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Synthesis of and is described
2021-04-28

Synthesis of 5–7, 12–14, and 18 is described in Scheme 3. Compounds 5–7 and 18 were prepared as outlined in Scheme 3a. Reaction of 4-bromomethylbenzoic glutathione reductase (36) with thionyl chloride yielded the corresponding acid chloride, which was converted to the corresponding amide 40a by the
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br Summary and perspectives In
2021-04-28

Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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Clofibric Acid Most remarkably an essentially identical coll
2021-04-28

Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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br Acknowledgements We thank Dr James Ritchie and his dedica
2021-04-28

Acknowledgements We thank Dr. James Ritchie and his dedicated staff (Deptartment of Pathology, Emory University) for performing measures of serum VPA levels; Sumitomo Pharmaceuticals (Osaka, Japan) for the generous donation of DOPS, which is required for breeding Dbh −/− mice; Pfizer (Sandwich, K
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Compounds that interact with MDR can do so by different
2021-04-28

Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant Wortmannin and there was no observed reduct
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To examine the influence of aromatic motifs on
2021-04-28

To examine the influence of aromatic motifs on the bridging lysine esters we analysed DNA alkylating activity of the set of compounds 1–6. The lysine derivatives were chosen as it is relatively easy to prepare different esters and thereby study the impact of different groups on the reactivity toward
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CA-074 Me br Structure of ketosteroid dehydrogenase Overall
2021-04-28

Structure of 3-ketosteroid Δ1-dehydrogenase Overall fold — High-resolution crystal structures of Δ1-KSTD are currently available for the Δ1-KSTD1 isoenzyme from R. erythropolis SQ1 [30]. The Δ1-KSTD1 molecule has an elongated shape, and consists of two domains, an FAD-binding domain and a catalyt
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In this review we first introduce the in
2021-04-27

In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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Finally unilateral microinjection of CP Astressin B CP
2021-04-27

Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, AN
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In this study we observed
2021-04-27

In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased sphingosine 1-phosphate receptor modulator when the sensitization condition was established
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In this study a GMI of was associated
2021-04-27

In this study, a GMI of 1.0 was associated with high sensitivity above 90%, specificity below 30% and higher negative predictive value. However, this cut-off couldn't have been optimal because of the lower level of Youden J Index which was 50% of patients with culture positive sputum had a GMI >6.0.
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Antioxidants such as SFN have been proposed to be
2021-04-27

Antioxidants such as SFN have been proposed to be chemopreventive agents to inhibit, delay or reverse the development of cancer (Bayat Mokhtari et al., 2018). SFN was shown in breast epithelial cell culture to suppress oxidative metabolism of E2/E1 and thus protect against estrogen-mediated DNA dama
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The immune control of CMV replication in vivo is primarily
2021-04-27

The immune control of CMV replication in vivo is primarily driven by the T-cell-mediated response, a characteristic that has been proposed as a tool to individualize and therefore to optimize antiviral treatment [6], [7], and it has been associated with spontaneous clearance of CMV viraemia in patie
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The results of physical parameters of the prepared samples a
2021-04-27

The results of physical parameters of the prepared samples are summarized in Table 2. The equivalent diameter ranged from 1.09 to 1.14 mm, which is within the required size distribution of 0.8–1.25 mm. A slight increase in size is probably caused by increasing the thickness of the second coat. To d
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What is the predominant mechanism underlying the
2021-04-27

What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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