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In the present study we
2020-09-15

In the present study, we determined concentration–response relationships for selected synthetic progestogens using in vitro luciferase transactivation assays driven by PR, ARα and ARβ from Murray–Darling rainbowfish () and compared the profiles with those obtained from similar assays based on human
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The use of recombinant ER and ER binding assays
2020-09-15

The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct DC260126 receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein production system used t
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In summary we have identified a series of amides
2020-09-15

In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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Docking experiments showed that Me MeGlcA Xyl
2020-09-15

Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same NB-598 and no new interactions were observed. The
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The main advantage of exploiting
2020-09-15

The main advantage of exploiting paper sludges as sources of cellulose-derived energy and chemicals in comparison to other lignocellulose substrates is their amenability, which is associated with an extensive pulping process that removes the majority of the lignin and exposes NVP-CGM097 fibers to e
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In addition to vasoconstrictor actions acute effects ET exer
2020-09-15

In addition to vasoconstrictor actions (acute effects), ET-1 exerts potent mitogenic actions on vascular smooth muscle cells and cardiac myocytes (chronic effects), hence causing vascular and cardiac hypertrophy [19,24,25]. These effects are mediated via stimulation of either ETA or ETB receptors, a
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The discovery of proteases that are
2020-09-15

The discovery of proteases that are active in organic solvent media has greatly extended their ability in the synthesis of useful products. Microbial proteases which are able be catalyse in non-aqueous solvents present new expectation in enzyme applications. This kind of enzymes gives a major contri
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In this study we were able derive new
2020-09-15

In this study, we were able derive new insights into the biology of DDR2 including the demonstration that cellular tyrosine phosphorylated proteins co-localise with DDR2 and exogenously added collagen I (Fig. 1G). This finding suggests that similar to the focal adhesion complexes associated with int
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In contrast T bet downregulated the expression of Tfh functi
2020-09-14

In contrast, T-bet downregulated the expression of Tfh functional molecules, CD40L, ICOS, and IL-21; accordingly, T-bet overexpression abrogated the helper function of IL-12-stimulated CD4+ T cells. Thus, T-bet seems more involved in the downregulation of the helper functions than in the differentia
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While oxysterols were most extensively studied for its poten
2020-09-14

While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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The idea that ASB can drive compartment expansion in
2020-09-14

The idea that ASB11 can drive compartment expansion in the CNS is further supported by in vitro work in human neuronal precursors. Nerve growth factor (NGF)-induced differentiation of PC12 pheochromocytoma Amiloride HCl sale [11] and RA-induced human pluripotent teratocarcinoma carcinoma (NT2) cell
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Experimental studies offer a means of developing an
2020-09-14

Experimental studies offer a means of developing an empirical basis for the development of forensic protocols in the investigations of specific crime types [12]. Such an evidence OSI-930 for ICST cases will help enable the identification of situations when there is likely to be recoverable DNA from
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Like compound substitution on compound contains amino and
2020-09-14

Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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br Introduction Although not fully understood the
2020-09-14

Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen
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Herein we explored by docking studies the effectiveness
2020-09-14

Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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