Understanding cell penetration of cyclic peptides

PG Dougherty, A Sahni, D Pei - Chemical Reviews, 2019 - ACS Publications
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

New modalities for challenging targets in drug discovery

E Valeur, SM Guéret, H Adihou… - Angewandte Chemie …, 2017 - Wiley Online Library
Our ever‐increasing understanding of biological systems is providing a range of exciting
novel biological targets, whose modulation may enable novel therapeutic options for many …

Functions of the aryl hydrocarbon receptor (AHR) beyond the canonical AHR/ARNT signaling pathway

NC Sondermann, S Faßbender, F Hartung… - Biochemical …, 2023 - Elsevier
The aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor regulating
adaptive and maladaptive responses toward exogenous and endogenous signals …

Modulating protein–protein interactions: the potential of peptides

L Nevola, E Giralt - Chemical Communications, 2015 - pubs.rsc.org
Protein–protein interactions (PPIs) have emerged as important and challenging targets in
chemical biology and medicinal chemistry. The main difficulty encountered in the discovery …

Cyclic and macrocyclic peptides as chemical tools to recognise protein surfaces and probe protein–protein interactions

TAF Cardote, A Ciulli - ChemMedChem, 2016 - Wiley Online Library
Targeting protein surfaces and protein–protein interactions (PPIs) with small molecules is a
frontier goal of chemical biology and provides attractive therapeutic opportunities in drug …

HIF-1α and PFKFB3 mediate a tight relationship between proinflammatory activation and anerobic metabolism in atherosclerotic macrophages

A Tawakol, P Singh, M Mojena… - … , and vascular biology, 2015 - Am Heart Assoc
Objective—Although it is accepted that macrophage glycolysis is upregulated under hypoxic
conditions, it is not known whether this is linked to a similar increase in macrophage …

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 …

SICLOPPS cyclic peptide libraries in drug discovery

A Tavassoli - Current Opinion in Chemical Biology, 2017 - Elsevier
Highlights•SICLOPPS allows the rapid generation of cyclic peptide libraries in cells.•A
variety of cyclic peptide ring sizes may be generated with SICLOPPS.•SICLOPPS libraries …

Inhibition of hypoxia-inducible transcription factor (HIF-1α) signaling with sulfonyl-γ-AApeptide helices

W Jiang, S Abdulkadir, X Zhao, P Sang… - Journal of the …, 2023 - ACS Publications
The development of inhibitors that selectively block protein–protein interactions (PPIs) is
crucial for chemical biology, medicinal chemistry, and biomedical sciences. Herein, we …

Targeting intracellular protein–protein interactions with cell-permeable cyclic peptides

Z Qian, PG Dougherty, D Pei - Current opinion in chemical biology, 2017 - Elsevier
Highlights•Cyclic peptides are an emerging class of drug modality for PPI
inhibition.•Rational design and library screening are established to generate lead …