Improved cytosolic delivery of macromolecules through dimerization of attenuated lytic peptides

Yohei Nomura, Kentarou Sakamoto, Misao Akishiba, Takahiro Iwata, Hisaaki Hirose, Shiroh Futaki

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

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.

Original languageEnglish
Article number127362
JournalBioorganic and Medicinal Chemistry Letters
Volume30
Issue number17
DOIs
Publication statusPublished - Sep 1 2020
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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