Lcn2 Promotes Ferroptosis in Intracerebral Hemorrhage by Targeting Keap1 Tyr572 and Restricting Nrf2 Activation. [PDF]
Dou YN +14 more
europepmc +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
IL15.3, a synthetic antimicrobial peptide, attenuates LPS-induced inflammatory responses in RAW 264.7 macrophages via transcriptional and proteomic modulation. [PDF]
Boonmark C +8 more
europepmc +1 more source
Thermodynamic characterisation of covalent ligand binding
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman +4 more
wiley +1 more source
Bidirectional crosstalk between the catalytic and moonlighting functions of human dipeptidyl peptidase 3: potential physiological implications. [PDF]
Matić A +9 more
europepmc +1 more source
Natural Product‐Induced Ferroptosis to Overcome Therapy Resistance in Aggressive Cancers
Natural products trigger ferroptosis through iron overload, glutathione depletion, glutathione peroxidase 4 inhibition, and reactive oxygen species accumulation, selectively targeting aggressive, and drug‐resistant cancers. Polyphenols, alkaloids and terpenoids emerge as promising multi‐target agents to overcome therapy resistance and improve future ...
Giorgio Antoniolli
wiley +1 more source
<i>Caenorhabditis elegans</i> as a Model for Studying Nrf2/SKN-1 Activation in Alzheimer's Disease: Plant Bioactive Compounds and Therapeutic Translation. [PDF]
Bellver-Sanchis A +6 more
europepmc +1 more source
Hybrid macrocyclic peptides unite genetically encoded peptide libraries with the structural complexity of synthetic small molecules. This Review critically analyzes phage‐compatible cyclization and diversification chemistries, highlights emerging opportunities beyond traditional cysteine‐based approaches, and outlines how future advances may enable the
Titia Rixt Oppewal, Clemens Mayer
wiley +1 more source
The Discovery of GSK3227634: A Potent Inhaled Inhibitor of the KEAP1/NRF2 Protein-Protein Interaction for the Treatment of Chronic Obstructive Pulmonary Disease. [PDF]
Callahan JF +36 more
europepmc +1 more source

