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Calcium mobilization FLIPR assay CHO
2022-08-26
Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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enkephalin mg br TGR Agonists br FXR TGR Dual
2022-08-26
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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The facts mentioned above indicate that glycine
2022-08-26
The facts mentioned above indicate that glycine function in brain is tightly regulated or pathologically altered mostly by glycine transporters. Modification of cytosolic regions of transporters, which interconnect them with intracellular regulatory pathways, could be one of the ways to provoke brai
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Enzyme linked immunosorbent assay ELISA
2022-08-26
Enzyme-linked immunosorbent assay (ELISA) is a rapid and simple test widely used for the detection of humoral immune responses following infection/vaccination. However, commercially available ILTV ELISA use the whole virus as the detecting antigen and therefore may not be sensitive for the detection
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To study the effects of
2022-08-26
To study the effects of GPR40 at the whole-animal level, GPR40 mice have been generated in two different genetic backgrounds [18], [19]. GPR40 mice from both backgrounds were apparently healthy with no overt signs of metabolic or other abnormalities. As expected, pancreatic islets taken from GPR40 m
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Accordingly it is tempting to speculate that the maintenance
2022-08-26
Accordingly, it is tempting to speculate that the maintenance of a stimulus representation in the A2 state for a short period of time after the presentation of a specific stimulus (i.e. self-generated priming) may rely upon GluR-A-dependent synaptic plasticity. If this were the case, GluR-A UNC 063
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Ghrelin receptors in non mammals
2022-08-25
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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br Experimental br Results and
2022-08-24
Experimental Results and discussion First of all we had to choose suitable electrolyte´s system. We utilized advantageously the composition of the background electrolyte for biogenic amines separation published in our work [13] to which we adapted the leading and terminating electrolytes. With
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br General aspects of HDACs br General
2022-08-24
General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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G protein coupled receptor kinases GRKs are
2022-08-24
G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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Given the role that activation of GC C has
2022-08-24
Given the role that activation of GC-C has in stimulating fluid secretion in the intestine, attempts have been made to exploit this pathway to relieve symptoms of chronic constipation. Currently, an orally administered synthetic ST mimic, linaclotide [29], has been successfully shown to alleviate co
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The identity of organelles is defined by
2022-08-24
The identity of organelles is defined by a particular set of molecules present on their surface. Most organelles in the endomembrane system (i.e., endoplasmic reticulum, Golgi apparatus, endosomes, and lysosomes) carry Rab GTPases (hereafter referred to as Rabs), which serve as binding platforms for
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GSTP is a class Glutathione S transferase
2022-08-24
GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting Dronedarone against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate carcinogen
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br Cholecystokinin CCK CCK is secreted
2022-08-24
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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Lactate induced GPR activation was confirmed
2022-08-24
Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within
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