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While the specific set of challenges associated with deorpha
2021-10-09
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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SAR around amino derivative revealed
2021-10-09
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-po
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Limited efforts were made to exploit the naturally occurring
2021-10-09
Limited efforts were made to exploit the naturally-occurring antigen-specific Treg for ex vivo expansion. This study sets up a reproducible protocol for the expansion of insulin-specific Treg isolated from NOD mice. These MTEP hydrochloride receptor exhibited higher suppressive capacity compared to
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As GLO is the major detoxification system of reactive
2021-10-09
As GLO1 is the major detoxification system of reactive dicarbonyls, it is plausible that differences in production and activity of the enzyme influences AGE production and the development and/or modulation of diabetic neuropathy. Glo1 exists as a copy number variant (CNV) in many inbred strains mice
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To verify the feasibility of the proposed
2021-10-09
To verify the feasibility of the proposed method, EIS is firstly adopted to study the modification processes of the electrode. As shown in Fig. 1A, the nyquist plot of bare gold electrode exhibits a straight line, which indicates a fast charge transfer process (curve a). After modified with probe a,
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After brain injury adenosine levels
2021-10-09
After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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It is an aspiring task to apply the glutamate biosensor
2021-10-09
It is an aspiring task to apply the glutamate biosensor for in vivo measurements in 2478 tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in diameter for the bi
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br Experimental methods br Acknowledgments We
2021-10-09
Experimental methods Acknowledgments We thank all members of the Hermanson lab, especially Ana Teixeira, Shirin Ilkhanizadeh and Karolina Wallenborg, for assistance and discussions, Peter Löw for anti-synaptotagmin antibody, and Lars Björklund, Ole Isacson, Christer Höög, Claes Wahlestedt and
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Free d glutamate also has been found in
2021-10-09
Free d-glutamate also has been found in various tissues of invertebrates and vertebrates including mammals (Han et al., 2011; Ariyoshi et al., 2017), fish (Kera et al., 2001) amphibians (Kera et al., 2001), birds (Kera et al., 2001), mollusks (Tarui et al., 2003; Patel et al., 2017) and arthropods (
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br Do the actions of
2021-10-09
Do the actions of GLP-1R agonists on the vascular endothelium account for GLP-1R agonist-mediated cardioprotection? The previous section highlighted the recent clinical evidence from cardiovascular outcomes studies supporting the notion that GLP-1R agonists confer cardioprotective actions in pati
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In total strains with relatively rapid acid
2021-10-08
In total, 5 strains with relatively rapid acid-producing ability (MA14, 15M2, DQHXNQ38–12, 5G2, and 6G5) were selected for further analysis. Compared with the strains ATCC19435, ZN8, and D-XJ4–12, which were used as controls, these 5 strains exhibited significantly different growth and titratable ac
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After the successful development of molecular targeted drugs
2021-10-08
After the successful development of molecular targeted drugs in lung adenocarcinoma, substantial efforts have been made to provide similar targeted drugs in lung squamous-cell carcinoma. Because FGFR gene alteration is the most frequent occurrence in squamous-cell carcinoma, targeted therapies for F
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Reducing the molecular weight According
2021-10-08
Reducing the molecular weight: According to a thorough analysis of a large, structurally diverse Caco-2 permeability dataset using a variety of statistical techniques by AstraZeneca researchers, logD and molecular weight are suggested the most important factors in determining the permeability of dru
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Type II diabetes is characterized by an inability to
2021-10-08
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty 5α-dihydro-11-keto Testosterone receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of
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It is well established that transcription factors
2021-10-08
It is well established that transcription factors are the major key players in regulating the transcriptional state of the targeted gene. 15 TFs were found in the present study, which were predicted to have the binding affinity with the EZH2 promoter region. Out of these, GCF, AP-2 and Sp1 were most
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