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To maintain low Glu concentrations in the synaptic
2022-05-16
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino dpat is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and in to a
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In order to discover novel small molecule compounds with
2022-05-16
In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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Epinephrine responses to hypoglycemia are probably triggered
2022-05-16
Epinephrine responses to hypoglycemia are probably triggered centrally, perhaps with input from peripheral hypoglycemia sensing [3], [4]. We observed increased epinephrine responses in GCK-MODY and I366F diabetic mice. Consistent with a role for fgfr inhibitor GCK in detecting a low blood glucose, w
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br Glucocorticosteroid receptor structure and
2022-05-16
Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,
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prostaglandin receptors Ghrelin receptors in non mammals are
2022-05-16
Ghrelin receptors in non-mammals are reportedly more “complicated/complex and diverse” than in mammals, having additional paralogs and splice variants (Kaiya et al., 2014). Several teleost fish GHS-Rs have been identified; however, functional characterization has been conducted in only a few (see, K
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Seizures in turn selectively modulate
2022-05-16
Seizures, in turn, selectively modulate the L-703,664 succinate of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could ha
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A relatively independent review of the history of the
2022-05-16
A relatively independent review of the history of the discovery of GABA (and L-glutamate) as neurotransmitters in the CNS can be found in ‘When and why amino acids?’ in the in 2010 by Kresimir Krnjevic , who spent a post-doc in Canberra in 1956–1958. Introduction The insect RDL GABA receptor is
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LXRs are physiological regulators of cholesterol
2022-05-16
LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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In summary PPARG and FFAR are connected in several
2022-05-16
In summary, PPARG and FFAR1 are connected in several ways, and the presented interaction is mechanistically reasonable. Additional investigations are required to elucidate the exact details of the underlying physiology. However, our findings are of immanent importance for the treatment of type 2 dia
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NMR analyses support the above statement Compound is
2022-05-16
NMR analyses support the above statement. Compound 32 is an interesting example of an isosteric analog of compounds 12–14. It has been demonstrated that 32 forms a rather stable six-membered ring via a hydrogen bond based on the chemical shift of the phosphorus Radicicol at the C-3 position as illu
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br Experimental br Results and discussion One of
2022-05-16
Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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In this review we focus
2022-05-16
In this review, we focus on the structure and function of the KDM4A protein, its role in cancer development, and the importance of this enzyme as a therapeutic target. For further review of the KDM4 family, see Shi et al., Whetstine et al., and Berry et al. , , . KDM4A protein structure and enzymol
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Introduction Post translational modifications to the N termi
2022-05-16
Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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Acknowledgements br Introduction Histamine mediates
2022-05-16
Acknowledgements Introduction Histamine mediates various physiological functions and pathological actions through its interactions with histamine receptors that belong to the superfamily of seven transmembrane G-protein-coupled receptors (GPCRs) (Haas et al., 2008). Four histamine receptor subty
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br Membrane Fusion Requires Rab GTPases Tethers and
2022-05-13
Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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