Improved cytosolic delivery of macromolecules through dimerization of attenuated lytic peptides.

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.
PMID: 32738963 [PubMed - in process]

Source: Bioorganic and Medicinal Chemistry Letters - August 4, 2020 Category: Chemistry Authors: Nomura Y, Sakamoto K, Akishiba M, Iwata T, Hirose H, Futaki S Tags: Bioorg Med Chem Lett Source Type: research