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As disclosed in our preceding paper medicinal chemistry SAR
2022-06-28
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, mt t lacks an esse
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Introduction Glycine Fig has two pivotal
2022-06-28
Introduction Glycine (Fig. 1; 1) has two pivotal functions as neurotransmitter in the central nervous system (CNS). Firstly, it can act as an inhibitory neurotransmitter at inhibitory glycinergic synapses where it binds to the strychnine-sensitive glycine-A binding site on glycine receptors (GlyR)
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The kinetic data obtained from incubation of BAB with GLO
2022-06-28
The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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Given and a module N we put The
2022-06-28
Given and a -module N, we put The right hand side makes sense because we regard g as an Pam2CSK4 of and meanwhile . It is also a skew group ring, identified with via the following equation It follows that becomes a -module, with Analogous to the situation of group representations, the underlyin
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An increased sympathetic tone and the
2022-06-28
An increased sympathetic tone and the hormone glucagon are the main glucose mobilizing factors [28], [29]. Single-cell transcriptome analysis of human islet cells suggests the expression of Ffar1 not only in β-cells but also in α-cells [30]. Moreover, analysis of rat α-cells indicates that FFAR1 exp
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br Methods GLUT DS was
2022-06-28
Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF bx795 below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percentile and CSF lacta
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br Involvement of gap junctions
2022-06-27
Involvement of gap junctions and Panx1 in spinal cord processing of pain information Several studies indicated that GJs in the CNS contribute to pain. A common finding in such studies is that intrathecal administration of GJ blocker attenuates pain behavior. For example, intrathecal CBX attenuate
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G quadruplex DNA structures may exist in either
2022-06-27
G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure
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GLP is released in response to ingestion of nutrients includ
2022-06-27
GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty parp-1 receptor 4 (FFA4/GPR120) as a potential 7TM receptor involved in lon
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br Methods br Results It
2022-06-27
Methods Results It is well known that during the onset of vasoconstriction there is an increase in intracellular Ca2+ which activates myosin light-chain kinase followed by cycling of actin-myosin cross-bridges in VSMCs. Recently, it has been recognized that Nile Red sale polymerization is als
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In this study we intended to explore the efficacy of
2022-06-27
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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Over the years a number of studies
2022-06-27
Over the years, a number of studies have reported results concerning the behavior of the two endothelin receptor subtypes, ETA and ETB, that do not fit the classical model of two G protein-coupled receptors acting independently of one another. For example, in the rat anterior pituitary gland, both E
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Despite these data implicating Kdm
2022-06-27
Despite these data implicating Kdm6b as a positive regulator of neuronal differentiation, and surprisingly, given the evidence that germline knockouts die perinatally due to an inability to breathe, the brains of Kdm6b knockout mice are remarkably normal in gross morphology [26,]. Interestingly, Kdm
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To identify genes with significant expression differences we
2022-06-27
To identify genes with significant bace inhibitor differences, we performed differential gene expression analysis between the two individuals with TRRAP variants (combined as biological replicates) and two unaffected controls. Gene ontology (GO) enrichment analysis of these genes with the GOrilla w
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tlr4 mg A recent novel and important finding is that YAP con
2022-06-27
A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1
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