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The effect of ET activity
2021-02-22
The effect of ET-1 activity on the development of experimental pulmonary fibrosis has also been examined by other investigators. One study found that repeated administration of Bosentan, an ERA used to treat pulmonary arterial hypertension (PAH), significantly decreased bleomycin-induced pulmonary f
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Aminothiazole derivatives have been reported to contain
2021-02-22
2-Aminothiazole derivatives have been reported to contain antiviral [17], anti-inflammatory [18], and antimicrobial [19] activities. The in vitro anticancer studies showed that different 2-aminothiazole derivatives possess selective and potent inhibitory effect against wide-ranging human cancerous c
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br Discussion The N terminal domain of DDRs has
2021-02-22
Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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Our study found a significant association between
2021-02-22
Our study found a significant association between the degree of primary tumor lobulation and EGFR mutations status (P EGFR dpp-4 inhibitor status. However, only a small portion of these previous studies included the evaluation of lobulation, and almost all of them reported no association between EGF
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AZD 2281 br Results br Discussion The ubiquitin system has
2021-02-22
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 Significance Dysregulation of dopamine homeostasis contri
2021-02-22
Significance Dysregulation of dopamine homeostasis contributes to Parkinson's disease (PD). The nuclear receptor Nurr1 plays a central role in dopamine homeostasis, regulating the transcription of URB597 governing the synthesis, packaging, and reuptake of dopamine. Efforts to capitalize on Nurr1
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br Application of D receptor PET in psychiatric disorders
2021-02-22
Application of D1-receptor PET in psychiatric disorders Discussion Compared to other markers of the DA system, only a limited number of studies have investigated D1-R in psychiatric disorders. In schizophrenia, which is the most studied condition with a total of 83 identified unique patients,
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br Hypothesis on DDR protective mode
2021-02-22
Hypothesis on DDR1 protective mode of action The documented protective role of DDR1 is quite impressive, demonstrated using different preclinical models (immunologic [46,54,58], obstructive [45], and hypertensive [50]) with different intervention paradigms: genetic ablation [45,50,58,72], silenci
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Several RNA BPs like the
2021-02-20
Several RNA-BPs, like the ELAV protein family member HuR, tristetraprolin (TTP) or the KH-type splicing regulatory protein (KSRP) have been shown to interact with these AREs and thereby lead to stabilization or destabilization of the mRNA [5]. Control of nucleocytoplasmic mRNA export is also very i
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br Conclusions When the authors joined
2021-02-20
Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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Several limitations of this study need
2021-02-19
Several limitations of this study need to be acknowledged. First, although 200 patients were recruited into this study and completed assessments at baseline, only 89 patients completed the cognitive tests after 8weeks of treatment. The relatively long study period (8weeks) was the main reason for th
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Recently naphthoquinone derivatives have shown
2021-02-19
Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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One possible explanation for differences in the binding abil
2021-02-19
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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N fowleri enters the host through the nasal
2021-02-19
N. fowleri enters the host through the nasal cavity and travels via the olfactory nerve into the Z DEVD FMK synthesis where it causes PAM (Visvesvara and Stehr-Green, 1990). The ameba most commonly infects healthy young adults and children and is able to evade the immune system but also elicits ext
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As described above we designed
2021-02-19
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl grou
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