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A novel series of DHODH inhibitors was developed by
2021-07-06
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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Nitric oxide NO is synthesized by conversion of the
2021-07-06
Nitric oxide (NO) is synthesized by conversion of the l-arginine to NO and l-citrulline through reaction which is catalyzed by nitric oxide synthetase (NOS) (Knowles and Moncada, 1994). NO as an important molecule not only play a role as second messenger but also binds to cytochrome c oxidase and de
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We aim to apply the same technology
2021-07-06
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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To date little is known
2021-07-06
To date, little is known about the regulation of PCD through phytocystatin inhibitory activity. Inhibitors that may regulate leaf senescence (Huang et al., 2001, Tajima et al., 2011) or may inhibit PCD induced by abiotic factors, such as mechanical tissue damage or oxidative stress caused by cold (B
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Citrus plants are of great interest because they
2021-07-06
Citrus plants are of great interest because they contain large amounts of flavonoids, and citrus fruits and their juices are consumed in large quantities around the world [18]. The flavonoid contents and profiles of citrus juices vary greatly with the type of fruit. It has been determined that citru
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QX 314 chloride mg The changes in the chemokine receptors
2021-07-06
The changes in the chemokine receptors CCR-5 and CXCR-4 in women and men with PTSD are completely different. In the group of women with PTSD alone the level of this QX 314 chloride mg increased six times, whereas, in women with APD and PTSD, the level of the receptor CCR-5 was eight times higher th
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In we studied normal rational varieties
2021-07-06
In [1] we studied normal, rational -varieties X of complexity one, where the latter means that X comes with an effective torus action such that holds. We showed that for affine X with and at most log terminal singularities, the iteration of Cox rings is possible. In the present article, we character
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This study demonstrates that GUL affects multiple pathways p
2021-07-06
This study demonstrates that GUL-1 affects multiple pathways/processes. As GUL-1 is likely to function as an RNA-binding protein, it is conceivable that the mRNAs involved are bound to GUL-1 as part of the regulatory function of the protein. In fact, in S. cerevisiae Ssd1 was shown to bind multiple
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This structure guided the variation
2021-07-06
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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br Summary and perspectives In recent decades enormous
2021-07-06
Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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Initially we ascertained that if
2021-07-06
Initially, we ascertained that if the dose of elastase was sufficient to cause pulmonary emphysema, then pulmonary emphysema could be maintained throughout the study. We found that elastase at 3U was sufficient to cause emphysema that remained over 35 days. In this experimental design of lung diseas
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br Multi subunit RINGs There are
2021-07-05
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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We also observed reduced insulinotropic effects after intrav
2021-07-05
We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i
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Poxviruses have double stranded DNA dsDNA genomes yet they r
2021-07-05
Poxviruses have double-stranded DNA (dsDNA) genomes, yet they replicate within the cytoplasm. Poxviruses that cause human disease include monkeypox virus (Reynolds et al., 2004), molluscum contagiosum virus (Hanson and Diven, 2003) and variola virus (VARV), the cause of smallpox, a disease eradicat
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Introduction In vitro synthetic biology has received conside
2021-07-05
Introduction In vitro synthetic biology has received considerably less attention than in vivo processes so far (Foster and Church, 2007). However, cell-free biosynthetic production is very likely to become important for many biotechnological challenges for reasons such as (energy) efficiency, syste
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