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In our current work we have undertaken liquid
2020-03-09
In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised AMG 337 were also screened by molecular docking studies over the reported hDHODH structure. The synthesised mole
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Our data show a site specific interaction of DDR
2020-03-09
Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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On the other hand the death domain is a conserved
2020-03-09
On the other hand, the death domain is a conserved stretch of around 80AA which is commonly found in death receptor proteins, it play a major role in the interaction between other proteins. Also as a platform for the death-inducing signaling complex (DISC) formation (Chaigne-Delalande et al., 2008).
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br Materials and methods br Results br Discussion CHIKV is
2020-03-09
Materials and methods Results Discussion CHIKV is an important arthropod borne virus with substantial impact on global health and cause a major viral disease that requires the development of antiviral drug to combat chikungunya disease. Virus specific proteases have particularly become an a
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br Conclusions Present work comprehensively characterizes th
2020-03-09
Conclusions Present work comprehensively characterizes the inhibitory activity of Yersinia enterocolitica against cysteine proteases. All tested strains, regardless of their bioserotype, genotype and the presence of virulence markers, synthesized the high-molecular-weight inhibitors of papain and
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We neither observed changes in
2020-03-09
We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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br Materials and methods br Results br Discussion
2020-03-09
Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc
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To characterize Ea and S DC AC
2020-03-09
To characterize Ea and γ·S, DC/AC electrical parameters will be determined from MIL standard measurements in a temperature range of −55 to +200°C. It is therefore necessary also to characterize the junction temperatures and hot points by infra-red or electrical method. The accelerated aging, represe
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In cholesterol synthesis HMG CoA reductase is the rate
2020-03-09
In cholesterol synthesis, HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins or HMG-CoA reductase inhibitors are commonly used for management of hypercholesterolemia. The presence of an HMG-like moiety on these drugs allows them to competitively bind to the catalytic do
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br Results br Discussion In this study we
2020-03-07
Results Discussion In this study, we have determined the pathway by which the 3ʹ end of the nascent leading strand is connected with CMGE after priming, revealing that Pol δ likely plays a crucial role in establishing all continuously synthesized leading strands at eukaryotic replication origi
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Compound was generated using a literature procedure and requ
2020-03-07
Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to 5(S),6(R)-7-trihydroxymethyl Heptanoate
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ERR and ERR share high sequence homology at their DNA
2020-03-07
ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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The isomeric phenyloxazole not only exhibited increased pote
2020-03-07
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 iniparib (as seen in compound pairs – and –) decreased ACE
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br Introduction Concern has been raised over
2020-03-07
Introduction Concern has been raised over free estrogens (estrone [E1], 17ß-estradiol [E2] and 17α-ethynylestradiol [EE2] particularly) in the past decade due to their endocrine disrupting effects on environmental biota [1], [2]. Estrogens are excreted by vertebrates primarily as sulfate or glucu
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br Introduction Concern has been raised over
2020-03-07
Introduction Concern has been raised over free estrogens (estrone [E1], 17ß-estradiol [E2] and 17α-ethynylestradiol [EE2] particularly) in the past decade due to their endocrine disrupting effects on environmental biota [1], [2]. Estrogens are excreted by vertebrates primarily as sulfate or glucu
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