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In conclusion we have identified
2022-06-13
In conclusion, we have identified ten novel GPCR genes and a pseudogene. Transcripts for GPR78, GPR81, GPR94, GPR95, GPR101, GPR103 and P2Y were detected in various CNS and peripheral tissues. Given the high levels of identity observed within paralogous oGPCR gene clusters, future efforts will likel
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Our synthetic approach to GPR
2022-06-13
Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic AH 7614 to 4-piperidone by first forming the ac
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Recently an increasing number of studies have highlighted th
2022-06-13
Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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br GPR is a class A GPCR expressed on pancreatic
2022-06-13
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Remodelin receptor which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated
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Considering the fact that OCL induced depletion
2022-06-13
Considering the fact that OCL induced depletion of T CCG 203971 in non-stimulated cultures, the only possible explanation of this effect is the elevated mortality of these cells. It was found that OCL at the higher concentration induced the apoptosis of CD4+ and CD8+ T cells. These results strongly
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It is interesting to note that
2022-06-13
It is interesting to note that GlyT1 and GlyT2 are modulated in a coordinated and opposite way as that shown in this work by different mechanisms and situations. An example is the purinergic control of GlyT1 and GlyT2 through P2Y receptors in brainstem and spinal cord neurons. This mechanism promote
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br Introduction Glycoproteins represent a staggeringly small
2022-06-13
Introduction Glycoproteins represent a staggeringly small fraction of proteins analyzed by high-resolution techniques despite high concentrations at the cell surface and critical roles in many human diseases. Though one-half or more of all human proteins are predicted to contain a carbohydrate ch
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HSOR belonging to the aldoketo reductase superfamily is a ra
2022-06-13
3α-HSOR, belonging to the aldoketo reductase superfamily, is a rate-limiting enzyme for the synthesis of 3α-reduced steroids, such as allopregnanolone and tetrahydrodeoxycorticosterone. 3α-HSOR was extensively expressed in the spinal dorsal horn and was upregulated following peripheral nerve injury,
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To get a broader view of the
2022-06-13
To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat Alda 1 receptor and confirm the inhibition of this inte
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The primary requirements of an ideal bioprobe for glucose tr
2022-06-13
The primary requirements of an ideal bioprobe for glucose transporter-mediated bioimaging include high specificity, sensitivity as well as low cytotoxicity [18]. According to these concepts, we recently reported the simple amide linked glycoconjugates which containing cyanine fluorophores (Cy3 and C
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HOSu synthesis br Experimental section br Introduction Fasti
2022-06-13
Experimental section Introduction Fasting hyperglycaemia in all forms of diabetes mellitus occurs primarily as a result of upsurge in hepatic glucose synthesis (HGS) [1], [2]. Two specific enzymes, glucokinase (GK) and glucose-6 phosphatase (Glu-6-Pase) play crucial role in hepatic glucose pro
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Disuflo Cy5 azide br Results br Discussion Our cardiomyocyte
2022-06-13
Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR Disuflo Cy5 azide mouse model using GR-floxed mice w
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These data suggest that the dehydration of the
2022-06-13
These data suggest that the dehydration of the SSRBCs induced by RANTES might result of an activation of the Gardos channel mediated by the chemokine receptor DARC. However, direct evidence of Gardos channel activation by chemokines in Duffy-positive SSRBCs leading to cell dehydration has not been e
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br Materials and methods br Results and discussion br Conclu
2022-06-10
Materials and methods Results and discussion Conclusion Altogether, our data provide an unexpected insight into Cx26 trafficking pathway and gap junction assembly in the cochlea. Since many of the disease-causing mutations in GJB2 impair the trafficking and delivery of Cx26 to the cell surf
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We next determined the selectivity profile of the most poten
2022-06-10
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty 8602 receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity to medium- and
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