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Acknowledgments We acknowledge the Danish Council for Indepe
2020-05-21
Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
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For the SAR optimization of the right hand side it
2020-05-21
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic 1347 mg moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by condensation
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As temperatures increase rates of spontaneous deamination al
2020-05-21
As temperatures increase, rates of spontaneous deamination also increase such that hyperthermophilic organisms must have efficient mechanisms for dealing with this potential hazard.8., 9. The hyperthermophile Methanococcus jannaschii has both a dCTP deaminase (encoded by the gene at locus MJ0430) an
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Previous studies on the chemokines role in depression are
2020-05-21
Previous studies on the chemokines role in depression are not detailed enough, and cannot sufficiently demonstrate even a hypothetical mechanism explaining the differences in levels of particular chemokines and their receptors, in relation to the severity of depression [29], [30]. Previous studies o
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Recent data obtained with etifoxine suggest that
2020-05-21
Recent data obtained with etifoxine suggest that facilitation of GABAergic inhibition may be also associated with an indirect mechanism implying activation of the peripheral benzodiazepine receptor with a subsequent increase in neurosteroid production (Schlichter et al., 2000, Verleye et al., 2005)
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br Introduction As a serine proteinase and
2020-05-20
Introduction As a serine proteinase and a sub-family of the chymotrypsin-like proteinase, Glutamyl endopeptidase (GE), which is mainly found in Bacillus species, specifically cleaves negatively charged amino c75 receptor residues (Glu/Asp) (Yokoi et al., 2001). Madsen et al. (Madsen & Qvist, 199
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Herein we explored by docking
2020-05-20
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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In a study on the time course of a
2020-05-20
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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Introduction Glucose is the major
2020-05-19
Introduction Glucose is the major carbon source in most organisms. Cancer FSLLRY-NH2 mg in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainly
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br Introduction Hydrogen sulfide H S and nitric
2020-05-19
Introduction Hydrogen sulfide (H2S) and nitric oxide (NO) are important gasotransmitters in the cardiovascular system and instrumental to the fine control of vascular tone [1] and cellular function [2]. NO is synthesized from l-arginine by calmodulin-dependent endothelial nitric oxide synthase (e
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Anaesthetized mice of one eNOS KO strain showed a
2020-05-19
Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin s
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Two GPCR subtypes of interest in the myocardium are
2020-05-19
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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Other membrane currents are affected as well
2020-05-18
Other membrane currents are affected as well. Some studies have provided evidence that sulfonylureas, in addition to blocking KATP channels, also inhibit chloride and calcium channels. GLYB has been shown to almost inhibit the current generated by Na+–K+ pumps in a concentration-dependent manner (wi
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Miltefosine The N B method has the overall
2020-05-18
The N&B method has the overall advantage that it is not restricted to certain dyes specific for energy transfer [55], and is also able to detect higher order receptor Miltefosine on the focal point in living cells. Conclusion The N&B method has shown to be a powerful tool to locate and quantify
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br Conclusion In conclusion our findings do not suggest that
2020-05-18
Conclusion In conclusion, our findings do not suggest that HT is an important determinant of future AD risk and are in line with a recent Cochrane review stating that HT is not indicated for preventing dementia or cognitive decline in postmenopausal women [13]. Contributors Conflict of inte
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