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Besides by substrate and product KSTDs may also be inhibited
2020-09-27

Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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Consistent with previous simulations on the DFG
2020-09-27

Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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The conventional medical therapy for IBD consists in reducin
2020-09-27

The conventional medical therapy for IBD consists in reducing the inflammatory response using various strategies that exert severe side-effects, a strategy that also decreases the risk of colon carcinoma [13], [14]. During the last decade, the activation of the cholinergic system has been proposed f
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It was recently reported that a functional single
2020-09-27

It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid GNE-7915 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an autosomal recessive for
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During the Lapita period in
2020-09-27

During the Lapita period in Tonga, the Talasiu site would have been an attractive location for human settlement as it overlooked an embayment holding large numbers of sessile and gregarious shellfish close to a fresh water solution channel, with gardening soils immediately inland. However, sea level
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As shown in Figs a and b with the
2020-09-27

As shown in Figs. 3(a) and (b), with the SO effect, the absolute values of the VDEs change by at most 0.19eV. Table 1 also shows that the observed peak splitting energies in the Sm-Ho complexes were reproduced even without the SO effect. Considering its significant importance in the electronic struc
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Collectively these data suggest the potential clinical utili
2020-09-27

Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone\'s effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced
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In this study CK C prepared from BL DE
2020-09-27

In this study, CK1δ(ΔC) prepared from BL21(DE3)pλPP had the highest kinase activity among the three isoforms tested when using casein as a substrate. Therefore, CK1δ(ΔC) from BL21(DE3)pλPP has the potential to be a “phosphorylating reagent” that may be widely used in experiments of phosphorylation a
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Several cholinesterase inhibitors have also been radiolabell
2020-09-27

Several cholinesterase inhibitors have also been radiolabelled with 11C as potential cholinesterase imaging agents. These include 11C-donepezil, 11C-methyltacrine, and 11C-physostigmine, which also have had limited success in demonstrating the known histochemically defined cholinesterase distributio
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Recently roflumilast has been approved
2020-09-25

Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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Because stimulation and blockade of dopamine
2020-09-25

Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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Studies on the external dehydrogenases
2020-09-24

Studies on the external dehydrogenases of N. crassa have shown that the NDE1 protein is a Ca2+-dependent external NADPH dehydrogenase, while NDE2 is characterized as a dehydrogenase oxidizing both cytosolic substrates (external NADH and/or NADPH) (Carneiro et al., 2004, Melo et al., 2001). All three
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Cytokines are small secreted proteins that mediate and regul
2020-09-24

Cytokines are small secreted proteins that mediate and regulate immunity, inflammation, and hematopoiesis. They are produced in response to an immune stimulus. Cytokines regulate the intensity and duration of the immune response by stimulating or inhibiting the activation, proliferation, and/or diff
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CysLTs trigger contractile and inflammatory processes throug
2020-09-24

CysLTs trigger contractile and inflammatory processes through the specific interaction with cell surface receptors belonging to the rhodopsin family of the G protein-coupled receptor (GPCR) genes. Until now, two receptor subtypes have been cloned, namely CysLT1 and CysLT2[8]. In particular, when the
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br Acknowledgements This work was supported by
2020-09-24

Acknowledgements This work was supported by the National Institute of Neurologic Disorders and Stroke (U54 HD061222, 1K23 NS107646-01, and 1K12NS089417-01), Rocky Mountain Rett Association, International Foundation for CDKL5 Research, the Ponzio Family Chair in Neurology Research, and NHMRC Senio
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