Stapled helical peptides bearing different anchoring residues

X Li, S Chen, WD Zhang, HG Hu - Chemical Reviews, 2020 - ACS Publications
A large proportion of protein–protein interactions (PPIs) occur between a short peptide and a
globular protein domain; the peptides involved in surface interactions play important roles …

Structure‐based design of inhibitors of protein–protein interactions: mimicking peptide binding epitopes

M Pelay‐Gimeno, A Glas, O Koch… - Angewandte Chemie …, 2015 - Wiley Online Library
Protein–protein interactions (PPIs) are involved at all levels of cellular organization, thus
making the development of PPI inhibitors extremely valuable. The identification of selective …

Design of stapled antimicrobial peptides that are stable, nontoxic and kill antibiotic-resistant bacteria in mice

R Mourtada, HD Herce, DJ Yin, JA Moroco… - Nature …, 2019 - nature.com
The clinical translation of cationic α-helical antimicrobial peptides (AMPs) has been
hindered by structural instability, proteolytic degradation and in vivo toxicity from nonspecific …

New modalities for challenging targets in drug discovery

E Valeur, SM Guéret, H Adihou… - Angewandte Chemie …, 2017 - Wiley Online Library
Our ever‐increasing understanding of biological systems is providing a range of exciting
novel biological targets, whose modulation may enable novel therapeutic options for many …

Hydrocarbon stapled peptides as modulators of biological function

PM Cromm, J Spiegel, TN Grossmann - ACS chemical biology, 2015 - ACS Publications
Peptide-based drug discovery has experienced a significant upturn within the past decade
since the introduction of chemical modifications and unnatural amino acids has allowed for …

Biophysical determinants for cellular uptake of hydrocarbon-stapled peptide helices

GH Bird, E Mazzola, K Opoku-Nsiah… - Nature chemical …, 2016 - nature.com
Hydrocarbon-stapled peptides are a class of bioactive alpha-helical ligands developed to
dissect and target protein interactions. While there is consensus that stapled peptides can …

Strukturbasierte Entwicklung von Protein‐Protein‐Interaktionsinhibitoren: Stabilisierung und Nachahmung von Peptidliganden

M Pelay‐Gimeno, A Glas, O Koch… - Angewandte …, 2015 - Wiley Online Library
Abstract Protein‐Protein‐Interaktionen (PPIs) spielen auf allen Ebenen der Zellorganisation
eine wichtige Rolle, was die Entwicklung von PPI‐Inhibitoren äußerst interessant macht. Die …

Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices

ES Leshchiner, A Parkhitko, GH Bird… - Proceedings of the …, 2015 - National Acad Sciences
Activating mutations in the Kirsten rat sarcoma viral oncogene homolog (KRAS) underlie the
pathogenesis and chemoresistance of∼ 30% of all human tumors, yet the development of …

Stitched α-helical peptides via bis ring-closing metathesis

GJ Hilinski, YW Kim, J Hong… - Journal of the …, 2014 - ACS Publications
Conformationally stabilized α-helical peptides are capable of inhibiting disease-relevant
intracellular or extracellular protein–protein interactions in vivo. We have previously reported …

Stapled peptide design: principles and roles of computation

YS Tan, DP Lane, CS Verma - Drug Discovery Today, 2016 - Elsevier
Highlights•One of the most widely adopted strategies for α-helix stabilisation is peptide
stapling.•Stapled peptides are highly promising therapeutic agents.•General design …