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KPT-9274 Against this backdrop we set out to identify synthe
2020-12-08

Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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br Enzymes involved in microbial
2020-12-08

Enzymes involved in microbial steroid degradation are generally not expressed constitutively, but they are upregulated depending on which steroid substrates are present [17,81]. Thus, a cell-free extract prepared from testosterone-adapted C. testosteroni ATCC 11996 cells displayed a 1(2)-dehydroge
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br General Characteristics of the
2020-12-08

General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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Our previous studies have demonstrated
2020-12-08

Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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DDR distribution in healthy fibrotic and inflamed tissues Wh
2020-12-08

DDR1 distribution in healthy, fibrotic and inflamed tissues Whereas we can easily mine publicly available databases to infer DDR1 expression profile in different tissues (as reported in Fig. 1), fine comprehension of DDR1 biology has been hampered by the absence of a commercially available specific
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As described above when EGCG was
2020-12-08

As described above, when EGCG was orally administered, CYP3A expression in the liver decreased; however, the CYP3A expression level in the intestine was unchanged (Fig. 3). Although we remain speculative, one reason for this may be that because the level of intestinal bacteria in the upper part of t
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Diclofenac ibuprofen and meloxicam are considered among
2020-12-08

Diclofenac, ibuprofen, and meloxicam are considered among the most commonly used NSAIDs in many countries [4]. Cardiovascular events were reported with these NSAIDs in several clinical studies. In this study, we provide novel information that diclofenac and ibuprofen altered gene expression and may
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Orange spotted grouper Epinephelus coioides
2020-12-08

Orange-spotted grouper (Epinephelus coioides) is a coral reef fish with a high commercial value in China and Southeast Asian countries. However, in recent years, various outbreaks of viral diseases have affected the grouper aquaculture industry (Wei et al., 2010). Specifically, Singapore grouper iri
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In humans individual differences in prefrontal dopamine are
2020-12-08

In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia
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Fmoc-Cl receptor SPR was used to measure biomolecular kineti
2020-12-08

SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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gsk3 Primary renal PNET was first
2020-12-07

Primary renal PNET was first reported by Seemayer et al in 1975. The possible etiology of rPNET is based on the theory of neural cell intussusception in the kidney during development that initiates the tumorigenesis. rPNET most commonly affects young adults, with a mean age of 30.4 years and male pr
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Interestingly global EGFR depletion increased the rate
2020-12-07

Interestingly, global EGFR depletion increased the rate of cell elimination everywhere in the notum (Figures 2B–2D), irrespective of the deformation status of the cells. Accordingly, we found that CI-1040 are not any more sensitive to stretching upon EGFR depletion (Figures S6A–S6C; Video S5). This
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br Non cyclic nucleotide EPAC regulators Despite
2020-12-07

Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su
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br Introduction Prostaglandin E PGE signals
2020-12-07

Introduction Prostaglandin E2 (PGE2) signals through 4 separate G-protein coupled receptor sub-types (EP1, EP2, EP3 and EP4) to elicit a variety of physiological and pathophysiologic effects. EP2 and EP4 increase cAMP levels in the cell via adenylate cyclase activation, whereas EP3 inhibits cAMP
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In conclusion the data suggest that doses
2020-12-07

In conclusion, the data suggest that doses of COX-2 inhibitors and EP1 receptor antagonists which have previously been reported to exert disease modulating or antiepileptic drug potentiating effects do not negatively affect seizure control in temporal lobe epilepsy. The contrasting impact of the EP1
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