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Replacement of the saturated propoxy
2019-10-14
Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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Baicalein trihydroxyflavone was first isolated from the root
2019-10-14
Baicalein (5,6,7- trihydroxyflavone) was first isolated from the roots of Scutellaria baicalensis Georgi (Lamiaceae family), a medicinal plant with diverse therapeutic implications; antibacterial, antiviral, and anti-inflammatory properties. It has been found that baicalein benefits neuroinflammatio
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The CYP A genes are regulated physiologically by
2019-10-14
The CYP3A genes are regulated physiologically by glucocorticosteroids, growth hormone, thyroid hormones and cytokines [13, 20, 30]. It has been shown that glucocorticoid receptor (GR), pregnane X receptor (PXR), constitutive androstane receptor (CAR) and vitamin D receptor (VDR) play an important ro
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Furthermore down regulation of Cpt
2019-10-14
Furthermore, down-regulation of Cpt1a, ApoE, Fasn, Pxr, and Srebp-1 genes indicates a down-regulation of lipid metabolism associated genes while Fatp1 is up-regulated and indicates an increase in fatty AZ 10606120 dihydrochloride transport genes involved in accumulation [84,85]. These changes in ge
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br The amygdala complex The amygdala
2019-10-14
The amygdala complex The amygdala complex is composed of distinct nuclei and subdivisions including the lateral (LA), basolateral (BL), and basomedial (BM) amygdala; the medial (Imp), lateral paracapsular (lpc), and main intercalated cell cluster (IN); and the lateral and medialcentral amygdala (
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Fisetin tetrahydroxyflavone is a flavonol present in several
2019-10-14
Fisetin (3,3′,4′,7-tetrahydroxyflavone) is a flavonol present in several fruits and vegetables such as grape, persimmon, strawberry, apple, and onion at concentrations rangeing from 2 to 160 μg/g. Fisetin is a well–known bioflavonoid with remarkable biological effects including chemopreventive/chemo
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Currently much effort has been
2019-10-14
Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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Collectively the results presented here provide new insights
2019-10-14
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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Emodin br Acknowledgements We thank Jeffrey D Konowalchuk an
2019-10-12
Acknowledgements We thank Jeffrey D. Konowalchuk and John Sony Robbins for their technical assistance. This work was supported by Natural Sciences and Engineering Research Council of Canada (NSERC) grants to DRB (RGPIN-2013-355303) and MB (RGPIN-2014-96395). AMR was supported by NSERC Vanier Doct
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g protein coupled receptors As one of the two receptors for
2019-10-12
As one of the two receptors for the primordial chemokine CXCL12, ACKR3 exists in jawless fish (Bajoghli, 2013, Nomiyama et al., 2011, Venkatesh et al., 2014). The sea lamprey genome contains two copies of the ACKR3 gene (Ensembl Acc. Nos.: ENSPMAP00000011187 and ENSPMAP00000011401) (Table 1), both e
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In a cell based functional assay the
2019-10-12
In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC
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Application of the CPH model
2019-10-12
Application of the CPH model relies on the assumption that the hazard ratio of two observations is constant over time [2]. This enables us to infer the rate of risk of the treatment. For example, in the study of patients with pulmonary arterial hypertension (PAH) [5], the hazard ratio of a group of
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br Study design br Results We enrolled subjects awaiting SOT
2019-10-12
Study design Results We enrolled 50 subjects awaiting SOT (15 kidney, 14 liver, 1 liver + small bowel, 11 lung, 9 heart) and 50 controls (Table 1) who were similar with respect to median age (subjects 49.1 yrs., controls 48.6 yrs.) gender (64% male subjects and controls), and CMV-seropositivit
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br Acknowledgments br Introduction Cell cycle arrest or dela
2019-10-12
Acknowledgments Introduction Cell cycle arrest or delay may occur at 3 major checkpoints, i.e. G1/S, intra-S and G2/M. p53 has a central role in controlling the G1/S checkpoint, and its loss or deactivation, occurring in the majority of cancers, forces cancer cells to rely on the S and G2/M ch
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In brief while previous studies have evaluated the individua
2019-10-12
In brief, while previous studies have evaluated the individual roles of VDR and ER signaling pathways in breast cancer, in the present study we performed an in silico approach for comparative evaluation of these pathways. Considering the complex interaction networks in the context of cancer, such co
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