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In this study we present the synthesis and structure activit
2022-02-11

In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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The ion conduction pathway reported herein accounts for all
2022-02-11

The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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In this present study the availability of commercial
2022-02-11

In this present study, the availability of commercial GLUT and SGLT Alogliptin mg directed against different epitopes, enabled us to screen for members of the SGLT family and compare the expression patterns of GLUTs and SGLTs in the different regions of the rat lens. Based on these regional and sub
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br Conclusions br Acknowledgement Work
2022-02-10

Conclusions Acknowledgement Work in the authors’ labs was funded by Natural Sciences and Engineering Research Council of Canada (OGP0194652 and OGP0041653) and Diabète Québec. Introduction Fifty years ago, Sydney Brenner proposed Caenorhabditis elegans as a useful model for the study of an
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Several other assay parameters were
2022-02-10

Several other assay parameters were also explored. First, the thermal dependence of the assay was investigated by measuring the specific activity at different temperatures (Fig. 7). That data show that enzymatic activity increases with increasing temperature. Interestingly, the observed rate increas
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In conclusion we have shown that the brain penetrating abili
2022-02-10

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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Introduction The Antiretroviral Therapy ART in
2022-02-10

Introduction The Antiretroviral Therapy (ART), in the last decade, has been providing a better treatment for the Human Immunodeficiency Virus 1 (HIV) infection, by reducing its viral load to undetectable levels and recovering the immune system. In fact, according to the last data from UNAIDS the mo
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FRAX486 Racemic protein crystallography has been
2022-02-10

Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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Dormancy is a physiological state when
2022-02-10

Dormancy is a physiological state when viable seeds do not germinate. Seed stratification, a commonly used technique, is used for dormancy removal and can be performed in moisture for an experimentally revealed time at warm or cold temperatures. All conditions depends on plant species (Dębska et al.
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Interestingly the rabbit cornea exhibited a more
2022-02-10

Interestingly, the rabbit cornea exhibited a more than two-fold higher level of total GST activity compared with that of the porcine cornea, whereas their levels of GSTO1‐1 and GSTP1‐1 activity were similar (Fig. 4). Because members of the GST Alpha, Mu, Pi and Omega VO-Ohpic trihydrate primarily ut
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NVP-BHG712 The biological activity at GPR a of
2022-02-10

The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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br The glyoxalase system has
2022-02-10

The glyoxalase system has not yet been studied in E. histolytica or G. lamblia. Searches in the G. lamblia genome (GiardiaDB.org) revealed two genes encoding hydroxyacylglutathione hydrolases (Morrison et al., 2007), but no glyoxalase I gene was found. The genome of E. histolytica does not have a
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br Conclusion These are exciting times in
2022-02-10

Conclusion These are exciting times in EAAT research. The discovery and use of the GltPh and GltTk transporters as model systems for EAATs has provided detailed understanding of structure–function aspects of the transporters. Moreover, recent studies into the physiological functions of the transp
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Both anxiety like behavior and sucrose preference intake wer
2022-02-09

Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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We have presented evidence that only muscle FBPase
2022-02-09

We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart palmitic acid expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our preliminary e
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