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br Transparency document br Acknowledgments This work was
2021-08-20

Transparency document Acknowledgments This work was supported by the Ministry of Education, Youth and Sports of the Czech Republic (the National Program of Sustainability I, Grants LO1204 and LO1304), by the Czech Science Foundation (15-17282Y) and by Palacký University Olomouc (IGA_PrF_2017_0
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First we synthesized inhibitor following the
2021-08-20

First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidin
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The synthesis of tricyclic analogs is described in
2021-08-20

The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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Various domains of the HSA molecule have
2021-08-20

Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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From the results of previous experiments with the purvalanol
2021-08-20

From the results of previous experiments with the purvalanol B affinity matrix, it is not clear whether the selective capture of parasite CK1 enzymes is a reflection of their high abundance or rather their affinity for the ligand compared with other kinases present in the lysates. Based on compariso
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ERR is present early in the developing
2021-08-20

ERRβ is present early in the developing placenta in a subset of FSLLRY-NH2 in extra-embryonic ectoderm destined to make up the chorion.19, 20 ERRβ is likely essential for reproduction. ERRβ expression is essential for the maintenance of pluripotency and self-renewal potential in mouse embryonic ste
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In the present study we
2021-08-20

In the present study, we found that the up-regulatory effects of androgens on ep1 transcripts might be mediated by Arα in the olfactory rosette of B. sinensis. However, in mammals, there is no evidence of AR expression in either the vomeronasal organ or the sensory epithelium of main olfactory epith
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PI K is a lipid
2021-08-19

PI3K is a lipid kinase and generates phosphatidylinositol-(3,4,5)-trisphosphate, which is a second messenger critical for the translocation of Akt to the cytoplasmic membrane. The phosphorylation of Ser473 Akt is important in the cell survival by regulating the eNOS among other targets (Dimmeler et
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Dual inhibition of ACE and NEP as a strategy
2021-08-19

Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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The role of activation of xenosensor nuclear receptors
2021-08-19

The role of activation of xenosensor nuclear receptors such as PPARα, CAR, and PXR in producing hepatomegaly and liver tumors in rodents has been well-established (Klaunig et al., 2003, Lake, 2009). In the case of PPARα, the increase in liver weight results from increased peroxisomal mass and expans
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br STAR Methods br Acknowledgments We thank the City
2021-08-19

STAR★Methods Acknowledgments We thank the City of Hope core facilities, including the Animal Model Core, Bioinformatic Core, NMR Core, Flow Cytometry Core, and Florescence Microscopy Core for excellent technical support, and NIH grants R01GM086171, R01GM102538, and R01CA212119, R01CA216987, an
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It was reported that the expressions
2021-08-19

It was reported that the expressions of DPP-4 and SDF-1α increase through HIF-1α [27], [28]. Myocardial ischemia by MI enhanced the DPP-4 and SDF-1α levels in myocardium in the present study. SDF-1α is released from cardiomyocytes and has beneficial effects on cardiomyocytes through SDF-1α/CXCR4 aft
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br Synthesis and mechanism of
2021-08-19

Synthesis and mechanism of fluorescent DNA-CuNMs Application of fluorescent DNA-CuNMs Summary and conclusions In summary, we introduce recent research progress in the synthesis and various applications of DNA-CuNMs. DNA-CuNMs with novel catalytic, electrical and optical properties can be ob
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Then we explored the MCLEIA methodology parameters including
2021-08-19

Then, we explored the MCLEIA methodology parameters including precision, accuracy and specificity. In the 0.5–128 ng/mL, the standard curve equation was = 0.5014 + 1.769 ( was log, was RLU/RLU with a correlation coefficient of 0.9907) (). On the one hand, same sample (0.5, 4.0, 32.0 ng/mL) detected
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As for antiviral activity eight out of synthesized
2021-08-19

As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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