Search results for "adenine"

Ibrutinib for the treatment of relapsed/refractory mantle cell lymphoma: extended 3.5-year follow up from a pooled analysis

2019

Differential Effects of Tenofovir/Emtricitabine and Abacavir/Lamivudine on Human Leukocyte Recruitment

2012

Background The association of abacavir (ABC) with cardiovascular disease has led to HIV treatment guidelines favouring the combination of tenofovir/emtricitabine (TDF/FTC) over that of ABC/lamivudine (ABC/3TC). We have analysed the effects of plasma-relevant concentrations of TDF, FTC, ABC and 3TC, individually and in clinically employed combinations, on human leukocyte accumulation. The effects of ABC, 3TC, TDF and FTC on the expression of adhesion molecules were also evaluated. Methods Interactions between human leukocytes – specifically peripheral blood polymorphonuclear or mono-nuclear cells – and human umbilical vein endothelial cells were evaluated in a flow chamber reproducing in viv…

MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate

2019

Polo-like kinase (PLK1) has been identified as a potential target for cancer treatment. Although a number of small molecules have been investigated as PLK1 inhibitors, many of which showed limited selectivity. PLK1 harbors a regulatory domain, the Polo box domain (PBD), which has a key regulatory function for kinase activity and substrate recognition. We report on 3-bromomethyl-benzofuran-2-carboxylic acid ethyl ester (designated: MCC1019) as selective PLK1 inhibitor targeting PLK1 PBD. Cytotoxicity and fluorescence polarization-based screening were applied to a library of 1162 drug-like compounds to identify potential inhibitors of PLK1 PBD. The activity of compound MC1019 against the PLK1…

Ultrafast dynamics of adenine following XUV ionization

2022

JPhys photonics 4, 034003 (2022). doi:10.1088/2515-7647/ac6ea5 special issue: "Focus on Nanophotonics and Biophotonics for Biomedical and Environmental Applications"

Suitability of non-glucose-carbohydrates for parenteral nutrition

1975

Postoperative parenteral nutrition can only be optimally effective if the characteristics of post-traumatic metabolism are taken into account. Two main possibilities are discussed for the carbohydrate component of parenteral nutrition during this phase: glucose with high doses of insulin or non-glucose carbohydrates (sugar substitutes) possibly in a suitable combination with glucose. The risks as well as the technical and organisational problems involved in the use of them are discussed and the authors prefer the second of the two alternatives. Possible side effects of non-glucose carbohydrates are pointed out and it is shown how these can be avoided by observing dose guidelines. So far a c…

Bestimmung von Glykolyse-Metaboliten in isolierten Zellkernen

1958

Isolated rat liver nuclei have been analyzed for the intranuclear concentration of 8 glycolytic metabolites, and in addition for the 3 adenine nucleotides, and for malate. All these substrates are to be found in nuclei in a range of concentration comparable to that in the whole tissue. The consequences of these findings with respect to the definite establishment of glycolysis in isolated nuclei, as well as for the intranuclear formation of energy-rich phosphate bonds, are discussed.

Therapeutic effect of enhancing endothelial nitric oxide synthase (eNOS) expression and preventing eNOS uncoupling

2011

Nitric oxide (NO) produced by the endothelium is an important protective molecule in the vasculature. It is generated by the enzyme endothelial NO synthase (eNOS). Similar to all NOS isoforms, functional eNOS transfers electrons from nicotinamide adenine dinucleotide phosphate (NADPH), via the flavins flavin adenine dinucleotide and flavin mononucleotide in the carboxy-terminal reductase domain, to the heme in the amino-terminal oxygenase domain. Here, the substrate L-arginine is oxidized to L-citrulline and NO. Cardiovascular risk factors such as diabetes mellitus, hypertension, hypercholesterolaemia or cigarette smoking reduce bioactive NO. These risk factors lead to an enhanced productio…

Influence of carboxylic acids on the stereospecific nicotinamide adenine dinucleotide-dependent and nicotinamide adenine dinucleotide-independent lac…

1971

Leuconostoc mesenteroides increased its lactic acid production from glucose threefold when malic acid was added to the culture. This increase resulted also in a reduction of the ratio of d -lactic acid to l -lactic acid (31.5 to 1.23). Addition of malic acid increased 6.5-fold the specific activity of nicotinamide adenine dinucleotide (NAD)-linked l -lactate dehydrogenase and increased 3.2-fold that of NAD-linked d -lactate dehydrogenase. The Michaelis constant ( K m ) for NAD of the NAD-linked l -lactate dehydrogenase increased with the addition of malate, but no change was observed in the K m values for the respective d -enzyme. The effect of carboxylic acids on the NAD-linked l -lactate…

Nicotinamide Adenine Dinucleotide-Dependent and Nicotinamide Adenine Dinucleotide-Independent Lactate Dehydrogenases in Homofermentative and Heterofe…

1971

Three homofermentative ( Lactobacillus plantarum B38, L. plantarum B33, Pediococcus pentosaceus B30) and three heterofermentative ( Leuconostoc mesenteroides 39, L. oenos B70, Lactobacillus brevis ) lactic acid bacteria were examined for the presence or absence of nicotinamide adenine dinucleotide (NAD)-dependent and NAD-independent d - and l -lactate dehydrogenases. Two of the six strains investigated, P. pentosaceus and L. oenos , did not exhibit an NAD-independent enzyme activity capable of reducing dichlorophenol indophenol. The p H optima of the lactic dehydrogenases were determined. The NAD-dependent enzymes from homofermentative strains exhibited optima at p H 7.8 to 8.8, whereas va…

Regulation of NADPH oxidase-mediated superoxide production by acetylation and deacetylation

2021

Oral treatment of apolipoprotein E-knockout (ApoE-KO) mice with the putative sirtuin 1 (SIRT1) activator resveratrol led to a reduction of nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activity in the heart. In contrast, the SIRT1 inhibitor EX527 enhanced the superoxide production in isolated human polymorphonuclear granulocytes. In human monocytic THP-1 cells, phorbol ester-stimulated superoxide production was enhanced by inhibitors of histone deacetylases (HDACs; including quisinostat, trichostatin A (TSA), PCI34051, and tubastatin A) and decreased by inhibitors of histone acetyltransferases [such as garcinol, curcumin, and histone acetyltransferase (HAT) Inhibitor II]. Thes…