Chemical-functional diversity in cell-penetrating peptides.
Chemical-functional diversity in cell-penetrating peptides.
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DOI：
10.1371/journal.pone.0071752
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发表时间：
2013
期刊：
影响因子：
3.7
通讯作者：
De Spiegeleer B
中科院分区：
文献类型：
--
作者：
Stalmans S;Wynendaele E;Bracke N;Gevaert B;D'Hondt M;Peremans K;Burvenich C;De Spiegeleer B
细胞穿透肽（CPP）是克服细胞膜屏障的有前途的工具。它们已经成功地用作几种有问题的货物的承运人，例如货物。质粒 DNA 和 (si)RNA，为新疗法打开了大门。尽管文献中已经描述了数百种 CPP，但目前只有少数 CPP 的商业应用可用。这些肽的细胞摄取研究由于所使用的技术和其他实验条件不一致，导致其摄取机制和结构特性的不确定性。为了阐明影响肽细胞穿透特性的结构特征，我们探索了已经研究了细胞摄取的肽的化学功能空间。对于 186 种肽，基于文献中细胞流入的分散定量结果，提出了一种新的细胞穿透 (CP) 反应。主成分分析 (PCA) 和定量结构-性质关系研究 (QSPR) 使用化学分子描述符和我们新定义的 CP 响应，了解到除了 CPP 的典型众所周知的性质（即正电荷和两亲性）之外，构成原子的形状、结构复杂性和 3D 模式也会影响肽的细胞摄取能力。
Cell-penetrating peptides (CPPs) are a promising tool to overcome cell membrane barriers. They have already been successfully applied as carriers for several problematic cargoes, like e.g. plasmid DNA and (si)RNA, opening doors for new therapeutics. Although several hundreds of CPPs are already described in the literature, only a few commercial applications of CPPs are currently available. Cellular uptake studies of these peptides suffer from inconsistencies in used techniques and other experimental conditions, leading to uncertainties about their uptake mechanisms and structural properties. To clarify the structural characteristics influencing the cell-penetrating properties of peptides, the chemical-functional space of peptides, already investigated for cellular uptake, was explored. For 186 peptides, a new cell-penetrating (CP)-response was proposed, based upon the scattered quantitative results for cellular influx available in the literature. Principal component analysis (PCA) and a quantitative structure-property relationship study (QSPR), using chemo-molecular descriptors and our newly defined CP-response, learned that besides typical well-known properties of CPPs, i.e. positive charge and amphipathicity, the shape, structure complexity and the 3D-pattern of constituting atoms influence the cellular uptake capacity of peptides.
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影响因子：
13.8
作者：
CHOU, PY;FASMAN, GD
通讯作者：
FASMAN, GD
影响因子：
3.7
作者：
Alves ID;Bechara C;Walrant A;Zaltsman Y;Jiao CY;Sagan S
通讯作者：
Sagan S
DOI：
10.1016/j.bbrc.2008.04.039
发表时间：
2008-07-11
影响因子：
3.1
作者：
Amand, Helene L.;Fant, Kristina;Esbjorner, Elin K.
通讯作者：
Esbjorner, Elin K.
影响因子：
4.8
作者：
Drin, G;Cottin, S;Temsamani, J
通讯作者：
Temsamani, J
DOI：
10.1046/j.1432-1327.2001.01997.x
发表时间：
2001-03-01
期刊：
EUROPEAN JOURNAL OF BIOCHEMISTRY
影响因子：
--
作者：
Drin, G;Mazel, M;Temsamani, J
通讯作者：
Temsamani, J