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A novel series of DHODH inhibitors was developed by us
2020-07-22

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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Introduction Formate dehydrogenase enzymes FDHs
2020-07-22

Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ
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Previous studies revealed the expression of the CCR receptor
2020-07-22

Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr
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To investigate the mechanism of action of
2020-07-22

To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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Located on the fore tarsals of the front pair
2020-07-22

Located on the fore-tarsals of the front pair of legs, the Haller’s organ is presumed central to tick chemosensation. Recent genomic, transcriptomic and proteomic investigations have identified several families of transmembrane proteins in the forelegs of ticks that are likely involved in olfactory
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P falciparum DHFR TS is a particularly important
2020-07-21

P. falciparum DHFR-TS is a particularly important enzyme, because it is from the protozoan species that is associated with most malaria infections. Since this enzyme is responsible for catalyzing sequential reactions in the thymidylate cycle, its inhibition slows malarial dTMP production and therefo
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Preparation of the pyridyl ether
2020-07-21

Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate, f
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This work aimed to investigate
2020-07-21

This work aimed to investigate whether the increase in liver lipid depots, observed in the fetuses from rats fed a saturated-fat-rich diet, persists later in life in the offspring (a) at 21days of age immediately after weaning and (b) at 140days of age, after healthy nourishing. Furthermore, we want
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Anisodamine In contrast to PEGylated proteins which tend to
2020-07-21

In contrast to PEGylated proteins which tend to have reduced Anisodamine in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applications in the field of c
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There is a considerable molecular
2020-07-21

There is a considerable molecular genetic heterogeneity within ES/PNET. As mentioned above, either or can rearrange with in these gene fusions. Furthermore, for either gene fusion, additional heterogeneity stems from the location of the genomic breakpoints of the translocation, resulting in differen
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br EBV Infection Epstein Barr virus
2020-07-21

EBV Infection Epstein–Barr virus (EBV, human herpesvirus 4) was discovered 50 years ago, when Epstein, Achong, and Barr used electron microscopy to identify viral particles in Burkitt\'s lymphoma cells. It belongs to the lymphocryptovirus (LCV) genus of the gammaherpesvirus subfamily (Fig. 1A). T
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br Results br Discussion The
2020-07-21

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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br Experimental Procedures br Author
2020-07-21

Experimental Procedures Author Contributions Acknowledgments We acknowledge Géraldine Le Goff and Mathieu Canales for blood sampling, Cécile Gameiro and Jean-Pierre Aubry for flow cytometry technical assistance, Giuseppe Pantaleo for support, and Britta Engelhardt, Gisella Puga-Young, Nicol
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Gupta et al have shown that a genetic variant
2020-07-20

Gupta et al have shown that a genetic variant associated with the 5 vascular diseases (coronary artery disease, migraine, carotid artery dissection, fibro-muscular dysplasia, and hypertension) is a distal regulator of the ET-1 gene [30]. They found that a single nucleotide polymorphism (SNP) located
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In addition to playing important roles in the immune system
2020-07-20

In addition to playing important roles in the immune system, EBI2 is also expressed in the Aprotinin of the central nervous system (CNS), namely astrocytes, and this receptor regulates astrocyte signalling, as well as astrocyte cell migration (Rutkowska et al., 2015, Rutkowska et al., 2016a). Moreo
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