Nucleoside phosphorylases (NPs) are pivotal enzymes in the salvage pathway, catalyzing the reversible phosphorolysis of nucleosides to produce nucleobases and α-D-ribose 1-phosphate.
Daniel Hormigo +4 more
doaj +1 more source
Descriptor-and fragment-based QSAR models for a series of Schistosoma mansoni purine nucleoside inhibitors [PDF]
The enzyme purine nucleoside phosphorylase from Schistosoma mansoni (SmPNP) is an attractive molecular target for the treatment of major parasitic infectious diseases, with special emphasis on its role in the discovery of new drugs against ...
ANDRICOPULO, Adriano Defini +3 more
core +1 more source
Objective Methotrexate (MTX) is the first‐line therapy for juvenile idiopathic arthritis (JIA), but up to 40% of patients do not respond to it. Low inosine triphosphate pyrophosphatase (ITPA) activity has been associated with reduced clinical remission. We investigated the role and underlying mechanisms of ITPA in vitro. Methods ITPA enzymatic activity
Sofia Sindici Forgiarini +19 more
wiley +1 more source
Boron‐10 carriers and their applications in boron neutron capture therapy
Summary of different types of boron drugs. Abstract Boron neutron capture therapy (BNCT) has emerged as a promising therapeutic modality in cancer treatment, demonstrating the ability to selectively eliminate cancer cells through the 10B(n,α)7Li nuclear reaction with minimal side effects on normal tissues.
Dachao Tang +7 more
wiley +1 more source
Inhibition of free radical generation and improved survival by protection of the hepatic microvascular endothelium by targeted erythrocytes in orthotopic rat liver transplantation [PDF]
The capacity of specifically targeted erythrocytes to inhibit free radical—mediated injury to the endothelial cell after cold preservation, and improve liver function was studied in two experimental models: An isolated perfused rat liver (IPRL) system ...
Demetris, AJ +8 more
core +1 more source
The study of biomolecular interactions between a drug and its biological target is of paramount importance for the design of novel bioactive compounds.
S. Decherchi +4 more
semanticscholar +1 more source
Structural insights into urocanate reductase using room‐temperature X‐ray crystallography
The active‐site dynamics of the microbial enzyme urocanate reductase were revealed by room‐temperature X‐ray crystallography.Urocanate reductase (UrdA) is a bacterial enzyme that converts urocanic acid to imidazole propionate. Its catalytic residue Arg411 undergoes a large conformational change in the substrate‐bound versus product‐bound states.
Swati Aggarwal +4 more
wiley +1 more source
Role of the human concentrative nucleoside transporter (hCNT1) in the cytotoxic action of 5[Prime]-deoxy-5-fluorouridine, an active intermediate metabolite of capecitabine, a novel oral anticancer drug. [PDF]
We attempt to identify the plasma membrane transporter involved in the uptake of 5'-deoxy-5-fluorouridine (5'-DFUR), an intermediate metabolite of capecitabine.
Casado, F.J. (F. Javier) +8 more
core +1 more source
Engineering Substrate Promiscuity of Nucleoside Phosphorylase Via an Insertions–Deletions Strategy
Nucleoside phosphorylases (NPs) are the key enzymes in the nucleoside metabolism pathway and are widely employed for the synthesis of nucleoside analogs, which are difficult to access via conventional synthetic methods.
Gaofei Liu +6 more
semanticscholar +1 more source
Carbohydrate‐Based Drug Discovery: Synthetic Strategies and Clinical Applications
The picture depicts the molecules discussed in the review. On the left side, the general scaffold of sugars is shown. Next to it are four carbohydrate‐based molecules, including remdesivir, islatravir, empagliflozin, and Globo‐H. Remdesivir and islatravir contain a substituted ribose ring attached to a modified nucleobase.
Stephan Scheeff +2 more
wiley +1 more source

