Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
A series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective inhibitor having a potency of approximately 2 picomolar was identified. Some of the compounds were examined for their ability to block pancreatic cancer cell growth and found to be about 10-fold more potent than SAHA. This research provides valuable, new molecular probes for use in exploring HDAC biology.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3913184 | PMC |
| http://dx.doi.org/10.1021/jm8002894 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Protective Role of NRG1/ErbB4 Signaling in Myocardial Ischemia-Reperfusion Injury.
J Vis Exp
August 2025
Department of Cardiology, First Hospital of Nanping City affiliated to Fujian Medical University;
Myocardial ischemia-reperfusion injury (MIRI) endures as a substantial impediment to the management of cardiovascular disease. The pathophysiology of MIRI is complex, involving oxidative stress, calcium overload, inflammation, and apoptosis. The NRG1/ErbB4 signaling pathway has been implicated in modulating oxidative stress responses in the heart, potentially reducing cellular damage caused by free radicals.
View Article and Find Full Text PDFPlatinum-group metal half-sandwich complexes of sugar-isoxazol(in)e conjugates - synthesis and evaluation of their antineoplastic and antimicrobial activities.
Eur J Pharm Sci
September 2025
Department of Organic Chemistry, University of Debrecen, P.O. Box 400, H-4002 Debrecen, Hungary. Electronic address:
Platinum-group metal half-sandwich complexes are considered to be potential replacements of the clinically widely used platins which have several side effects and tend to cause resistance to develop. In our previous works, we used a range of 2-pyridyl-substituted N- and C-glycosyl heterocycles as N,N-chelating ligands to prepare ruthenium(II), osmium(II), iridium(III) and rhodium(III) polyhapto arene/arenyl half-sandwich complexes. Some of these complexes, particularly with the C-glucopyranosyl isoxazole derived ligand in its O-perbenzoylated form, exhibited greater anticancer efficiency than cisplatin and had minimal or negligible effects on non-transformed fibroblasts.
View Article and Find Full Text PDFThioester-mediated RNA aminoacylation and peptidyl-RNA synthesis in water.
Nature
August 2025
Department of Chemistry, University College London, London, UK.
To orchestrate ribosomal peptide synthesis, transfer RNAs (tRNAs) must be aminoacylated, with activated amino acids, at their 2',3'-diol moiety, and so the selective aminoacylation of RNA in water is a key challenge that must be resolved to explain the origin of protein biosynthesis. So far, there have been no chemical methods to effectively and selectively aminoacylate RNA-2',3'-diols with the breadth of proteinogenic amino acids in water. Here we demonstrate that (biological) aminoacyl-thiols (1) react selectively with RNA diols over amine nucleophiles, promoting aminoacylation over adventitious (non-coded) peptide bond formation.
View Article and Find Full Text PDFTeriflunomide Inhibits Human FOXP3 Regulatory T Cell Function by Interference With Mitochondrial Respiration.
Eur J Immunol
July 2025
Laboratory of Translational Immunomodulation, VIB Center for Inflammation Research (IRC), Hasselt University, Diepenbeek, Belgium.
Regulatory FOXP3 T cells (Tregs) have been characterized with unique metabolic demands, preferentially relying on fatty acid β-oxidation (FAO) and oxidative phosphorylation (OXPHOS). Several studies have indicated that Treg mitochondrial fitness is crucial for maintaining their stability and suppressive activity with an emphasis on complex-III of the electron transport chain (ETC). Dysfunctional Tregs isolated from patients with autoimmunity like multiple sclerosis (MS) show diminished mitochondrial respiration and the induction of a T helper (Th)1-like phenotype, characterized by increased production of interferon (IFN)-γ.
View Article and Find Full Text PDFGold-Catalyzed Single -Transfer to Internal CF-Alkynes. Regioselective Synthesis of 4-Trifluoromethylated Oxazoles.
J Org Chem
September 2025
Saint Petersburg State University, Universitetskaya Nab. 7/9, 199034 Saint Petersburg, Russian Federation.
A highly regioselective gold-catalyzed single oxygen transfer reaction, involving internal trifluoromethylated alkynes, pyridine -oxides, and nitriles, has been developed. The alkyne-attached CF-moiety functions through an inductive mechanism to direct -nucleophilic attack specifically to the β-alkyne position. This three-component transformation yields a diverse array of valuable 4-trifluoromethylated oxazoles in high yields (30 examples; up to 96%) under relatively mild gold-catalyzed conditions, demonstrating significant tolerance for various functional groups.
View Article and Find Full Text PDF