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In our previous report we synthesized derivatives with some
2023-04-25

In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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In addition to pH regulation by ion counter
2023-04-25

In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa
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To evaluate the ability of both sets of
2023-04-25

To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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324 4 Mass spectrometry Matrix assisted laser desorption
2023-04-21

Mass spectrometry. Matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) MS experiment was performed in linear and positive-ion mode on a DE-STR instrument equipped with a nitrogen laser (PE Biosystems, Foster City, CA). Each spectrum was calibrated in the default mode in which 0.1%
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br Introduction Heart Failure HF is a major and
2023-04-21

Introduction Heart Failure (HF) is a major and growing health challenge in India and the developing countries. It is one of the most important causes of morbidity and mortality in the industrialized world. The incidence and prevalence estimates of HF are unreliable in India because of the lack of
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Introduction The burden of cardiovascular disease CVD
2023-04-21

Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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Introduction The burden of cardiovascular disease CVD
2023-04-21

Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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Bioinformatics tools are becoming more powerful
2023-04-21

Bioinformatics tools are becoming more powerful and reliable due to the growing number and availability of experimentally determined protein structures (Arnold et al., 2006, Suplatov et al., 2015, Wiltgen and Tilz, 2009). The SWISS-MODEL and MODELLER programs are most frequently used for homology or
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Ginsenosides are the major bioactive constituents of the Pan
2023-04-21

Ginsenosides are the major bioactive constituents of the Panax ginseng root, which contain many types of ginsenosides including Rb1, Rg1, Rc, and Rg3. The ginsenoside Rb1 appears to be the most abundant of the bioactive ginsenosides [15]. Rb1 exhibits antiinflammatory, anticarcinogenic, and antioxid
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As we previously observed in
2023-04-21

As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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ACE inhibition is often thought to play
2023-04-20

ACE inhibition is often thought to play a central role in the mechanisms of blood pressure reduction in vivo, and most ACE inhibitory (ACEi) peptides were characterized based on in vitro ACE inhibition. A relationship between in vitro ACE inhibition and antihypertensive activity, however, is not app
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The inhibition of the exacerbated inflammatory
2023-04-20

The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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Interestingly this situation might be changed
2023-04-20

Interestingly, this situation might be changed by the immunological context, in particular by the cytokines encountered during differentiation or activation. LPS-activation of bone marrow-derived DCs differentiated in GM-CSF decreases autophagy, CP2, and subsequent activation of CD4+ T cells (Fig. 2
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What can we learn about the anticancer
2023-04-20

What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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There are two major isoforms of LO in
2023-04-20

There are two major isoforms of 12/15-LO in mammalian, 12 and 15- LO, with different cellular distributions. To determine the relative contributions of these isoforms towards glucose-induced monocyte-endothelial interactions, the distribution of these isoforms in the two cell types involved in leuko
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