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I bungarotoxin competes with ACh an endogenous activator of
2021-01-14

[125I] α-bungarotoxin competes with ACh, an endogenous activator of α7-nACh receptors by binding to the ACh binding site on the receptor (Albuquerque et al., 2009). For this reason, the effect of curcumin was investigated on the specific binding of [125I] α-bungarotoxin. Saturation curves for the bi
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Initially we ascertained that if the
2021-01-13

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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In summary we hypothesize that targeting the A R D
2021-01-13

In summary, we hypothesize that targeting the A1R–D1R heterotetramer with heteromer-selective drugs might improve safety and efficacy of the pharmacological therapy for RLS and other motor diseases, resulting in fewer side effects than classical drugs developed for targeting monomeric A1R or D1R.
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br Results br Discussion In addition
2021-01-13

Results Discussion In addition to contributing to amino nmda receptor antagonist and lipid biosynthesis, mitochondrial metabolism affects nucleotide biosynthesis. Indeed, many components that contribute to both pyrimidine and purine bases are derived directly or indirectly from mitochondria.
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Preclinical and clinical research indicates
2021-01-13

Preclinical and clinical research indicates that inflammation contributes to the progression of ICH injury. Therefore, there is a pressing need to develop interventions that can limit neuroinflammation and its detrimental effects on sodium channel blockers function. Inflammatory cytokines are secre
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Agglutinin like sequence ALS gene is well
2021-01-13

Agglutinin-like sequence (ALS) gene is well-characterized gene family in candidiasis due to its importance in pathogenicity of C albicans. Previously, C. albicans ALS1 gene product was reported as cell surface protein that mediates adherence to endothelial and epithelial Vicriviroc Malate mg in vit
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A previous report showed that
2021-01-13

A previous report showed that the transfer of the CSF1 gene into tumor myc inhibitor induced TAM infiltration into syngeneic BALB/c mice. High expressions of CSF-1 and CSF-1R in tumor and stromal cells and a high TAM density are known to be correlated with poor prognoses in many cancer types. CSF-1
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Acidic substituents showed moderate biochemical activity but
2021-01-13

Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic bcrp inhibitor were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemi
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br Results br Discussion GPCRs recognize
2021-01-13

Results Discussion GPCRs recognize a broad range of molecules with a vast chemical TAPI-1 through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabinoids includin
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Kumar et al studied Umbelliferone D galactopyranoside UFG be
2021-01-13

Kumar et al. studied Umbelliferone β-D-galactopyranoside (UFG) (benzopyrone), found in many plants exhibiting numerous pharmacological actions. The results of the study showed that UFG in a dose of 10, 20 or 40mgkg-1 per day, helps to prevent paw edema and arthritic score development for arthritis i
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Based on the above we hypothesized
2021-01-13

Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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What is the predominant mechanism underlying
2021-01-13

What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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br Materials and methods br Results br
2021-01-12

Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic auz induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter status epilepticu
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To provide a brief critical evaluation of
2021-01-12

To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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br O GlcNAcase Human OGA is a multidomain protein
2021-01-12

O-GlcNAcase Human OGA is a multidomain protein with an N-terminal domain similar to glycoside hydrolase family 84 (GH84) enzymes, a stalk domain, a C-terminal pseudo histone acetyltransferase (HAT) domain, and several low-complexity regions (Figure 1f) [43]. A splice variant that lacks the HAT do
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