PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

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 …

Ultrashort all-hydrocarbon stapled α-helix amphiphile as a potent and stable antimicrobial compound

C Shao, Q Jian, B Li, Y Zhu, W Yu, Z Li… - Journal of Medicinal …, 2023 - ACS Publications
The ravaging effect of drug-resistant bacteria has heightened the need for the development
of membrane-soluble antimicrobial peptides (AMPs). However, their potential for clinical use …

A PROTAC peptide induces durable β-catenin degradation and suppresses Wnt-dependent intestinal cancer

H Liao, X Li, L Zhao, Y Wang, X Wang, Y Wu, X Zhou… - Cell discovery, 2020 - nature.com
Aberrant activation of Wnt/β-catenin signaling has been associated with the onset and
progression of many types of tumors and thus β-catenin represents one attractive …

Recent advances in chemical protein synthesis: method developments and biological applications

S Dong, JS Zheng, Y Li, H Wang, G Chen… - Science China …, 2024 - Springer
The central dogma of modern biology underscores the pivotal roles proteins play in diverse
biological processes, the study of which necessitates advanced methods to produce …

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 …

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 …

Targeting intracellular protein–protein interactions with macrocyclic peptides

M Buyanova, D Pei - Trends in pharmacological sciences, 2022 - cell.com
Intracellular protein–protein interactions (PPIs) are challenging targets for traditional drug
modalities. Macrocyclic peptides (MPs) prove highly effective PPI inhibitors in vitro and can …

Cyclobutane-bearing restricted anchoring residues enabled geometry-specific hydrocarbon peptide stapling

B Chen, C Liu, W Cong, F Gao, Y Zou, L Su, L Liu… - Chemical …, 2023 - pubs.rsc.org
Stapled peptides are regarded as the promising next-generation therapeutics because of
their improved secondary structure, membrane permeability and metabolic stability as …

Binary combinatorial scanning reveals potent poly-alanine-substituted inhibitors of protein-protein interactions

X Ye, YC Lee, ZP Gates, Y Ling… - Communications …, 2022 - nature.com
Establishing structure–activity relationships is crucial to understand and optimize the activity
of peptide-based inhibitors of protein–protein interactions. Single alanine substitutions …