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Natural product based drug discovery can be enhanced
2022-01-04

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in TW37 binding assays, we used molecular modeling to predict how well these compounds fit th
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Magtanong et al have demonstrated that MUFAs
2022-01-04

Magtanong et al. (2019) have demonstrated that MUFAs induce a ferroptosis-resistant state in cells in an ACSL3 (acyl-CoA synthetase long-chain family member 3) dependent manner. They observed that MUFAs did not increase the expression of GPX4, which opposes ferroptosis. However, they blocked plasma
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Liver and muscle isozymes have
2022-01-04

Liver and muscle isozymes have been found in vertebrate tissues [2], [5], [6]. The liver FBPase is recognized as a regulatory enzyme of gluconeogenesis. The muscle isozyme participates in the glycogen synthesis from lactate and in the regulation of glycolysis [7], [8], [9]. The basic difference betw
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The GPR receptor is also emerging as an important
2022-01-03

The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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mCAP With an ever increasing incidence rate of type
2022-01-03

With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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In addition to the role of
2022-01-03

In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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To determine the functional consequences of HIV
2022-01-03

To determine the functional consequences of HIV gp120 binding to vaginal epithelial cells, an annotation clustering of the differentially expressed genes was performed. The top enriched biological processes included an inflammatory immune response, defense response and the pathways included the SODD
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Molidustat br Acknowledgements Support provided by
2022-01-03

Acknowledgements Support provided by projects PTDC/SAU-MIC/115178/2009 and PEst-OE/QUI/UI0612/2011 from the Fundação para a Ciência e a Tecnologia, Portugal. Diabetes Mellitus Diabetes mellitus is a chronic, multisystem metabolic disorder caused by a combination of environmental and genetic f
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br Experimental br Results and discussions br
2022-01-03

Experimental Results and discussions Conclusions In this work, a novel label-free ECL biosensing method was developed to detect TDG activity using signal amplification strategy of HCR which was triggered by DNA functionalized AuNPs. The label-free ECL biosensing platform has been constructe
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Although we showed that RBL H
2022-01-03

Although we showed that RBL-2H3 Sc98 o6 took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SERT for se
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Based on the molecular weights of glutamate g
2022-01-03

Based on the molecular weights of glutamate (147.13 g/mol) and MSG (169.111 g/mol), the amount of free glutamate intake obtained in this study was equivalent to 297 mg MSG/d and 370 mg MSG/d for children and adults, respectively. Several previous studies have assessed population intake of MSG from f
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The effects of GHS R a blockade on
2022-01-03

The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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br Results and discussion The synthesis of
2022-01-03

Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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br Acknowledgement This research was
2022-01-03

Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral Argatroban is the most popular administration route due to good patients’ com
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br Drugs approved or in development To date three
2022-01-03

Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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