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Histamine which was used as the agonist had
2022-01-20

Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct
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br Results br Discussion Our current study demonstrates
2022-01-20

Results Discussion Our current study demonstrates that the sustained activation of Yap overrides the p27-mediated checkpoint, at least in part, through the degradation of FoxO family proteins, allowing polyploid cells to proliferate inappropriately with mitotic defects and resulting in centros
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BMS-911543 Diabetes and atherosclerosis are paralleled by im
2022-01-20

Diabetes and atherosclerosis are paralleled by impaired wound healing and endothelial angiogenesis in the periphery, which cause severe complications and mainly occur as a result of the elevated circulating levels of glucose and free fatty acids. Yuan et al. recently showed that palmitic BMS-911543
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br Pharmacological anti aging approaches and the
2022-01-20

Pharmacological anti-aging approaches and the Hippo pathway Aging and age-related pathologies are the main causes of disabilities and death. As Magalhañes and colleagues suggest, the challenges of developing anti-aging pharmacological therapies may, in part, be due to the complexity of aging mole
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Chlorocresol receptor br Mutagenesis and Receptor Modeling S
2022-01-19

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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We first set out to identify the minimum
2022-01-19

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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Spatial working memory improved in the Balb c strain
2022-01-19

Spatial working memory improved in the Balb/c strain at a dose of VU0410120 (i.e., 30mg/kg) that disrupted spatial working memory in the Swiss Webster comparator strain. Consistent with a recent PET study in rhesus macaques suggesting a relationship between the extent of the dose-dependent occupancy
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Tamoxifen is still the most frequently used
2022-01-19

Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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Growing evidence suggests that the glycine site seems
2022-01-19

Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it TH588 has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Moreover, mice with
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ICH induced striatal lesion produced
2022-01-19

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino Cy3-dCTP transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia (
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The manner in which various residue
2022-01-19

The manner in which various residue side chains are oriented in the active site of HsHxKIV was a driving factor for why glucosamine analogues could not bind, as we previously proposed [16]. These compounds would have difficulty managing access into the active site based on residue P153 in addition t
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Next we asked how a common activation
2022-01-19

Next, we asked how a common activation marker of fibroblasts, Acta2, defined gene expression signatures in alveolar airspaces by using Acta2-mKO1 reporter mice (Fig. 2A). In the lungs of Acta2-mKO1 mice, mKO1 was expressed in smooth muscle cells and mesenchymal cells in thapsigargin (Fig. 2B). By so
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The general aim of our
2022-01-19

The general aim of our in vitro experiments was to analyze the patterns of ghrelin and GHSR-1a expression in the mammary glands of dairy goats during pregnancy and to examine the direct effect of ghrelin on cell proliferation in cultured MECs of pregnant dairy goats. For this purpose, we cultured go
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Although NCT undergoes complex glycosylation processing for
2022-01-19

Although NCT undergoes complex glycosylation processing for maturation through trafficking from endoplasmic reticulum to Golgi or additional compartments, the effect of NCT glycosylation on γ-secretase activity and substrate specificity is still unknown. The present study focused on glycosylation st
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Gal is a amino acid residue peptide comprising amino
2022-01-19

Gal is a 29-amino prostaglandin receptor residue peptide, comprising 30 amino acids in humans, isolated from the porcine intestine 30 years ago (Tatemoto et al., 1983). It has been shown to be involved in the regulation of numerous processes, including neuroendocrine control of systems such as the
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