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 …

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 …

Multicomponent reaction toolbox for peptide macrocyclization and stapling

L Reguera, DG Rivera - Chemical reviews, 2019 - ACS Publications
In the past decade, multicomponent reactions have experienced a renaissance as powerful
peptide macrocyclization tools enabling the rapid creation of skeletal complexity and …

Peptide stapling techniques based on different macrocyclisation chemistries

YH Lau, P De Andrade, Y Wu, DR Spring - Chemical Society Reviews, 2015 - pubs.rsc.org
Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical
conformation. Stapling is carried out by covalently linking the side-chains of two amino …

Chemical protein modification through cysteine

SB Gunnoo, A Madder - ChemBioChem, 2016 - Wiley Online Library
The modification of proteins with non‐protein entities is important for a wealth of
applications, and methods for chemically modifying proteins attract considerable attention …

Inhibition of α-helix-mediated protein–protein interactions using designed molecules

V Azzarito, K Long, NS Murphy, AJ Wilson - Nature chemistry, 2013 - nature.com
Inhibition of protein–protein interactions (PPIs) represents a significant challenge because it
is unclear how they can be effectively and selectively targeted using small molecules …

Constraining cyclic peptides to mimic protein structure motifs

TA Hill, NE Shepherd, F Diness… - Angewandte Chemie …, 2014 - Wiley Online Library
Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …

Modulators of protein–protein interactions

LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Peptide therapeutics: targeting the undruggable space

N Tsomaia - European journal of medicinal chemistry, 2015 - Elsevier
Rapid advancements in genomics have brought a better understanding of molecular
mechanisms for various pathologies and identified a number of highly attractive target …