Efficient Cellular Delivery of 尾-Galactosidase Mediated by NrTPs, a New Family of Cell-Penetrating Peptides

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• 作者：Margarida Rodrigues ; Beatriz G. de la Torre ; Gandhi R谩dis-Baptista ; Nuno C. Santos ; David Andreu
• 刊名：Bioconjugate Chemistry
• 出版年：2011
• 出版时间：November 16, 2011
• 年：2011
• 卷：22
• 期：11
• 页码：2339-2344
• 全文大小：273K
• 年卷期：v.22,no.11(November 16, 2011)
• ISSN：1520-4812

文摘

Nucleolar targeting peptides (NrTPs), a recently developed family of cell-penetrating peptides, have been shown to be very efficient in entering cells and accumulating in their nucleoli. In this work, we have used conjugates of NrTP6 (YKQSHKKGGKKGSG) covalently linked to 尾-galactosidase in order to demonstrate the capacity of NrTP for intracellular delivery of large molecules. NrTP6/尾-galactosidase conjugates, prepared by maleimide-based chemistry, were stable and enzymatically active on the standard 4-methylumbelliferyl 尾-d-galactopyranoside substrate. Their translocation into HeLa cells, monitored by 尾-galactosidase activity as a readout of the uptake, showed efficient cellular entry and thus demonstrated the potential of NrTPs for intracellular delivery of large-size cargos with preservation of biological activity.