Intracellular delivery of biomacromolecules is a challenging research field in chemical biology and drug delivery. We previously reported a peptide named L17E, which successfully delivered functional proteins, including antibodies, into cells. However, relatively high concentrations of L17E and proteins are needed. In this study, we prepared dimers of L17E and its analog L17E/Q21E. Dimerization of L17E increased cytotoxicity leading to reduced intracellular delivery compared with L17E. On the other hand, the dimers of the L17E analog, L17E/Q21E, especially when tethered at the N-termini, yielded a comparable level of intracellular delivery with L17E at decreased amounts of delivery peptides and cargoes.

生物大分子的细胞内递送是化学生物学和药物递送中具有挑战性的研究领域。我们之前曾报道过一种名为L17E的肽，它可以将包括抗体在内的功能蛋白成功地传递到细胞中。但是，需要相对较高浓度的L17E和蛋白质。在这项研究中，我们制备了L17E及其类似物L17E / Q21E的二聚体。与L17E相比，L17E的二聚化增加了细胞毒性，导致细胞内递送减少。另一方面，L17E类似物L17E / Q21E的二聚体，特别是当在N末端连接时，产生了与L17E相当的细胞内递送水平，但递送肽和货物的量减少了。