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Third we performed correlation analysis
2022-02-22

Third, we performed correlation analysis between the results obtained using DMR agonist assay in HT-29 and Tango assay in the engineered U2OS cells. First, we compared their relative efficacy, the maximal responses after normalized to the maximal responses of zaprinast obtained using both DMR and Ta
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In the present study we conducted a search for
2022-02-22

In the present study, we conducted a search for other possible endogenous ligands for GPR35. We focused on lysophospholipids because of the homology (30%) between GPR35 and GPR55 whose endogenous ligand is lysophosphatidylinositol (LPI) [9], especially 2-arachidonoyl LPI [10]. Notably, the GPR35 gen
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A high throughput screening campaign of the
2022-02-22

A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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br Acknowledgments This work was supported by the Slovak
2022-02-22

Acknowledgments This work was supported by the Slovak grant agency VEGA, Grant 2/0084/13. We would like to thank Dr. J. Bauer for careful reading of the manuscript. Introduction Glycine is an important neurotransmitter which regulates both Ac-DEVD-AFC receptor inhibitory neurotransmission and
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To date glycine receptors have been found in
2022-02-22

To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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br Material and methods br Results br Discussion
2022-02-22

Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new Phosphatase Inhibitor Cocktail 2 (100X in ddH2O) with different struc
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Griseofulvin In this study we investigated
2022-02-22

In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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A number of models have been proposed
2022-02-22

A number of models have been proposed in order to explain the mechanisms of protein transport through nuclear pore complexes. One theory is that the transport is mediated by specific peptide signals known as NLSs. The classical NLSs are short sequences containing a high proportion of the positively
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br Results and discussion br Conclusion In the continued SAR
2022-02-21

Results and discussion Conclusion In the continued SAR study of our previous heterocycle scaffolds represented by luteolin receptor 2, we focused especially on improving their drug-like physicochemical properties directed by lipophilicity, LE and LLE. After explored several heterocyclic scaff
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The other type of cell death that occurs in activated
2022-02-21

The other type of cell death that occurs in activated T Sodium ascorbate is caused by growth factor withdrawal following TCR-mediated activation, whereby most of the activated T cells die by apoptosis following the eradication of bacteria during an acute infection in order to reduce the level of cyt
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A second site of histone core domain acetylation that
2022-02-21

A second site of histone core domain acetylation that that has been observed on newly synthesized histones is histone H4 lysine 91 [34]. H4 lysine 91 lies along the interface between the H3/H4 tetramer and the H2A/H2B dimers. In fact, H4 lysine 91 normally forms a salt bridge with an aspartic Hydrox
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Histamine which was used as the agonist
2022-02-21

Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct
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br Introduction Histamine stored in mast cells and basophils
2022-02-21

Introduction Histamine stored in mast cells and basophils has been recognized as one of the most critical mediators in allergic reactions and plays an important role in eliciting the nasal symptoms of allergic rhinitis, such as sneezing, nasal itch, pain, rhinorrhea, and congestion [1], [2]. It i
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br Methods br Transfollicular penetration
2022-02-21

Methods Transfollicular penetration of herbs and their active constituents used for hair loss treatment The transfollicular administration of pharmacologically active molecules is recognised as a significant element for therapeutic interest, mainly with regard to delivery to specific sites of
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Selective pharmacological inhibition of tonic currents indic
2022-02-21

Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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