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Analysis of published albumin X ray structures had
2022-01-24

Analysis of published albumin X-ray structures had suggested that an allosteric link may exist, but could not establish whether Zn2+ prevented FFA binding or vice versa. This question was answered through competition experiments monitored by isothermal titration calorimetry (ITC; Fig. 3) for BSA [55
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According to Laplace s law loss
2022-01-24

According to Laplace’s law, loss of myogenic response would increase wall stress and tension in downstream vessels and subsequently induce endothelial dysfunction and arterial stiffness [36]. Indeed, we found that arteries from FPR-1 KO mice presented with a leftward shift in the stress-strain curve
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The lack of biological activity http
2022-01-24

The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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Fomepizole br Acknowledgments R Dalmann has obtained a
2022-01-24

Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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In order to establish proper folding
2022-01-24

In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both LB Broth, Miller contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top left), whereas o
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Whether histamine receptor distribution is altered in
2022-01-24

Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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For further understanding of the interaction between these
2022-01-24

For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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To investigate the simultaneous effects of
2022-01-24

To investigate the simultaneous effects of possible confounding factors in the urinary 1-OHP excretion, multivariate regression analysis was performed (Table 3). Based on stepwise regression analysis, four independent variables (age, CYP1A1⁎4, GSTM1 and GSTP1 polymorphisms) entered into the final mo
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br Materials and methods br
2022-01-24

Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic 2×Taq PCR Master Mix(with dye) is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is
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Modulation of the cannabinoid system has
2022-01-24

Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a
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br The mode of binding
2022-01-24

The mode of binding of ligands to GPR35 As noted above, although kynurenic KN-62 is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importantly, in studie
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In normal tissues the expression patterns of
2022-01-24

In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet Ion Channel Compound Library synthesis and intestinal tract [7], [20]. It is considered that
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Acknowledgments This research was supported by the
2022-01-24

Acknowledgments This research was supported by the Korea Research Institute of Chemical Technology (KRICT) funded by the Ministry of Science, ICT & Future Planning (KK1703-G00, KK1707-C05, SI1707-02, KK-1607-C09, and SKO1707C05) and a grant of the Korea Health Technology R&D Project through the Kor
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P gps expressed in cells
2022-01-21

P-gps, expressed in Sotalol and tissues of human and animals, play an active role in cellular protection against multiple toxicants by transporting them out of a cell. Thus, improving transport activity of P-gp may contribute to removing Cd from living oysters. Cd accumulation in the cultured cells
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The lactam compounds including ceftriaxone CEF
2022-01-21

The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati
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