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br H R agonists In search for potent
2021-12-06

H2R agonists In search for potent and selective H2R agonists, comprehensive structure–activity relationship studies have been conducted and led to the first H2R agonists, e.g. 4(5)-methylhistamine (16) which is actually now used as selective H4R agonist (Fig. 4) (Durant et al., 1975, Lim et al.,
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The transcription factor Nrf is
2021-12-06

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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In our previous study we designed and synthesized compounds
2021-12-06

In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic SB 242084 (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro antitumo
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The neotropical fish Prochilodus lineatus has been widely us
2021-12-06

The neotropical fish Prochilodus lineatus has been widely used in experimental designs for being sensitive to variations in water quality and tolerant to laboratory conditions (Camargo and Martinez, 2006, Cazenave et al., 2014, da Silva and Martinez, 2014, Vieira et al., 2016). Concern and reports a
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Apart from the different assays used biased agonism could al
2021-12-06

Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 D-erythro-Sphingosine (synthetic) stably transfected with human GPR55. They found that the effect of both ligands o
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In the present study we found
2021-12-06

In the present study, we found that the expression of GPR120 in decidua from women of spontaneous abortion was significantly downregulated compared to the decidua from that of normal pregnancy. Moreover, GPR120 deletion (GPR120−/−) or inhibition predisposed mice to LPS or RU486 induced abortion, ind
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MRS 1220 The GLU Epac transgenic mouse enabled
2021-12-06

The GLU-Epac transgenic mouse enabled us to monitor cAMP responses to GPR119 ligands in individual primary cultured L-cells. Not all L-cells were found to be responsive to AR231453, suggesting there may be a subpopulation of L-cells that do not express functional GPR119. There was a tendency for sma
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br Conclusion br Conflict of interest statement br
2021-12-06

Conclusion Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as Introduction Over the past decade, more than a hundred new biopharmaceutical products have been approved and market
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Bacterial GluRS comes in two flavors discriminatory GluRS D
2021-12-06

Bacterial GluRS comes in two flavors, discriminatory GluRS (D-GluRS) and non-discriminatory GluRS (ND-GluRS). While D-GluRS exclusively catalyses the transfer of Glu to tRNAGlu, the ND-GluRS can also glutamylate tRNAGln forming Glu-tRNAGln. The misacylated product is then transformed to Gln-tRNAGln
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Therefore as it stands presenilin has a secretase independen
2021-12-06

Therefore as it stands, presenilin has a γ-secretase-independent role in regulating protein trafficking, proteolysis and degradation, however given that inhibition of γ-secretase activity can have a negative effect on protein trafficking [69], [98], we cannot exclude the possibility that some of the
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By association a possible mechanism which may underlie the
2021-12-06

By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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bromhexine In addition several other considerations
2021-12-04

In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty bromhexine receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were com
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Senger et al performed a
2021-12-04

Senger et al. performed a retrospective review of 17 patients with ICH on dabigatran or rivaroxaban who received 4F-PCC. Eight patients had a traumatic WAY-100635 maleate salt injury (TBI) and nine patients had a spontaneous ICH. Nine patients had a devastating outcome, including severe neurologic d
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Thus both in Drosophila and mammals the Hippo pathway
2021-12-04

Thus, both in Drosophila and mammals, the Hippo pathway responds to cell–cell junctions via an apical NF2/Mer-containing complex. Indeed, Hippo signalling and NF2 are required for contact inhibition of growth in cell culture, which is thought to reflect an in vivo function as a sensor of tissue crow
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br Acknowledgments br Introduction Liver
2021-12-04

Acknowledgments Introduction Liver disease is one of the leading causes of death worldwide. Death from any type of acute or chronic liver injury results when sufficient healthy hepatic parenchyma cannot be regenerated to perform vital liver-specific functions. Although the regenerative capabil
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