Multimeric Amphipathic α-Helical Sequences for Rapid and Efficient Intracellular Protein Transport at Nanomolar Concentrations.

ABSTRACT: An amphipathic leucine (L) and lysine (K)-rich α-helical peptide is multimerized based on helix-loop-helix structures to maximize the penetrating activities. The multimeric LK-based cell penetrating peptides (LK-CPPs) can penetrate cells as protein-fused forms at 100-1000-fold lower concentrations than Tat peptide. The enhanced penetrating activity is increased through multimerization by degrees up to the tetramer level. The multimeric LK-CPPs show rapid cell penetration through macropinocytosis at low nanomolar concentrations, unlike the monomeric LK, which have slower penetrating kinetics at much higher concentrations. The heparan sulfate proteoglycan (HSPG) receptors are highly involved in the rapid internalization of multimeric LK-CPPs. As a proof of concept of biomedical applications,

SUBMITTER: Oh JH 

PROVIDER: S-EPMC6096998 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature