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CYP A is involved in the
2021-02-22

CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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To extend these toxicity minimization strategies
2021-02-22

To extend these toxicity minimization strategies to 3D tissues, a more complicated mass transfer model is necessary to account diffusion in the interstitial space, as well as transport across cell membranes. Until recently, tissue mass transport in cryobiology was modeled using classic spatially de
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Khan et al investigatedAnomalin a pyranocoumarin constituent
2021-02-22

Khan et al. investigatedAnomalin 44, a pyranocoumarin constituent of S. divaricata, which exhibits potent anti-inflammatory activity. The anomalin 44 dose-dependently inhibited inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) mRNA and protein expression in LPS-stimulated RAW 264.7
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Two additional hydrogen bonds are formed by the
2021-02-22

Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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The ACC receptor family appear to
2021-02-22

The ACC receptor family appear to be attractive targets for the development of novel anthelmintics. With this in mind we also tested the activity of the anthelmintics levamisole and pyrantel which activate the nematode nAChR (Martin and Robertson, 2007). We found both molecules were partial agonists
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br Materials and methods br Results br Discussion
2021-02-22

Materials and methods Results Discussion The effect of progestogen treatment showed some tendencies affecting the body length and weight, however these data were not verifiable statistically. This observation could be explained with the relatively short exposure period and/or the relatively
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Several questions remain to be addressed The
2021-02-22

Several questions remain to be addressed. The hormones and metabolites that modulate expression of EERγ in the steps leading to maturation need to be identified to learn more about physiological and pathophysiological regulation of EERγ in β cells. Considering that ERRγ repressed cell cycle genes in
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Although the mechanisms underlying the EP
2021-02-22

Although the mechanisms underlying the EP4-mediated increase in the frequency of mEPSCs via PGE2 remain unclear, mechanisms similar to those driven by EP2 may be involved because activation of both these receptor subtypes increases the intracellular concentration of cAMP (Nishigaki et al., 1995, Sug
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br Materials and methods br Results
2021-02-22

Materials and methods Results + discussion Conclusions We have demonstrated the systematic optimization of the functional folding of a CF synthesized GPCR. The approach addresses central issues relevant for many membrane proteins such as disulfide bridge formation, proper hydrophobic enviro
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br Effects of culture conditions on drug induced gene
2021-02-22

Effects of culture conditions on drug-induced gene Triptolide in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that are most criti
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The ability of minor groove binding agents
2021-02-22

The ability of minor groove binding agents to inhibit the activity of DNA helicases is not without precedence. Similar effective inhibition of the unwinding of DNA by the BLM and Werner's DNA helicases by the minor groove binder distamycin A has been observed. Further, and similar to RecBCD, interca
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br Experimental Procedures br Acknowledgments br Bisphenol A
2021-02-20

Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that Pimozide receptor (ER) would mediate these effects of low-dose BPA, studies revealed that BPA boun
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Several studies have shown that independently of body
2021-02-20

Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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The isomeric phenyloxazole not only exhibited
2021-02-20

The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand Direct Mouse Genotyping Kit (as seen in compound pairs – an
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In conclusion we demonstrate that infection of
2021-02-20

In conclusion we demonstrate that infection of salmon cells with ISAV induce the main branches of the cellular UPR machinery, but also one of its main negative regulators, GADD34. This is probably important for maintaining translation of interferon and interferon stimulated genes (ISGs), keeping ISA
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