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Finally our work showed that HAART resulted in significant i
2022-03-23
Finally, our work showed that HAART resulted in significant inter-individual variability among DEGs, which reflected the 3787 receptor in HIV-affected human gene expressions (Fig. 1, Fig. 2, Fig. 3, Fig. 4). These observations also highlighted the importance of determining common as well as persona
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The compounds described in this paper
2022-03-22
The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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SAR around amino derivative revealed a number of
2022-03-22
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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Similar to GPR A activation
2022-03-22
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic neomycin sulfate receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al., 196
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The expression of heat shock proteins HSPs can
2022-03-22
The expression of heat-shock proteins (HSPs) can be upregulated by viral infection, nutritional deficiency, TNF-α and oxidative stress in Paeonol [44], [45] HSPs are classified in six families (including the HSP10, HSP40, HSP60, HSP70, HSP90 and HSP100 families). HSP90 [46] for example provides a na
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In addition to vertebrate species GnRH has been identified
2022-03-22
In addition to vertebrate species, GnRH has been identified in invertebrates, such as in the Protochordate Ciona intestinalis (Powell et al., 1996; Adams et al., 2003), the decapods mollusk Octopus vulgaris (Iwakoshi et al., 2002), the gastropod mollusk, the sea hare Aplysia californica (Zhang et al
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Introduction The West syndrome or epilepsy with epileptic
2022-03-22
Introduction The West syndrome or epilepsy with epileptic spasms (ES) is an epileptic encephalopathy in early infancy with probable seizure-related developmental regression. According to the United Kingdom Infantile Spams Study (UKISS), common causes of infantile spasms include hypoxic-ischemic enc
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Unfortunately the approved drugs suffer from failure in
2022-03-21
Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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We are pursuing a hit to lead medicinal
2022-03-21
We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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In this precancerous condition though cancer develops from t
2022-03-21
In this precancerous condition, though cancer develops from the epithelium, the subepithelial connective tissue also play crucial biological role in pathogenesis and progression to malignancy. In this context it may be noted that some recent reports addressed the problem of the mechanical interactio
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Compared with the tetrazole derivative the potency of analog
2022-03-21
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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Reduction of the hydrolysis of ATP is
2022-03-21
Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct
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Racemic protein crystallography has been
2022-03-21
Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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br Conclusion The following is the
2022-03-21
Conclusion The following is the supplementary data related to this article. Conflict of interest Funding Acknowledgements Peroxiredoxin VI (Prdx6) is a dual-functioning antioxidant enzyme that acts to protect biological membranes against damage caused by lipid peroxidation , . The enz
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In addition to their functional activation of GPR
2022-03-21
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic Probucol to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unlab
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