Understanding cell penetration of cyclic peptides

PG Dougherty, A Sahni, D Pei - Chemical Reviews, 2019 - ACS Publications
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

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 …

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 …

Advances in developing ACE2 derivatives against SARS-CoV-2

H Zhang, P Lv, J Jiang, Y Liu, R Yan, S Shu… - The Lancet …, 2023 - thelancet.com
Extensive immune evasion of SARS-CoV-2 rendered therapeutic antibodies ineffective in
the COVID-19 pandemic. Propagating SARS-CoV-2 variants are characterised by immune …

Strategies for the diversity-oriented synthesis of macrocycles

KT Mortensen, TJ Osberger, TA King, HF Sore… - Chemical …, 2019 - ACS Publications
Macrocycles have long been recognized as useful chemical entities for medicine, with
naturally occurring and synthetic macrocycles clinically approved for use as prescription …

Peptide-based inhibitors of protein–protein interactions: biophysical, structural and cellular consequences of introducing a constraint

H Wang, RS Dawber, P Zhang, M Walko, AJ Wilson… - Chemical …, 2021 - pubs.rsc.org
Protein–protein interactions (PPIs) are implicated in the majority of cellular processes by
enabling and regulating the function of individual proteins. Thus, PPIs represent high-value …

Cys–Cys and Cys–Lys stapling of unprotected peptides enabled by hypervalent iodine reagents

J Ceballos, E Grinhagena, G Sangouard… - Angewandte …, 2021 - Wiley Online Library
Easy access to a wide range of structurally diverse stapled peptides is crucial for the
development of inhibitors of protein‐protein interactions. Herein, we report bis‐functional …

Stapled Peptides Based on Human Angiotensin-Converting Enzyme 2 (ACE2) Potently Inhibit SARS-CoV-2 Infection In Vitro

F Curreli, SMB Victor, S Ahmed, A Drelich, X Tong… - MBio, 2020 - Am Soc Microbiol
ABSTRACT SARS-CoV-2 uses human angiotensin-converting enzyme 2 (ACE2) as the
primary receptor to enter host cells and initiate the infection. The critical binding region of …

Photo-induced radical thiol–ene chemistry: a versatile toolbox for peptide-based drug design

M Ahangarpour, I Kavianinia, PWR Harris… - Chemical Society …, 2021 - pubs.rsc.org
While the global market for peptide/protein-based therapeutics is witnessing significant
growth, the development of peptide drugs remains challenging due to their low oral …