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Microtubule dynamics as a target in oncology.
TLDR
This review discusses the molecular mechanisms as well as preclinical and clinical results for a variety of microtubule-targeting agents in various stages of development and offers a frank discussion of which micro Tubule- targeting agents are amenable to further development based on their availability, efficacy and toxic profile. Expand
Different ubiquitin signals act at the Golgi and plasma membrane to direct GAP1 trafficking.
TLDR
This work defines unique requirements for each of the ubiquitin-mediated sorting steps involved in delivery of Gap1p to the vacuole upon amino acid addition and demonstrates a previously unrecognized level of specificity in ubiquitIn-mediated protein sorting. Expand
Activity-dependent reversible inactivation of the general amino acid permease.
TLDR
It is reported that amino acid transport activity of Gap1p(K9R,K16R) can be rapidly and reversibly inactivated at the plasma membrane by the presence of amino acid mixtures, and a new mechanism for inhibition of permease activity in response to elevated amino acid levels is uncovered. Expand
Potent taccalonolides, AF and AJ, inform significant structure-activity relationships and tubulin as the binding site of these microtubule stabilizers.
TLDR
The potencies of taccalonolides AF and AJ and their direct interaction with tubulin, together with the previous excellent in vivo antitumor activity of this class, reveal the potential of the tacconolides as new anticancer agents. Expand
Taccalonolide binding to tubulin imparts microtubule stability and potent in vivo activity.
TLDR
AJ imparts strong inter-protofilament stability in a manner different from other microtubule stabilizers that covalently bind to tubulin, consistent with the distinct effects of the taccalonolides as compared with other stabilizers. Expand
Identification and biological activities of new taccalonolide microtubule stabilizers.
TLDR
In vivo antitumor evaluations of taccalonolides A, E, and N show that each of these molecules has in vivo antitUMor activity. Expand
α- and β-Santalols Directly Interact with Tubulin and Cause Mitotic Arrest and Cytotoxicity in Oral Cancer Cells.
TLDR
East Indian sandalwood oil and its two major constituents, α- and β-santalol, are explored against a variety of HNSCC lines and it is indicated for the first time that these compounds have the ability to directly bind to tubulin and affect microtubule formation. Expand
A Potent HDAC Inhibitor, 1-Alaninechlamydocin, from a Tolypocladium sp. Induces G2/M Cell Cycle Arrest and Apoptosis in MIA PaCa-2 Cells
TLDR
1-Alaninechlamydocin showed potent antiproliferative/cytotoxic activities in a human pancreatic cancer cell line (MIA PaCa-2) at low-nanomolar concentrations and induced G2/M cell cycle arrest and apoptosis. Expand
Taccalonolide microtubule stabilizers.
TLDR
Binding studies with the newly identified, potent taccalonolide AJ demonstrated covalent binding to β-tubulin at or near the luminal and/or pore taxane binding site(s) which stabilizes microtubule protofilaments in a unique manner as compared to other micro Tubule stabilizers. Expand
Elucidating target specificity of the taccalonolide covalent microtubule stabilizers employing a combinatorial chemical approach
TLDR
These carefully optimized, cell-permeable probes outperform commercial taxane-based probes and enable direct visualization of taccalonolides in both live and fixed cells with dramatic microtubule colocalization. Expand
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