Syringolin B-inspired proteasome inhibitor analogue TIR-203 exhibits enhanced biological activity in multiple myeloma and neuroblastoma.
作者： John Opoku-Ansah , Tannya R. Ibarra-Rivera , Michael C. Pirrung , André S. Bachmann
DOI: 10.3109/13880209.2011.626784
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摘要: Context: The bacterium Pseudomonas syringae pv. (Pss) is a pathogen of many plant species and causes, for example, brown spot disease in bean plants (Phaseolus vulgaris). Pss excretes the syringolins, natural product molecules that act as virulence factors inhibit proteasome host plants.Objective: Proteasome inhibitors belong to an important class anticancer agents bortezomib (Velcade®) has been Food Drug Administration-approved treatment multiple myeloma (MM) mantle cell lymphoma. Syringolins represent new present work was undertaken design potent syringolin-inspired analogue (TIR-203) drug development.Materials methods: TIR-203 tested against human MM neuroblastoma (NB) cells. Cancer cells were treated with at various concentrations (0–10 µM) viability measured using MTS assay. To determine effects on proteasomal activities, culture-based ...
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