Macromol Biosci. 2010 Jun 11;10(6):580-4. doi: 10.1002/mabi.200900382.
In this study we formed and characterized dynamic hydrogel microspheres in which a protein conformational change was used to control microsphere volume changes and the release of an encapsulated drug. In particular, a specific biochemical ligand, trifluoperazine, induced calmodulin's nanometer scale conformation change, which translated to a 48.7% microsphere volume decrease. This specific, ligand-induced volume change triggered the release of a model drug, vascular endothelial growth factor (VEGF), at pre-determined times. After release from the microspheres, 85.6 +/- 10.5% of VEGF was in its native conformation. Taken together, these results suggest that protein conformational change could serve as a useful mechanism to control drug release from dynamic hydrogels.
在这项研究中，我们形成并表征了动态水凝胶微球，其中蛋白质构象变化用于控制微球体积变化和封装药物的释放。具体来说，一种特定的生化配体三氟拉嗪诱导钙调蛋白的纳米级构象变化，导致微球体积缩小 48.7%。这种特定的、配体诱导的体积变化触发了模型药物血管内皮生长因子（VEGF）的预定时间释放。从微球中释放后，85.6 +/- 10.5%的 VEGF 保持其天然构象。总的来说，这些结果表明蛋白质构象变化可以作为一种有用的机制来控制动态水凝胶中药物的释放。
