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Lipid sensing GPCRs as therapeutic targets
2022-01-12

Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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In summary our findings support the hypothesis
2022-01-12

In summary, our findings support the hypothesis that activation of GPR55 protects against deficits in neurogenesis induced by inflammatory insult both in vitro and in vivo through direct targeting of NSCs. Better understanding of the mechanisms by which GPR55 provides neuroprotection is critically n
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To assess the roles of GPR and GPR
2022-01-12

To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) T7 High Yield RNA from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh120
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br Introduction Over the past two decades the prevalence
2022-01-12

Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life
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Acknowledgements br Introduction The neurotransmitter glycin
2022-01-12

Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is
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br NMDA receptor LBDs The
2022-01-11

NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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Acarbose and voglibose the classic glucosidase inhibitors
2022-01-11

Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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Seizures in turn selectively modulate the
2022-01-11

Seizures, in turn, selectively modulate the SB-334867 free base sale of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 cou
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Development of few more dihydroxy
2022-01-11

Development of few more dihydroxy-pyrimidine and N-methylpyrimidone analogues as HIV-integrase inhibitors was attempted involving substitution of variety of five- and six-membered rings via the introduction of a simple methyl substituent in the α-position of the C-2 side chains in order to improve p
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This study is intriguing for
2022-01-11

This study is intriguing for several reasons. For acute pancreatitis and acute hepatitis, the early impact of inflammatory cell activation has recently been highlighted and macrophages seem to play a critical role in the disease initiation and severity., , To activate the NLRP3 inflammasome, a 2-ch
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Fludara br Differences among flavivirus vaccines and
2022-01-11

Differences among flavivirus vaccines and implications for CD4 T cell immunity There are currently three classes of flavivirus vaccines in use – live-attenuated virus (for immunoprophylaxis against YF and JE), whole inactivated virus vaccines (JE, TBE) and chimeric vaccines (JE, DEN). The chimeri
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In vertebrates three cognate receptors or receptor
2022-01-10

In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino nsc libra
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We started our investigation by
2022-01-10

We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition.
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We and others have previously reported that neurons generate
2022-01-10

We and others have previously reported that neurons generated from iPSCs with genetic forms of AD recapitulate aspects of the disease, including increased Aβ peptide production in trisomy 21 and APP duplication neurons (Moore et al., 2015, Israel et al., 2012) and increased production of longer form
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Among sensitizers tested in the previous study
2022-01-10

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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