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As part of our discovery efforts searching for small molecul
2021-10-11
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragmen
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SAR around amino derivative revealed a number of interesting
2021-10-11
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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Dendritic damage and loss of synaptic connections
2021-10-11
Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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br Introduction Connexins are transmembrane
2021-10-11
Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent PD153035 hydrochloride receptor via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nutrien
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Butyrolactone 3 The presence of FBP in nuclei seems to accom
2021-10-09
The presence of FBP2 in nuclei seems to accompany the cells' potential to divide as it has been shown that during differentiation of the satellite cells (myogenic progenitor cells) the amount of nuclear FBP2 decreases and in differentiated myotubes, the localisation of FBP2 is restricted to cytoplas
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Chi square tests with significance set to p
2021-10-09
Chi-square tests with significance set to p Results There were 4090 hip fracture patients included in the study. 2326 of these received enoxaparin, 929 received XaI, and 835 received warfarin. The mean CCI for each group was 3 (Table 2). There were some significant differences in demographics betw
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Endotoxin induced pulmonary hypertension is a reproducible f
2021-10-09
Endotoxin induced-pulmonary 98 is a reproducible finding in various animal models Leeper-Woodford et al., 1991, Weitzberg et al., 1993 and is also a feature of human sepsis where it may affect right ventricular function (Vincent, 1998). Mechanisms such as vasoconstriction and leukocyte aggregation
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The Scribble complex localizes to
2021-10-09
The Scribble complex localizes to the leading edge in response to integrin engagement. There, Scribble controls the activation Rac and PAK via the Rac GEF β-Pix (Bahri et al., 2010), which is required for collective cell migration (Omelchenko et al., 2014). However, on the rear edge, Scribble can be
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The top concern for the clinical use of CRISPR
2021-10-09
The top concern for the clinical use of CRISPR-Cas9 technology is safety. Off-target alterations must be avoided to ensure genome integrity and proper cellular function. WGS found no off-target effects among the top 49 predicted off-target sites. WGS did find 4,658 indels and 1,891 SNVs in sgRNA1/2-
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Piericidin A mg The diverse biochemistry of zinc means that
2021-10-08
The diverse biochemistry of zinc means that, in many cases, more than one factor (or pathway) is at play. Whilst catalytic Zn2+ sites are now typically well-understood, the recognition that Zn2+ levels regulate the function of many cell types has led to vigorous interest in the fate and role of mobi
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In Gallus gallus four FGFRs FGFR have been
2021-10-08
In Gallus gallus, four FGFRs (FGFR1-4) have been identified, along with 13 FGFs (FGF1–4, 8–10, 12, 13, 16, 18–20) (Thisse and Thisse, 2005). FGFRs are tyrosine kinase receptors that contain an extracellular ligand binding domain, a transmembrane domain and an intracellular tyrosine kinase domain. Th
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Histamine receptors were largely linked with allergic and in
2021-10-08
Histamine receptors were largely linked with allergic and inflammatory reactions before the recognition of the histamine H3R in 1983 that proved its function as auto- as well as heteroreceptor at pre- and postsynaptic membranes and demonstrated its intense regulating influence on release of numerous
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Netilmicin Sulfate Importantly the regulation of the
2021-10-08
Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d
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br Tissue Specific Roles for HIF PHD Isoforms Hypoxia
2021-10-08
Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune 96 4 receptor and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory
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In our substudy patients carrying the Ile Val or Val
2021-10-08
In our substudy, patients carrying the Ile/Val or Val/Val genotypes had significantly worse DFS compared to patients carrying the Ile/Ile genotype, after adjustment for potential confounders. Two previous studies examining the association between HER2 Ile655Val polymorphism and trastuzumab response
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