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Immune modulation by steroid hormones is a
2021-01-11
Immune modulation by steroid hormones is a rather new aspect of the research on endocrine interactions in lower vertebrates (Harris and Bird, 2000). In the classical view, steroids exert their effects by binding to specific intracellular receptors that function as ligand-activated transcriptional re
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The defining molecular feature of Ewing sarcoma is the
2021-01-11
The defining molecular feature of Ewing sarcoma is the characteristic EWSR1/ETS fusion protein, most commonly involving EWSR1 and FLI1 (Delattre et al., 1992, May et al., 1993). EWS–FLI1 causes global changes in gene expression both by directly regulating gene expression and by causing changes in ch
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Given the potency enhancing effect of the
2021-01-11
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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Fmoc-His(Trt)-OH LVDP values of at the
2021-01-11
LVDP values of ~80% at the end of reperfusion. L-NAME treatment did not modify the contractility detected in ischemic control hearts but annulled the actions of BZ acquiring LVDP values up to 40% (Fig. 4 A). A similar pattern was observed when +dP/dtmax was analysed (Fig. 4 B). LVEDP, as an index o
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Therefore HNE is an attractive therapeutic target and the de
2021-01-11
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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CZC-25146 Collectively the results presented here provide ne
2021-01-11
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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Herbal products may alter the metabolism
2021-01-11
Herbal products may alter the metabolism of certain drugs and, likewise, the metabolism of components of herbal products may be altered by some drugs, specifically those that affect cytochrome P450 SNDX-275 (CYP). These can bring about an alteration of the pharmacokinetics and pharmacological activi
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We recently reported that the information about the electron
2021-01-09
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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br Conclusions Cereal seeds like the seeds of
2021-01-09
Conclusions Cereal seeds, like the seeds of all plants, are responsible for the development, protection, dispersal, and nutrition of the next generation. Moreover, cereal caryopses have a high nutritional value for humans and animals. The stable and proper growth of cereal seeds is made possible
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rock inhibitor Introduction The Bromeliaceae family is one o
2021-01-09
Introduction The Bromeliaceae family is one of the most morphologically and ecologically diverse flowering plant families native to the tropics and subtropics of the New World (Benzing, 2000). They comprise >3000 species and are traditionally divided into three subfamilies: Pitcairnioideae, Bromeli
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beta adrenergic receptors br Chemistry Scheme shows the synt
2021-01-09
Chemistry Scheme 1 shows the synthesis of compounds 15-1–15-33 from commercially available 2-(4-aminophenyl)acetonitrile (8a). Protection of the starting material 8a with di-t-butyl dicarbonate afforded 9. The reaction of 9 with methyl 1-chloroisoquinoline-4-carboxylate in the presence of sodium
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Furthermore the determination of downstream
2021-01-09
Furthermore, the determination of downstream target genes induced by CdCl2 is noteworthy and can help to define its underlying carcinogenesis mechanism. Therefore, we evaluated c-fos and c-jun expression which are stimulated by estrogen through ERK/MAPK pathway. These are not only proto-oncogenes wh
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Amphiphilic compounds lower interfacial tension and
2021-01-09
Amphiphilic compounds lower interfacial tension and its biological production often results in a competitive environmental advantage (Darvishi et al., 2011). The reduction of interfacial tension can increase the biologically available surface areas resulting in increased metabolism of insoluble comp
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br Iterative design approach overview An iterative design st
2021-01-09
Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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Lavallee et al reported that PREG could be
2021-01-09
Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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