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In the course of our program
2019-10-11
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Evidence for interactions between the endothelin
2019-10-11
Evidence for interactions between the endothelin and the angiotensin system has also become plentiful. It has become clear that the two systems, in addition to acting independently, can act synergistically (Emori et al., 1989, Imai et al., 1992) as well as promote the peptide mRNA expression in endo
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Immune modulation by steroid hormones is
2019-10-11
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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br Results The AR genotype frequencies are shown
2019-10-10
Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find
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Recently naphthoquinone derivatives have shown promising
2019-10-10
Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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Inhibition of DHODH is reflected by an antiproliferative eff
2019-10-10
Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear H 89 (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few selected compounds are
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Caspase-10/a, human recombinant protein Hepatic steatosis i
2019-10-10
Hepatic steatosis is strongly associated with insulin resistance. Numerous studies in humans and animals have shown that insulin-resistant states are often accompanied by hepatic steatosis (Angulo and Lindor, 2001, Marchesini et al., 1999, Marchesini et al., 2005, Petersen and Shulman, 2006, Seppala
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GW-786034 clinical Presumably LBPs have health promoting act
2019-10-10
Presumably, LBPs have health-promoting activities, such as antioxidant, immune regulation, anti-stress, anticancer, neuroprotective and antidiabetic activities [[7], [8], [9], [10], [11]]; LBPs can improve the whole-body health status of mice and stimulate the expressions of IL-2, IL-12 and TNF-α, w
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CYP enzymes have an important role in microsomal
2019-10-10
CYP450 Glutathione (GSH/GSSG/Total) Fluorometric Assay Kit pathway have an important role in microsomal oxidase function across a broad range of taxa (Pakharukova et al., 2012). They are involved in metabolism and detoxification of both internally generated compounds and xenobiotics as the phase I
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Beside the previously reported Topo I
2019-10-10
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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The anticholinesterase activities of all subfractions derive
2019-10-10
The anticholinesterase activities of all subfractions derived from EtOAc extract were detected and summarized in . Fraction 5 and its resulting subfractions (5B, 5C, 5D, 5C3, 5C4, 5D3, and 5D4) were found to show attractive activities. Subsequently, ten compounds (–) were obtained from these active
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River sand was graded in accordance with ASTM C
2019-10-10
River sand was graded in accordance with ASTM C778 [47] (see Table 2). The graded sand had a water Myriocin of 1.00%, fineness modulus of 3.49 and specific gravity of 2350kg/m3. A polycarboxylate based superplasticizer called ZP with pH of 7±1 and specific gravity of 1.1±0.02 was also used to adjus
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We obtained two bands in RT
2019-10-10
We obtained two bands in RT-PCR for detection of SERPIN1-FOSB fusion when Taq DNA polymerase was used (Fig. 3A). Genuine RT-PCR product of SERPIN1-FOSB fusion was proved to be the shorter one (733 EPZ031686 and pairs) by sequencing, and the longer band (863 base pairs) was shown to be derived from
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Acknowledgments br Introduction Steroidogenesis the process
2019-10-10
Acknowledgments Introduction Steroidogenesis, the process of testosterone synthesis, occurs in the adrenal cortex, testis and ovary, and it is controlled by luteinizing hormone (LH), which is synthesized and secreted from the pituitary (Hanukoglu, 1992, Payne and Youngblood, 1995). In the testis
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Given that dimethylamine substitution was tolerated as in
2019-10-10
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated 2478 amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The slightly
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