Towards understanding cell penetration by stapled peptides

Q Chu, RE Moellering, GJ Hilinski, YW Kim… - …, 2015 - pubs.rsc.org
… As cell penetration is a critical property of stapled peptides, … of stapled peptide properties with
the capacity for cellular uptake… that stapled peptides, including some stapled versions of the …

Enhancing the cell permeability of stapled peptides with a cyclic cell-penetrating peptide

PG Dougherty, J Wen, X Pan, A Koley… - Journal of medicinal …, 2019 - ACS Publications
… to the cell membrane. We show herein that stapled peptides can be rendered highly cell-permeable
by conjugating a cyclic cell-penetrating peptide to their N-terminus, C-terminus, …

Stapled peptides for intracellular drug targets

GL Verdine, GJ Hilinski - Methods in enzymology, 2012 - Elsevier
… to afford high levels of cell penetration, and of those that are cell-penetrant; to our
knowledge, only one has been demonstrated safe and efficacious in vivo. That class, all-hydrocarbon-…

Lactam-stapled cell-penetrating peptides: cell uptake and membrane binding properties

MJ Klein, S Schmidt, P Wadhwani… - Journal of Medicinal …, 2017 - ACS Publications
… Here, we compare four amphiphilic stapled peptides with their linear counterparts in terms
of their membrane binding and conformational features in order to correlate these with uptake …

Development of hydrophobic cell-penetrating stapled peptides as drug carriers

K Tsuchiya, K Horikoshi, M Fujita, M Hirano… - International Journal of …, 2023 - mdpi.com
… helicity and cell penetrating efficiency. … stapled peptide F-3 with CF, in which the stapling
structure was introduced at Gly residues, formed a stable α-helical structure and the highest cell

Stapled peptides—a useful improvement for peptide-based drugs

M Moiola, MG Memeo, P Quadrelli - Molecules, 2019 - mdpi.com
Stapled peptides consist of peptide chains that bring an external brace that force the peptide
… The capacity of cell penetration is directly linked to some peptide properties, such as the …

Biophysical determinants for cellular uptake of hydrocarbon-stapled peptide helices

GH Bird, E Mazzola, K Opoku-Nsiah… - Nature chemical …, 2016 - nature.com
… We envision that implementing these design principles will expedite the advancement of
cell-penetrating stapled peptides with on-mechanism biological and therapeutic activities. …

Hydrocarbon stapled peptides as modulators of biological function

PM Cromm, J Spiegel, TN Grossmann - ACS chemical biology, 2015 - ACS Publications
… (44) So far, strict rules for the implementation of cell permeability have not … cellular uptake
of more than 200 stapled peptides revealed that cell penetration is mainly depending on staple

All-hydrocarbon stapled peptides as synthetic cell-accessible mini-proteins

GL Verdine, GJ Hilinski - Drug Discovery Today: Technologies, 2012 - Elsevier
… atoms, in contrast to all other previously reported designs which bore heteroatoms that
we viewed as probable impediments to efficient cell penetration. The all-hydrocarbon …

Cell permeable stapled peptide inhibitor of Wnt signaling that targets β-catenin protein-protein interactions

L Dietrich, B Rathmer, K Ewan, T Bange, S Heinrichs… - Cell chemical …, 2017 - cell.com
… a stapled peptide inhibitor that targets the interaction between β-catenin and T cell factor/…
learned from cell-penetrating peptide (CPP) design to maximize cellular uptake resulting in …