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Based on the role of NMDA receptors
2022-07-21
Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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AFB Fapy dG has been long recognized as a substrate
2022-07-21
AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by Amphotericin B excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG fr
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Entry into CNS is tightly regulated by highly
2022-07-21
Entry into CNS is tightly regulated by highly dynamic barriers, namely, the BBB, the blood-CSF barrier, and the arachnoid epithelium (Abbott et al., 2010; Yasuda et al., 2013). Similar barriers also exist within the CNS including the ependymal barrier as well as the cellular membrane barriers of the
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The bioconversion of inositol from glucose was anticipated n
2022-07-21
The bioconversion of inositol from glucose was anticipated nearly a century ago and later confirmed by isotope tracing methods [[22], [23]]. This biosynthesis of inositol involves three sequentially acting enzymes: Firstly, ATP-dependent glucokinase converts glucose to glucose-6-phosphate (G-6P) [[2
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Animal studies have shown that various antidepressant treatm
2022-07-21
Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key (R,S)-Anatabine regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate the nega
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br Acknowledgements br Introduction Glucagon a amino acid pe
2022-07-21
Acknowledgements Introduction Glucagon, a 29-amino Scrambled 10Panx peptide, is released from the pancreatic islets, intestine and stomach. Glucagon is released under hypoglycemic conditions and then elevates blood glucose levels, serving as a major counter hormone [1]. The regulation of gluc
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In addition to our results Chen et al
2022-07-21
In addition to our results, Chen et al. showed that administration of the GalR1 antagonist M40 improves cardiac function and attenuates cardiac remodeling in rats with heart failure [26]. These effects might be attributed to M40 suppression of galanin inhibitory effect on the vagal nerve in heart fa
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br Conclusions GPCRs are versatile signaling
2022-07-21
Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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Asiaticoside Recently they reported an enyne chemotype agoni
2022-07-21
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral Asiaticoside (tmax=15min) and a decent pharmacokinetic profile,
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br Materials methods br Results FAS c AA AG
2022-07-21
Materials & methods Results FAS c.-671AA, AG and GG genotypes and A and G AY 9944 dihydrochloride frequencies were similar in both patients with FMF and healthy control groups, and no significant difference was found (P>0.05, Table 1). The frequency of TC genotype in FASLG in the healthy cont
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Dual H H receptor antagonists developed by
2022-07-20
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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GSK has also been used as PET
2022-07-20
GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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br Tissue Specific Roles for
2022-07-20
Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune BMS-345541 mg and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory
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In cancer cells HIF upregulates HK II expression by
2022-07-20
In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi
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Recently some published studies showed that HBV can induce
2022-07-19
Recently, some published studies showed that HBV can induce autophagy in vitro and vivo [[19], [20], [21]]. The critical role of autophagy in HBV normal life cycle, such as HBV envelopment, has been gradually accepted by researchers from different laboratories [22,23]. HBV can trigger the autophagic
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