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The potential therapeutic actions of GHSR in the central
2021-11-01

The potential therapeutic actions of GHSR in the central nervous system has been in the limelight lately. Peripheral administration of GHSR agonists have been shown to inhibit oxidative stress, apoptosis, proinflammatory cytokine production, microglia activation, mitochondrial dysfunction, and excit
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Ghrelin readily crosses the blood brain barrier Banks et al
2021-11-01

Ghrelin readily crosses the blood Lapatinib barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al., 2011, Schele et al., 2016, Skibicka et al.
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Hydantoin in region F bridging
2021-11-01

Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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mu receptor antagonist Glucose induced nuclear translocation
2021-11-01

Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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br Materials and methods br Results To examine
2021-11-01

Materials and methods Results To examine the apoptosis in FLS in vitro, we measured the number of ion channels in early apoptosis (Annexin V+, 7-AAD−) and late apoptosis/necrosis (Annexin V+, 7-AAD+) using flow cytometry after incubation with or without stimulating Fas antibody. In the absenc
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We characterized the enzyme corresponding to N FPP was the
2021-11-01

We characterized the enzyme corresponding to N1. FPP was the most effective substrate as allylic diphosphate, and the activities with GPP and DMAPP were 50% and 11% that with FPP, respectively. The analysis of the prenols resulting from the treatment of prenyl diphosphates with histamine-2 receptor
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In studies described earlier IRL was administered intravenou
2021-11-01

In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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br Acknowledgement The authors would like to thank the
2021-11-01

Acknowledgement The authors would like to thank the University of Johannesburg and the National Research Foundation for the financial support. Mr. D Harris and Dr. R Meyer from Shimadzu South Africa are thanked for their technical support. Prof Ian Dubery is thanked for access to the LC-MS instru
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Apicidin australia The stability and function of
2021-11-01

The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m
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In three independent groups identified GPR A HM A
2021-10-29

In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niacin
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Inhibitors against the proteasome a component
2021-10-29

Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor A23187, free acid sale and were show
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In this study an galactosidase gene GalA from
2021-10-29

In this study, an α-galactosidase gene, GalA, from a Aspergillus oryzae strain RIB40 [14] was artificially synthesized. To produce high levels of secretory expression in Pichia and facilitate its industrial application, we systematically investigated the gene dosages and the role of the ERSAs, namel
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The NGS of six Southern Brazil patients revealed three diffe
2021-10-29

The NGS of six Southern Brazil patients revealed three different variants: c.472C > T (p.Arg158Trp); c.958G>A (p.Gly320Arg) and c.986T>C (p.Leu329Pro) (Table 2). The amino acids involved in these substitutions were evolutionarily conserved in different species (Fig. 1B). The amino 4716 synthesis in
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Dysregulation of the HPA axis resulting in alteration to
2021-10-29

Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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br Conflicts of interest br Acknowledgments
2021-10-29

Conflicts of interest Acknowledgments This work was supported by the Project of Huzhou Municipal Science and Technology Bureau of Zhejiang Province (No. 2016GY45 to YGC) and he Project of Zhejiang Basic Public Benefit research of Zhejiang Province (No. LGF18H160005 to YGC) Introduction Wit
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