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Another breakthrough towards the understanding of the
2021-04-17

Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t
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Various domains of the HSA molecule have
2021-04-17

Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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amantadine hcl br Introduction Maintaining the normal
2021-04-17

Introduction Maintaining the normal function of fetal trophoblasts is essential for a successful pregnancy. Preeclampsia (PE), a pregnancy-specific disorder, is often associated with excessive trophoblast cell apoptosis and superficial trophoblast invasion leading to insufficient spiral artery r
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Our previous high throughput screening HTS campaign using
2021-04-17

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Mifepristone assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22],
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Collectively the results presented here provide new insights
2021-04-17

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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The total reduced glutathione content
2021-04-17

The total reduced glutathione content was determined in both c-di-AMP to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0.2±0.1 μmol/g
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In some cases more than one CYP enzyme may be
2021-04-17

In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple CGP 42112 (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape to determine the k
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Immunomodulation effects of certain oxysterols were previous
2021-04-17

Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychol
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SIRT is a representative member of Sirtuins which is a
2021-04-17

SIRT1 is a representative member of Sirtuins, which is a family of highly conserved NAD+-dependent class III histone deacetylases. SIRT1 deacetylates plentiful nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016; Gu et al., 2016; Tu et al., 2018) to p
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The quaternary structure of many of
2021-04-17

The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and SC 144 receptor receptors) have been actively studied and it has been demonstrated that they can form homodimers/oligomers (Gao et al., 2009; Ng & Chow, 2015; Ng, Lee, & Chow, 2013). Hariku
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Air trapping at the small
2021-04-17

Air-trapping at the small airways is related to severe MK1775 (Bjermer, 2014), and acute exacerbation (Mahut et al., 2010). Although asthma patients are generally treated with inhaled corticosteroid (ICS) or with ICS and long-acting β2 agonist (LABA), the efficacy of such treatment depends on drug p
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BAY 87-2243 While several C terminal peptides have
2021-04-17

While several C-terminal peptides have been reported to have modest (astressin) or substantial (astressin2-B, antisauvagine-30) subtype selectivity for the CRF2 receptor (), [125I]YP20 is the first reported small analog of the C-terminus of CRF exhibiting subtype selectivity for the CRF1 receptor vs
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Tacrine amino tetrahydroacridine I Fig was
2021-04-16

Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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br Introduction Oral contraceptives OCs are the most
2021-04-16

Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol
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MK-2206 receptor br Materials and methods br Results br Disc
2021-04-16

Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed
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