and absolute stereochemistry of hectochlorin, a potent stimulator of actin assembly.
TLDR
Hectochlorin shows both a unique profile of cytotoxicity by the COMPARE algorithm and potent inhibitory activity toward the fungus Candida albicans.
Discodermolide, a cytotoxic marine agent that stabilizes microtubules more potently than taxol.
TLDR
Discodermolide arrests Burkitt lymphoma cells in mitosis and shows spectacular rearrangement of the microtubule cytoskeleton, including extensive microtubules bundling in breast carcinoma cells.
Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum.
TLDR
The structural simplicity and ready synthesis of combretastatin A-1 and combretastsatin B-1 suggest that these new biosynthetic products will become useful in a variety of biological endeavors.
The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and
TLDR
It is demonstrated that discodermolide is a competitive inhibitor with [3H]paclitaxel in binding to tubulin polymer, with an apparent Ki value of 0.4 microM, and that these properties represent hypernucleation phenomena.
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