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Drug discovery targeting amino acid racemases.
Drug Discovery Targeting Amino Acid Racemases Paola Conti, Lucia Tamborini, Andrea Pinto, Arnaud Blondel, Paola Minoprio, Andrea Mozzarelli, and Carlo De Micheli* Dipartimento di Scienze…
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors.
- S. Castellano, D. Kuck, G. Sbardella
- Chemistry, BiologyJournal of medicinal chemistry
- 1 September 2010
A series of Δ(2)-isoxazoline constrained analogues of procaine/procainamide (7a-k and 8a-k) were prepared and their inhibitory activity against DNA methyltransferase 1 (DNMT1) was tested. Among them,…
The Glial Glutamate Transporter 1 (GLT1) Is Expressed by Pancreatic β-Cells and Prevents Glutamate-induced β-Cell Death*
The present study identifies GLT1 as a new player in glutamate homeostasis and signaling in the islet of Langerhans and demonstrates that β-cells critically depend on its activity to control extracellular glutamate levels and cellular integrity.
Mutant p53 prevents GAPDH nuclear translocation in pancreatic cancer cells favoring glycolysis and 2-deoxyglucose sensitivity.
Marine Microorganisms as Source of Stereoselective Esterases and Ketoreductases: Kinetic Resolution of a Prostaglandin Intermediate
A screening among bacterial strains isolated from water-brine interface of the deep hypersaline anoxic basins of the Eastern Mediterranean was carried out for the biocatalytical resolution of racemic propyl ester of anti-2-oxotricyclo (R,S)-1, a key intermediate for the synthesis of d-cloprostenol.
Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors.
Inspired by Nature: The 3‐Halo‐4,5‐dihydroisoxazole Moiety as a Novel Molecular Warhead for the Design of Covalent Inhibitors
It is shown that the 3‐halo‐4,5‐dihydroisoxazole moiety represents an outstanding warhead with high potential for the design of novel covalent enzyme inhibitors.
Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M.