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br Introduction Human immunodeficiency virus HIV is a retrov
2022-01-19
Introduction Human immunodeficiency virus-1 (HIV-1) is a retrovirus that primarily infects components of the human immune system, such as CD4+ T cells, macrophages and dendritic Amikacin disulfate (Clapham and McKnight, 2001). HIV directly and indirectly destroys CD4+ T cells, which leads to seve
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Finally we investigated increasing basicity as a
2022-01-19
Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, L-690,330 mg demonstrated significant improvement of values of solubility for the two media, especially f
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br Materials and methods br Results br Discussion Until very
2022-01-19
Materials and methods Results Discussion Until very recently, the anti-atherogenic activity of niacin was attributed almost exclusively to its impact on HDL and other plasma lipids, perhaps mediated via its action on GPR109A expressed in adipose or other tissues. However, recent clinical st
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On the other hand it is
2022-01-19
On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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br Experimental procedures br Results br Discussion Although
2022-01-19
Experimental procedures Results Discussion Although the presence and localization of the GlyR subunits have been determined in the adult retina, the proportion of each GlyR subunit has not been assessed in the adult or in the developing retina. In the present study, we carried out the absol
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The functionally crucial arginine within M is not encoded
2022-01-19
The functionally crucial arginine within M2 is not encoded by the gluR2 gene, but rather arises within the pre-mRNA by editing of a codon for the neutral glutamine residue25, 26. RNA editing at the Q/R site is specific to GluR2 and is extremely efficient. In neonatal and adult rat brain, almost 100%
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The development of immobilization techniques for
2022-01-19
The development of immobilization techniques for β-glucosidase offers a potential way to enable its reuse several times [13]. The aim of immobilization is to trap the enzyme within or on the surface of an insoluble material with retention of its catalytic activity [14]. The immobilization strategy a
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To synthesize the azaindole based compound Suzuki coupling o
2022-01-19
To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic pituitary adenylate cyclase-activating peptide was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position resulted 3-io
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Two excellent GSMs with clear pharmacological effect across
2022-01-19
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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Most of the above mechanisms are implicated in attenuation
2022-01-19
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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ep4 antagonist FXR agonists represent an attractive class of
2022-01-19
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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The improved glucose tolerance of Ffar R W
2022-01-19
The improved glucose tolerance of Ffar1R258W/R258W mice on HFD was unexpected. In combination with similar fasting blood glucose levels, the significant lower fasting plasma insulin of mutant mice compared to wild-type mice is indicative of improved insulin sensitivity. However, peripheral insulin r
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br Introduction In addition to glucose which is the foremost
2022-01-19
Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in
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PG 01037 dihydrochloride This hypothesis is in line with our
2022-01-19
This hypothesis is in line with our phylogenetic analysis of FBPase sequences which revealed that vertebrate FBP2 evolved significantly faster than FBP1 (Fig. 2). An average distance between FBP2 and ancestral vertebrate FBPase was higher than that for FBP1. Moreover, preliminary study on amphibia
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br Declarations of interest br Founding information This wor
2022-01-19
Declarations of interest Founding information This work was partially supported by the New Energy and Industrial Technology Development Organization (NEDO) Japan [grant number P03043]; and Grants-in-Aid for Scientific Research [grant number 16H00738 to H.M.] from the Japan Society for the Prom
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