Peptidomimetics: an overview of recent medicinal chemistry efforts toward the discovery of novel small molecule inhibitors

G Li Petri, S Di Martino, M De Rosa - Journal of Medicinal …, 2022 - ACS Publications
The use of peptides as therapeutics has often been associated with several drawbacks such
as poor absorption, low stability to proteolytic digestion, and fast clearance. Peptidomimetics …

Rational design of peptide-based inhibitors disrupting protein-protein interactions

X Wang, D Ni, Y Liu, S Lu - Frontiers in chemistry, 2021 - frontiersin.org
Protein-protein interactions (PPIs) are well-established as a class of promising drug targets
for their implications in a wide range of biological processes. However, drug development …

Cyclic Peptide Screening Methods for Preclinical Drug Discovery: Miniperspective

X Li, TW Craven, PM Levine - Journal of Medicinal Chemistry, 2022 - ACS Publications
Cyclic peptides are among the most diverse architectures for current drug discovery efforts.
Their size, stability, and ease of synthesis provide attractive scaffolds to engage and …

Chemical synthesis of bioactive proteins

O Harel, M Jbara - Angewandte Chemie, 2023 - Wiley Online Library
Nature has developed a plethora of protein machinery to operate and maintain nearly every
task of cellular life. These processes are tightly regulated via post‐expression modifications …

Selective thiazoline peptide cyclisation compatible with mRNA display and efficient synthesis

M Liu, R Morewood, R Yoshisada, MN Pascha… - Chemical …, 2023 - pubs.rsc.org
Peptide display technologies are a powerful method for discovery of new bioactive
sequences, but linear sequences are often very unstable in a biological setting …

Peptide‐based covalent inhibitors of protein–protein interactions

FM Paulussen, TN Grossmann - Journal of Peptide Science, 2023 - Wiley Online Library
Protein–protein interactions (PPI) are involved in all cellular processes and many represent
attractive therapeutic targets. However, the frequently rather flat and large interaction areas …

Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets

K Colas, D Bindl, H Suga - Chemical Reviews, 2024 - ACS Publications
Technological advances and breakthrough developments in the pharmaceutical field are
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …

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 …

Covalent proteomimetic inhibitor of the bacterial FtsQB divisome complex

FM Paulussen, GK Schouten, C Moertl… - Journal of the …, 2022 - ACS Publications
The use of antibiotics is threatened by the emergence and spread of multidrug-resistant
strains of bacteria. Thus, there is a need to develop antibiotics that address new targets. In …

Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics

CS Swenson, G Mandava, DM Thomas… - Chemical …, 2024 - ACS Publications
The development of potent, specific, and pharmacologically viable chemical probes and
therapeutics is a central focus of chemical biology and therapeutic development. However, a …