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Corresponding to the different insulinotropic signaling the
2021-09-18
Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Chlorpromazine HCl on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for ful
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Through the analysis of various synthetic
2021-09-18
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic N6-Methyl-ATP motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering
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In principle an ideal Fenton reaction element should
2021-09-18
In principle, an ideal Fenton reaction element should have multiple oxidation states to form a redox cycle in the process of H2O2 decomposition to HO•. Although iron is very effective in catalyzing Fenton reaction, it requires a low pH value (pH 2-4) to reach the optimal catalytic efficiency, which
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To date the underlying mechanism of ropivacaine in inducing
2021-09-18
To date, the underlying mechanism of ropivacaine in inducing neurotoxicity remains unclear. Cell death was intimately involved in local-anesthetic neurotoxicity [6,18]. Two classic signaling pathways triggered cell death: the extrinsic pathway and the intrinsic pathway [12]. Our study demonstrated t
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br Acknowledgments This research was
2021-09-18
Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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According to the implication of the
2021-09-18
According to the implication of the endocannabinoid system in IBD, we decided in our laboratory to develop selective CB agonists and FAAH inhibitors to treat these diseases. Recently, we described 3-carboxamido-5-aryl-isoxazoles as selective CB agonists. This series of isoxazoles possesses a 2-subst
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To date three other allosteric binding sites
2021-09-18
To date, three other allosteric binding sites of HIV-1 IN have also been reported. In the work of Wielens and co-workers [33], a pocket formed by the residues Tyr83, Trp108, Asn184, Ile200 and Val201 was found, which can be bound by small molecules. In the work by Rhodes et al. [34], a small-molecul
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Evidence demonstrating the interplay between hypoxia and the
2021-09-18
Evidence demonstrating the interplay between hypoxia and the dynamics of histone methylation is mounting [15], [43]. For example, hypoxia leads to an increase in H3K4me3 by inhibiting their responsible demethylase [44]. Hypoxia also leads to an increase in H3K9me2 by upregulating the methyltransfera
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HCV is a highly diverse virus with seven known
2021-09-18
HCV is a highly diverse virus with seven known genotypes (GT1–7) and multiple subtypes (Gower et al., 2014, Messina et al., 2015, Smith et al., 2014). Patients infected with HCV develop a heterogeneous population of viral species known as quasispecies due to low fidelity of the RNA-dependent RNA pol
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Posttraining memory facilitation by histamine infused into t
2021-09-18
Posttraining memory facilitation by histamine infused into the dorsal hippocampus was also observed in two more recently described and very important non-aversive forms of memory: object recognition (da Silveira, Furini, Benetti, Monteiro, & Izquierdo, 2013) and social recognition (Garrido Zinn et a
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Allergic rhinitis characterized by inflammation of the
2021-09-18
Allergic rhinitis, characterized by inflammation of the nasal membrane, results from an over-activated immune system exposed to 9-Phenanthrol in sensitized individuals, and is associated with nasal congestion, rhinorrhea, sneezing, and pruritus. As histamine is a key mediator in triggering allergic
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In humans polymorphisms in the lengths of GT sequences from
2021-09-18
In humans, polymorphisms in the lengths of GT sequences (from 11 to 40) within the HMOX1 promoter impact the magnitude of HO-1 expression profiles. Long GT repeats code for less stable (Z-conformational) DNA with blunted transcriptional activity resulting in lower resting and stimulated HO-1 protein
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Roflumilast br Discussion Regulation of redox homeostasis is
2021-09-18
Discussion Regulation of redox homeostasis is critical in the maintenance of normal cell functions, and both glutathione S-transferase and peroxiredoxin enzymes are important contributors to this process. There are numerous reports of aberrant expression patterns of GSTP linked with cancer and wi
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br Results br Discussion ER and GR play opposite phenotypic
2021-09-17
Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in
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Data were collected using a Powerlab and Chart
2021-09-17
Data were collected using a Powerlab and Chart 5 software (ADInstruments, Bella Vista, NSW, Australia) and were analysed using GraphPad Prism 5 (GraphPad Software, San Diego, CA). Responses to ghrelin receptor agonists in phenylephrine, methoxamine, endothelin-1, U46619 and 60mM [K+] contracted vess
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