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Reduction of N(ω)-hydroxy-L-arginine by the mitochondrial amidoxime reducing component (mARC).
TLDR
It is shown for the first time that both human isoforms of the newly identified mARC (mitochondrial amidoxime reducing component) enhance the rate of reduction of NOHA, in the presence of NADH cytochrome b₅ reductase and cy tochrome b ₅, by more than 500-fold, providing the first hints that mARC might be involved in mitochondrial NOHA reduction and could be of physiological significance in affecting endogenous nitric oxide levels. Expand
The fourth molybdenum containing enzyme mARC: cloning and involvement in the activation of N-hydroxylated prodrugs.
TLDR
The recombinant enzyme allows prediction about in vivo reduction of N-hydroxylated prodrugs, and the prodrug principle is not dependent on cytochrome P450 enzymes. Expand
New Prodrugs of the Antiprotozoal Drug Pentamidine
TLDR
The objective of this investigation was the systematic characterisation and evaluation of eight pentamidine prodrugs in order to identify the most appropriate strategy to improve the properties of the parent drug. Expand
Synthesis and biological evaluation of L-valine-amidoximeesters as double prodrugs of amidines.
TLDR
Bioactivation of N-valoxybenzamidine and N,N'-bis(valoxy)pentamidine via hydrolysis and reduction has been demonstrated in vitro with porcine and human subcellular enzyme preparations and the mitochondrial Amidoxime Reducing Component (mARC). Expand
Development of novel potent orally bioavailable oseltamivir derivatives active against resistant influenza A.
TLDR
Bioisosteric replacement of the 5-guanidine with an acetamidine-in the form of its N-hydroxy prodrug-successfully tackled the two key limitations of currently used NA inhibitors, as exemplified with oseltamivir. Expand
Prodrug design for the potent cardiovascular agent Nω-hydroxy-L-arginine (NOHA): synthetic approaches and physicochemical characterization.
TLDR
This work describes an approach to impart NOHA drug-like properties by wrapping up the chemically and metabolically instable N-hydroxyguanidine moiety with different prodrug groups, and essentially presents the first prodrug approaches for an interesting pharmacophoric moiety, i.e., N-HydroxyGuanidine. Expand
Highly Potent and Selective Substrate Analogue Factor Xa Inhibitors Containing D‐Homophenylalanine Analogues as P3 Residue: Part 2
TLDR
A series of highly potent substrate‐analogue factor Xa inhibitors containing D‐homophenylalanine analogues as the P3 residue has been identified by systematic optimization of a previously described inhibitor structure with significantly enhanced potency and selectivity. Expand
Zanamivir Amidoxime- and N-Hydroxyguanidine-Based Prodrug Approaches to Tackle Poor Oral Bioavailability.
TLDR
Different prodrug approaches are described that aimed at overcoming zanamivir's lack of oral bioavailability, and the most promising prodrug candidates, amidoxime ester 7 and N-hydroxyguanidine ester 8, were subjected to in vivo bioavailability studies. Expand
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.
A novel series of matriptase inhibitors based on previously identified tribasic 3-amidinophenylalanine derivatives was prepared. The C-terminal basic group was replaced by neutral residues to reduceExpand
MS³ fragmentation patterns of monomethylarginine species and the quantification of all methylarginine species in yeast using MRM³.
TLDR
It is demonstrated that the two forms of MMA have indistinguishable primary product ion spectra, however, the secondary product Ion spectra of δMMA and ηMMA exhibited distinct patterns of ions. Expand
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