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br Model Fig demonstrates the block scheme of main
2023-02-07
Model Fig. 1 demonstrates the block-scheme of main interactions between variables of the model under investigation. These interactions are described below in details and are expressed in mathematical form as well, where all variables are the functions of space and time coordinates, r and t, which
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Perforation of the surface membrane however is
2023-02-07
Perforation of the surface membrane, however, is not the only mechanism of calcium dysregulation by Aβ at the presynaptic terminals. When in excess, both monomers and oligomers modulate biophysical properties of voltage-activated calcium 69 8 as well as calcium release from the endoplasmic reticulum
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Our conclusion was confirmed by two experiments The addition
2023-02-07
Our conclusion was confirmed by two experiments. The addition of aminopeptidase-specific inhibitors at high concentrations allowed us to exclude the possibility of substrate hydrolysis by other proteases present in the samples, for example, endoproteases. After the application of inhibitors, we were
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br Understanding AD through Transcriptome Analysis
2023-02-07
Understanding AD through Transcriptome Analysis Both classical gene discovery and pathway-based analysis of AD GWAS shed light on the range of biological processes that contribute to AD in addition to amyloid pathology. The straightforward interpretation and functional investigation of the associ
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-02-06
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Furthermore we found up regulated protein and mRNA levels
2023-02-06
Furthermore, we found up-regulated protein and mRNA levels of adenosine kinase in mouse retina with TON. The up-regulation of ADK was previously demonstrated in diabetic retinopathy (Pang et al., 2010). Greater levels of ADK in activated macrophages and microglial cells abrogate the immune response.
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In terms of the ring B C position while C
2023-02-06
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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Several reports of single cases of MG
2023-02-06
Several reports of single cases of MG patients treated with Rituximab have claimed a favourable response (Baek et al., 2007, Gajra et al., 2004, Hain et al., 2006, Thakre et al., 2007, Wylam et al., 2003, Zaja et al., 2000). We report our experience with Rituximab in 6 patients with severe MG, 3 pa
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br Discussion The clinical course of our patient until May
2023-02-06
Discussion The clinical course of our patient until May 2012 was rather typical of early onset AChR-MG. Later on, the pattern of the disease was more typical of MuSK-MG, as evidenced by the distribution of myasthenic weakness and the unprovoked exacerbations. The KPT-276 australia of MuSK-MG app
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It is already established in the
2023-02-06
It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ
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need that moment The discovery of acetylsalicylic acid aspir
2023-02-06
The discovery of acetylsalicylic need that moment (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy and in partic
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Additionally regulation of GPCR heteromerization by specific
2023-02-06
Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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Previous studies have demonstrated that the expression of
2023-02-06
Previous studies have demonstrated that the expression of the Aurora B gene is maximally increased at G2/M phage during mitosis (Honda et al., 2003, Fu et al., 2007, Goldenson and Crispino, 2015), and exhibits an extraordinary upregulation in a number of human cancers (Fu et al., 2007, Kollareddy et
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Matthew et al synthesized and carried out SAR studies of
2023-02-06
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that R 59-022 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC5
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The canonical binding sites to which or
2023-02-06
The canonical CGS 21680 receptor to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of compound effects
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