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首页> 外文期刊>Pharmaceutical research >Novel cyclopeptides for the design of MMP directed delivery devices: a novel smart delivery paradigm.
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Novel cyclopeptides for the design of MMP directed delivery devices: a novel smart delivery paradigm.

机译：用于设计MMP定向递送装置的新型环肽：一种新型的智能递送范例。

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PURPOSE: Matrix metalloproteinases (MMP) are a family of proteolytic enzymes, the expression of which in a key step of tumor progression has been better defined recently. The studies highlighted the ongoing need for very specific inhibitors, substrates or release devices designed to be selective for one or at least very few MMPs. METHODS: This report deals with the design, synthesis and in vitro evaluation of linear and especially novel cyclic peptidic moieties, embodying MMP cleavable sequences designed to answer these questions. FRET (fluorescence resonance energy transfer) labelling via chromophore-modified amino-acids was used to give access to enzyme kinetics. RESULTS: Evaluation of these peptides showed that cyclisation gives rise to high specificity for certain MMP, suggesting that this approach could provide very specific MMP substrate. Moreover, cyclic structures present a very good plasma stability. CONCLUSIONS: These original derivatives could allow the design of MMP-controlled delivery devices, the specificity of which will be retained in complex biological media and in vivo.
机译：目的：基质金属蛋白酶（MMP）是一类蛋白水解酶，其在肿瘤进展的关键步骤中的表达最近得到了更好的定义。研究强调了对非常特异性的抑制剂，底物或释放装置的持续需求，这些抑制剂，底物或释放装置旨在对一种或至少几种MMP具有选择性。方法：本报告涉及线性，尤其是新的环状肽部分的设计，合成和体外评估，其中包含旨在回答这些问题的MMP可裂解序列。通过发色团修饰的氨基酸进行的FRET（荧光共振能量转移）标记用于获得酶动力学。结果：对这些肽的评估表明环化对某些MMP具有很高的特异性，这表明该方法可以提供非常特异性的MMP底物。此外，环状结构具有非常好的等离子体稳定性。结论：这些原始衍生物可以设计MMP控制的递送装置，其特异性将保留在复杂的生物介质和体内。

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