Ruthenium-catalyzed azide alkyne cycloaddition reaction: scope, mechanism, and applications

JR Johansson, T Beke-Somfai… - Chemical …, 2016 - ACS Publications
The ruthenium-catalyzed azide alkyne cycloaddition (RuAAC) affords 1, 5-disubstituted 1, 2,
3-triazoles in one step and complements the more established copper-catalyzed reaction …

Inhibition of protein–protein interactions using designed molecules

AJ Wilson - Chemical Society Reviews, 2009 - pubs.rsc.org
Although many cellular processes depend upon enzymatic reactions, protein–protein
interactions (PPIs) mediate a large number of important regulatory pathways and thus play a …

Sulfono-γ-AApeptides as helical mimetics: Crystal structures and applications

P Sang, Y Shi, B Huang, S Xue, T Odom… - Accounts of chemical …, 2020 - ACS Publications
Conspectus Foldamers have defined and predictable structures, improved resistance to
proteolytic degradation, enhanced chemical diversity, and are versatile in their mimicry of …

Pseudo-isolated α-helix platform for the recognition of deep and narrow targets

D Kim, S Han, H Park, S Choi, M Kaur… - Journal of the …, 2022 - ACS Publications
Although interest in stabilized α-helical peptides as next-generation therapeutics for
modulating biomolecular interfaces is increasing, peptides have limited functionality and …

α-Helix-mimicking sulfono-γ-AApeptide inhibitors for p53–MDM2/MDMX protein–protein interactions

P Sang, Y Shi, J Lu, L Chen, L Yang… - Journal of medicinal …, 2020 - ACS Publications
The use of peptidomimetic scaffolds is a promising strategy for the inhibition of protein–
protein interactions (PPIs). Herein, we demonstrate that sulfono-γ-AApeptides can be …

Enhancements of screening collections to address areas of unmet medical need: an industry perspective

DH Drewry, R Macarron - Current opinion in chemical biology, 2010 - Elsevier
The past 20 years have witnessed an impressive expansion of the 'drug space'; defined as
the intersection of the Medicinal Chemistry space and the Biologically Active space relevant …

Peptidomimetic-based vesicles inhibit amyloid-β fibrillation and attenuate cytotoxicity

D Maity, M Howarth, MC Vogel… - Journal of the …, 2021 - ACS Publications
An interruption in Aβ homeostasis leads to the deposit of neurotoxic amyloid plaques and is
associated with Alzheimer's disease. A supramolecular strategy based on the assembly of …

Selective and potent proteomimetic inhibitors of intracellular protein–protein interactions

A Barnard, K Long, HL Martin, JA Miles… - Angewandte …, 2015 - Wiley Online Library
Inhibition of protein–protein interactions (PPIs) represents a major challenge in chemical
biology and drug discovery. α‐Helix mediated PPIs may be amenable to modulation using …

Discovery of leukotriene A4 hydrolase inhibitors using metabolomics biased fragment crystallography

DR Davies, B Mamat, OT Magnusson… - Journal of medicinal …, 2009 - ACS Publications
We describe a novel fragment library termed fragments of life (FOL) for structure-based drug
discovery. The FOL library includes natural small molecules of life, derivatives thereof, and …

Surfing the protein-protein interaction surface using docking methods: application to the design of PPI inhibitors

R Sable, S Jois - Molecules, 2015 - mdpi.com
Blocking protein-protein interactions (PPI) using small molecules or peptides modulates
biochemical pathways and has therapeutic significance. PPI inhibition for designing drug …