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Exploring the Ascorbate Requirement of the 2-Oxoglutarate-Dependent Dioxygenases.
J Med Chem
January 2025
Ma̅tai Ha̅ora - Centre for Redox Biology and Medicine, Department of Biomedical Science and Pathology, University of Otago, Christchurch, Christchurch 8140, New Zealand.
In humans, the 2-oxoglutarate-dependent dioxygenases (2-OGDDs) catalyze hydroxylation reactions involved in cell metabolism, the biosynthesis of small molecules, DNA and RNA demethylation, the hypoxic response and the formation of collagen. The reaction is catalyzed by a highly oxidizing ferryl-oxo species produced when the active site non-heme iron engages molecular oxygen. Enzyme activity is specifically stimulated by l-ascorbic acid (ascorbate, vitamin C), an effect not well mimicked by other reducing agents.
View Article and Find Full Text PDFDiscovery, Optimization, and Preclinical Pharmacology of EP652, a METTL3 Inhibitor with Efficacy in Liquid and Solid Tumor Models.
J Med Chem
January 2025
Epics Therapeutics SA, rue Adrienne Bolland 47, Gosselies 6041, Belgium.
METTL3 is the RNA methyltransferase predominantly responsible for the addition of N-methyladenosine (mA), the most abundant modification to mRNA. The prevalence of mA and the activity and expression of METTL3 have been linked to the appearance and progression of acute myeloid leukemia (AML), thereby making METTL3 an attractive target for cancer therapeutics. We report herein the discovery and optimization of small-molecule inhibitors of METTL3, culminating in the selection of as an proof-of-concept compound.
View Article and Find Full Text PDFNexinhib20 inhibits JFC1-mediated mobilization of a subset of CD11b/CD18+ vesicles decreasing integrin avidity, but does not inhibit Rac1.
J Leukoc Biol
January 2025
Department of Molecular and Cellular Biology, The Scripps Research Institute, La Jolla, CA.
Regulated sequential exocytosis of neutrophil granules is essential in orchestrating the innate immune response, while uncontrolled secretion causes inflammation. We developed and characterized Nexinhib20, a small-molecule inhibitor that targets azurophilic granule exocytosis in neutrophils by blocking the interaction between the small GTPase Rab27a and its effector JFC1. Its therapeutic potential has been demonstrated in several pre-clinical models of inflammatory disease.
View Article and Find Full Text PDFUnveiling the Promoting Effects of Zr and the Hydrothermal Treatment on the NH-SCR Activity of the Cu-SAPO-18 Catalyst.
Environ Sci Technol
January 2025
State Key Laboratory of Chemical Resource Engineering, Beijing University of Chemical Technology, Beijing 100029, China.
Selective catalytic reduction of NO by NH(NH-SCR) remains challenging for diesel vehicles due to the complex exhaust condition. Cu-SAPO-18 zeolite has emerged as an efficient catalyst for the NH-SCR process, attributed to its unique small pore configuration and high NH-SCR activity. Herein, Zr-modified Cu-SAPO-18 has been fabricated and evaluated for the reduction of NO.
View Article and Find Full Text PDFNondeterministic dynamics in the η-to-θ phase transition of alumina nanoparticles.
Science
January 2025
Department of Chemistry, The University of Tokyo, Bunkyo-ku, Tokyo, Japan.
Phase diagrams and crystallography are standard tools for studying structural phase transitions, whereas acquiring kinetic information at the atomistic level has been considered essential but challenging. The η-to-θ phase transition of alumina is unidirectional in bulk and retains the crystal lattice orientation. We report a rare example of a statistical kinetics study showing that for nanoparticles on a bulk Al(OH) surface, this phase transition occurs nondeterministically through an ergodic equilibrium through the molten state, and the memory of the lattice orientation is lost in this process.
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