E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

The RaPID platform for the discovery of pseudo-natural macrocyclic peptides

Y Goto, H Suga - Accounts of Chemical Research, 2021 - ACS Publications
Conspectus Although macrocyclic peptides bearing exotic building blocks have proven their
utility as pharmaceuticals, the sources of macrocyclic peptide drugs have been largely …

A gold mine for drug discovery: Strategies to develop cyclic peptides into therapies

X Jing, K Jin - Medicinal research reviews, 2020 - Wiley Online Library
As a versatile therapeutic modality, peptides attract much attention because of their great
binding affinity, low toxicity, and the capability of targeting traditionally “undruggable” protein …

MOrPH-PhD: an integrated phage display platform for the discovery of functional genetically encoded peptide macrocycles

AE Owens, JA Iannuzzelli, Y Gu, R Fasan - ACS central science, 2020 - ACS Publications
Macrocyclic peptides represent attractive scaffolds for targeting protein–protein interactions,
making methods for the diversification and functional selection of these molecules highly …

Combining Chemical Protein Synthesis and Random Nonstandard Peptides Integrated Discovery for Modulating Biological Processes

A Saha, H Suga, A Brik - Accounts of Chemical Research, 2023 - ACS Publications
Conspectus Chemical manipulation of naturally occurring peptides offers a convenient route
for generating analogs to screen against different therapeutic targets. However, the limited …

A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation

HL Pietz, A Abbas, ZL Johnson… - Proceedings of the …, 2023 - National Acad Sciences
Adenosine triphosphate-binding cassette (ABC) transporters, such as multidrug resistance
protein 1 (MRP1), protect against cellular toxicity by exporting xenobiotic compounds across …

In Vitro Selection of Peptides and Proteins—Advantages of mRNA Display

MS Newton, Y Cabezas-Perusse, CL Tong… - ACS synthetic …, 2019 - ACS Publications
mRNA display is a robust in vitro selection technique that allows the selection of peptides
and proteins with desired functions from libraries of trillions of variants. mRNA display relies …

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 …

Potent de novo macrocyclic peptides that inhibit O‐GlcNAc transferase through an allosteric mechanism

MG Alteen, H Peacock, RW Meek… - Angewandte Chemie …, 2023 - Wiley Online Library
Glycosyltransferases are a superfamily of enzymes that are notoriously difficult to inhibit.
Here we apply an mRNA display technology integrated with genetic code reprogramming …

Discovery of cyclic peptide ligands to the SARS-CoV-2 spike protein using mRNA display

A Norman, C Franck, M Christie… - ACS Central …, 2021 - ACS Publications
The COVID-19 pandemic, caused by SARS-CoV-2, has led to substantial morbidity,
mortality, and disruption globally. Cellular entry of SARS-CoV-2 is mediated by the viral …