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AVE 0991 A series of monocarboxylated chalcones e
2021-05-10

A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 AVE 0991 was not sensitiv
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As we all known hypoxia is a
2021-05-10

As we all known, hypoxia is a hallmark of tumour microenvironment, which is a key regulator of tumour growth and metastasis [4]. Hypoxia meditates a series of cellular responses including angiogenesis by activating transcriptional factor hypoxia inducible factor (HIF), which is consist of an obligat
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In addition to its HEAT
2021-05-10

In addition to its HEAT repeats, CRM1 also possesses a C-terminal extension (C-extension, residues 1032–1071), composed of a helix (C-helix) followed by a short stretch of residues (C-tail). In the absence of Ran, the C-extension adopts a conspicuous conformation that bridges across the ring-shaped
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Tanshinone IIA---sulfonic sodium In this study we characteri
2021-05-08

In this study, we characterized the metabolic function of tra2 in the Drosophila fat body. Similar to the 9G8 phenotype, decreasing tra2 levels in the Drosophila fat body using RNAi resulted in increased starvation resistance and a large increase in triglycerides. This increased storage of triglycer
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galanin Interestingly Carver Johnson and Kim investigated a
2021-05-08

Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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Ki16425 The anticholinesterase activities of all subfraction
2021-05-08

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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The Fontan circulation When first described in the
2021-05-08

The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital Ibrutinib disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates a total cavop
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A French cohort study reported
2021-05-08

A French cohort study reported that micronized progesterone or didrogesterone used with oral or percutaneous estradiol showed no increase or decrease in the risk of breast cancer compared to synthetic progestins for at least 4 years of treatment [22] and even after 8 years [23]. Although the results
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Our previous work has demonstrated that two glutamate
2021-05-08

Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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Despite a high affinity for progesterone and
2021-05-08

Despite a high affinity for progesterone and a relatively high affinity for testosterone [7], the binding of progesterone and testosterone to CBG is often disregarded [1], [2], [3]. However, the concentrations of these two hormones varies considerably under both normal physiological and pathophysiol
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In summary we elucidated the in vitro activities of KDM
2021-05-08

In summary, we elucidated the in vitro activities of KDM1B in regulation of PC cell proliferation and apoptosis. These studies provided a novel insight into the previously unrecognized roles of KDM1B in human PC cells. We showed for the first time that KDM1B knockdown attenuated proliferation and in
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br Analytical improvements Since our review of Oxysterol
2021-05-08

Analytical improvements Since our review of “Oxysterol Metabolomes” in 2011 [7], there have been a number of improvements in analytical methods for the analysis of oxysterols and related compounds. McDonald and colleagues in Dallas have refined their LC-MS methods which are now applicable for ana
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p as a cyclin dependent
2021-05-08

p21, as a cyclin-dependent kinase inhibitor, exert significant negative regulator of proliferation, and it could be transcriptional upregulated by p53 in order to impel transient osi sc 175 mg arrest (Romanov et al., 2010). Using western blotting, we found that the protein expression of p21 upgrades
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Gardiquimod In this contribution herein we report our newly
2021-05-08

In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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Dihydrofolate reductase DHFR is an excellent molecular targe
2021-05-08

Dihydrofolate reductase (DHFR) is an excellent molecular target for this study because it has been and is currently studied by using different molecular modeling techniques [6], [7], [8], [9]. Kerrigan et al. have reported an interesting review about recent progress in molecular dynamics simulations
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