Antiradical, Chelating and Antioxidant Activities of Hydroxamic Acids and Hydroxyureas
Reactive oxygen species, along with reactive nitrogen species, may play an important role in the pathogenesis and progress of many diseases, including cancer, diabetes and sickle cell disease.
Branka Zorc +3 more
doaj +1 more source
Histone deacetylase inhibitors induce invasion of human melanoma cells in vitro via differential regulation of N-cadherin expression and RhoA activity [PDF]
Background: Histone deacetylase inhibitors (HDACi) exert multiple cytotoxic actions on cancer cells. Currently, different synthetic HDACi are in clinical use or clinical trials; nevertheless, since both pro-invasive and anti-invasive activities have been
Andrade, Ricardo +6 more
core +4 more sources
Pharmacological Effects of Anthranilic Hydroxamic Acid and Certain Other Hydroxamic Acids
SummaryThe hydroxamate of anthranilic acid injected intraperitoneally into rats in a dose of 1.0 mg/g causes anesthesia lasting 10 hours or more. Recovery is apparently complete. One half this dose causes tranquilization and suppression of the conditioned avoidance response. The compound protects mice against twice the lethal dose of strychnine.
F. Bernheim, J. K. Stoops
openaire +1 more source
Inhibitors of insulin‐degrading enzyme boost PI cytotoxicity through an increased sensitivity of proteasome to PI inhibitors, induction of ISR, DNA damage and Myc down‐regulation. They overcome PI resistance in vitro and induce tumour regression in vivo.
Laetitia Lesire +28 more
wiley +1 more source
Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors [PDF]
Plasmodium parasites, the causative agents of malaria, have developed resistance to most of our current antimalarial therapies, including artemisinin combination therapies which are widely described as our last line of defense. Antimalarial agents with a
Abdel-Magid A. F. +79 more
core +4 more sources
Chemical Ligation of Backbone N‐hydroxylated Peptides
Peptide backbone N‐hydroxylation enables sequence‐agnostic fragment ligation via hydroxamate O‐acyl capture and O→N acyl transfer in water. Broad tolerance of sterically demanding nucleophilic residues is observed, and reductive N─O cleavage restores the native amide bond.
Natalia Cano‐Sampaio +1 more
wiley +1 more source
Carbamates as Potential Prodrugs and a New Warhead for HDAC Inhibition
We designed and synthesized carbamates of the clinically-approved HDAC (histone deacetylase) inhibitor vorinostat (suberoylanilide hydroxamic acid, SAHA) in order to validate our previously-proposed hypothesis that these carbamates might serve as ...
Kristina King +4 more
doaj +1 more source
Regulated Cell Death in Idiopathic Pulmonary Fibrosis
This graphical abstract illustrates regulated cell death (RCD) across key pulmonary cell types—including alveolar epithelial cells, fibroblasts, macrophages, and endothelial cells—modulated through a dynamic death modulation network within the IPF microenvironment.
Xiaoyue Pan +10 more
wiley +1 more source
Trichostatin A (TSA) and suberoylanilide hydroxamic acid (SAHA) were reported in our recent publication as novel human high density lipoprotein (HDL) receptor CD36 and Lysosomal integral membrane protein-II Analogous-1 (CLA-1) up-regulators. As part of a
Yu Du +6 more
doaj +1 more source
Contemporary Applications of Chemical Libraries for Drug Discovery and Methods for Their Synthesis
Screening of chemical libraries has over the past decades become a cornerstone of drug discovery. Today, a broad range of chemical libraries exist but they are often not well described in terms of diversity. This review describes current efforts which aim to visualize chemical diversity in compound collections and discuss current trends in synthetic ...
Tobias N. Hansen, Nils J. V. Hansen
wiley +1 more source

