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 …
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 …
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 …
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
Macrocyclic peptides represent attractive scaffolds for targeting protein–protein interactions,
making methods for the diversification and functional selection of these molecules highly …
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
Conspectus Chemical manipulation of naturally occurring peptides offers a convenient route
for generating analogs to screen against different therapeutic targets. However, the limited …
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 …
protein 1 (MRP1), protect against cellular toxicity by exporting xenobiotic compounds across …
In Vitro Selection of Peptides and Proteins—Advantages of mRNA Display
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 …
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 …
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
Glycosyltransferases are a superfamily of enzymes that are notoriously difficult to inhibit.
Here we apply an mRNA display technology integrated with genetic code reprogramming …
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 …
mortality, and disruption globally. Cellular entry of SARS-CoV-2 is mediated by the viral …