Macrocyclic peptides as drug candidates: recent progress and remaining challenges

AA Vinogradov, Y Yin, H Suga - Journal of the American Chemical …, 2019 - ACS Publications
Peptides as a therapeutic modality attract much attention due to their synthetic accessibility,
high degree of specific binding, and the ability to target protein surfaces traditionally …

The current state of peptide drug discovery: back to the future?

A Henninot, JC Collins, JM Nuss - Journal of medicinal chemistry, 2018 - ACS Publications
Over the past decade, peptide drug discovery has experienced a revival of interest and
scientific momentum, as the pharmaceutical industry has come to appreciate the role that …

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 …

Macrocyclization strategies for cyclic peptides and peptidomimetics

C Bechtler, C Lamers - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

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 …

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 …

Orally absorbed cyclic peptides

DS Nielsen, NE Shepherd, W Xu, AJ Lucke… - Chemical …, 2017 - ACS Publications
Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …

Inhibition of calcium-triggered secretion by hydrocarbon-stapled peptides

Y Lai, G Fois, JR Flores, MJ Tuvim, Q Zhou, K Yang… - Nature, 2022 - nature.com
Membrane fusion triggered by Ca2+ is orchestrated by a conserved set of proteins to
mediate synaptic neurotransmitter release, mucin secretion and other regulated exocytic …

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: principles, practice, and progress: miniperspective

LD Walensky, GH Bird - Journal of medicinal chemistry, 2014 - ACS Publications
Protein structure underlies essential biological processes and provides a blueprint for
molecular mimicry that drives drug discovery. Although small molecules represent the lion's …