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Prior to cellular uptake studies of compound docking simulat
2022-10-12
Prior to cellular uptake studies of Cy7 NHS ester , docking simulation was performed (A). The result suggested this complex was capable of binding in the cavity of an outward open XylE. The orientation of the sugar moiety in the docked complex was similar to that of the glucose unit bound in the cr
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As our earlier study investigated glut mRNA levels in
2022-10-12
As our earlier study investigated glut mRNA levels in response to a protein load contained in a meal and the studies that used glucose and insulin injections did not examine GLUT expression, this study sought to investigate the effects of hyperglycaemia and insulin on mRNA levels in the spiny dogfis
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br Summary br Acknowledgement br
2022-10-12
Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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Moreover we examined inhibition of GLI
2022-10-12
Moreover, we examined inhibition of GLI-mediated mRNA expression by 1. Colubrinic mimosine (1) inhibited the mRNA production of PTCH in PANC1 cells in the dose-dependent manner. This result clearly shows 1 inhibits GLI-mediated transcription (Fig. 6). Discussion In this study, we identified thre
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C598-0466 The usefulness of GIP R antagonism
2022-10-12
The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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br Acknowledgments We would like to acknowledge Jenna
2022-10-12
Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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Though regulation of ghrelin interaction
2022-10-11
Though regulation of ghrelin interaction with GHSR has not been described previously, a precedent for a similar regulatory mechanism exists in the form of the interaction between Agouti-Related Protein (AgRP) and melanocortin receptor subtypes MC3R and MC4R (Ollmann, 1997). AgRP is produced by hypot
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Although GABA C receptors were originally described in the s
2022-10-11
Although, GABA-C receptors were originally described in the spinal cord [16], clues to their physiological function arise mainly from studies in the visual system [5], [26]. In mammals, GABA-C receptors are found abundantly in cone photoreceptors and bipolar cell axon terminals, where they participa
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br Short Communication Free fatty acid receptors FFAR play
2022-10-11
Short Communication Free fatty Heme Colorimetric Assay Kit receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2
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Considering together the conformational docking and SAR resu
2022-10-11
Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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Erythropoiesis involves the proliferation and differentiatio
2022-10-11
Erythropoiesis involves the proliferation and differentiation of hematopoietic stem DAPTinhibitor to mature RBCs. This process is a tightly-regulated to adjust rates of RBC production based on physiologic need. Fas-mediated apoptosis is one mechanism that controls erythropoiesis. The role of Fas-si
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In the present study we investigated the mechanisms underlyi
2022-10-10
In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip
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Literature review suggests a strong presence of central hist
2022-10-10
Literature review suggests a strong presence of central histaminergic transmission in the teniposide areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in the bra
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br Regulation of HO expression
2022-10-10
Regulation of HO-1 expression under conditions of ischemic cardiac damage Heart is a vital organ with high metabolic demand, rich in mitochondria and it is very vulnerable to oxidative damage [85]. Disruption in coronary blood flow following MI leads to hypoxia (a reduction in the amount of avail
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Studies utilising GPR mice however report different
2022-10-10
Studies utilising GPR55−/− mice, however, report different effects of GPR55 on body weight and insulin sensitivity. Genetic deletion of GPR55 appears to have no effect on overall body weight 5, 6, 7. However, one of these studies found increased fat deposition and insulin resistance in GPR55−/− mice
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