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首页> 外文期刊>Acta biomaterialia >pH-controllable cell-penetrating polypeptide that exhibits cancer targeting
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pH-controllable cell-penetrating polypeptide that exhibits cancer targeting

机译：pH可控的细胞穿透多肽，其呈现癌症靶向

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Helical peptides were naturally-occurring ordered conformations that mediated various biological functions essential for biotechnology. However, it was difficult for natural helical polypeptides to be applied in biomedical fields due to low bioavailability. To avoid these problems, synthetic alpha-helical polypeptides have recently been introduced by further modifying pendants in the side chain. In spite of an attractive biomimetic helical motif, these systems could not be tailored for targeted delivery mainly due to nonspecific binding events. To address these issues, we created a conformation-transformable polypeptide capable of eliciting a pH-activated cell-penetrating property solely at the cancer region. The developed novel polypeptide showed that the bare helical conformation had a function at physiological conditions while the pH-induced helical motif provided an active cell-penetrating characteristic at a tumor extracellular matrix pH. The unusual conformation-transformable system can elicit bioactive properties exclusively at mild acidic pH.
机译：螺旋肽是天然存在的有序的顺序构象，介导对生物技术至关重要的各种生物学功能。然而，由于低生物利用度，天然螺旋多肽难以应用于生物医学领域。为了避免这些问题，最近通过侧链的进一步改性侧链引入合成α-螺旋多肽。尽管有吸引力的生物仿生螺旋图案，但这些系统无法针对有针对性的递送量身定制，主要是由于非特异性结合事件。为了解决这些问题，我们创建了一种能够仅在癌症区域引发pH激活的细胞穿透性的构象可转化的多肽。开发的新型多肽表明，裸螺旋构象在生理条件下具有功能，而pH诱导的螺旋基序在肿瘤细胞外基质pH下提供了活性细胞穿透性。不寻常的构象可转化的系统可以专门在轻度酸性pH下引发生物活性性质。

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