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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 ScienzeExpand
Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors.
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,Expand
Flow-based stereoselective reduction of ketones using an immobilized ketoreductase/glucose dehydrogenase mixed bed system
A robust two-enzyme system composed of an immobilized ketoreductase (KRED1-Pglu) and a glucose dehydrogenase (BmGDH) was developed via immobilization on aldehyde agarose for the stereoselectiveExpand
Marine Microorganisms as Source of Stereoselective Esterases and Ketoreductases: Kinetic Resolution of a Prostaglandin Intermediate
TLDR
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. Expand
Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors.
TLDR
Following the concept that increasing the molecular complexity may enhance the receptor selectivity, the model compound tricholomic acid was replaced with a 3-hydroxy-pyrazoline ring, which could be variously decorated at the N1 position, inserting groups characterized by different electronic and steric properties. Expand
Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M.
TLDR
In in vivo tests non-quaternary compounds were able to evoke central muscarinic effects, with a potency order parallel to that observed in vitro. Expand
The Glial Glutamate Transporter 1 (GLT1) Is Expressed by Pancreatic β-Cells and Prevents Glutamate-induced β-Cell Death*
TLDR
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. Expand
UCP2 inhibition induces ROS/Akt/mTOR axis: Role of GAPDH nuclear translocation in genipin/everolimus anticancer synergism
TLDR
It is demonstrated that inhibition of UCP2 triggers Akt/mTOR pathway in a ROS‐dependent mechanism in pancreatic adenocarcinoma cells, creating the conditions for the synergistic counteraction of cancer cell growth with the mTOR inhibitor everolimus. Expand
Mutant p53 prevents GAPDH nuclear translocation in pancreatic cancer cells favoring glycolysis and 2-deoxyglucose sensitivity.
TLDR
It is demonstrated that mutant p53 prevents the nuclear translocation of the glycolytic enzyme glyceraldehyde-3-phosphate dehydrogenase (GAPDH) stabilizing its cytoplasmic localization, thus supporting glycoleysis of cancer cells and inhibiting cell death mechanisms mediated by nuclear GAPDH. Expand
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