Understanding cell penetration of cyclic peptides
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …
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 …
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 …
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 …
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 …
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 …
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
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 …
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 …
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
The development of inhibitors that selectively block protein–protein interactions (PPIs) is
crucial for chemical biology, medicinal chemistry, and biomedical sciences. Herein, we …
crucial for chemical biology, medicinal chemistry, and biomedical sciences. Herein, we …
Targeting intracellular protein–protein interactions with cell-permeable cyclic peptides
Highlights•Cyclic peptides are an emerging class of drug modality for PPI
inhibition.•Rational design and library screening are established to generate lead …
inhibition.•Rational design and library screening are established to generate lead …