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The physicochemical properties of the prodrugs provided
2021-09-02

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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br Conclusion Discovery of an ideal orally active antithromb
2021-09-02

Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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In the present study we used linagliptin one of the
2021-09-02

In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma
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br Conclusions In this paper
2021-09-01

Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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br Discussion Electroporation is a convenient and efficient
2021-09-01

Discussion Electroporation is a convenient and efficient way to introduce foreign material into isoquercitrin receptor [10], [16], [17], [18]. There are a lot of different protocols for transfection with electroporation. It was reported that there are several parameters that are relevant to succ
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We show that direct contact
2021-09-01

We show that direct contact with MSCs is necessary and sufficient to induce DDR2 upregulation in breast cancer cells. DDR2 expression in MSC is required for collagen deposition and leads to increased DDR2 expression and activation in breast cancer cells. This paracrine-autocrine MSC-cancer cell axis
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The physiological role of the UCNs in the
2021-09-01

The physiological role of the UCNs in the regulation of the HPA axis is still under debate (Fekete and Zorrilla, 2007, Suda et al., 2004). UCN 1 was proved to increase the plasma ACTH and corticosterone levels in rats (Bagosi et al., 2014, Vaughan et al., 1995), whereas UCN 2 and UCN 3 were shown to
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Natural progestogens play an important role in the stimulati
2021-09-01

Natural progestogens play an important role in the stimulation of oocyte growth and maturation as well as in spermatogenesis and sperm maturation, and they act as sex pheromones in teleost fish (Kime, 1990, Kobayashi et al., 2002, Nagahama and Yamashita, 2008, Scott et al., 2010). A complex series o
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substance p The same reservoir of genes is involved
2021-09-01

The same reservoir of substance p is involved in fusions in all types of cancers, which predominantly encode kinases and transcriptional factors [102]. This makes fusion genes potential pan-cancer targets, and renders tumor categorization based on genetic profiling therapeutically reasonable. For i
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Here two labs that helped
2021-09-01

Here, two labs that helped characterize these two pathways have worked together to further test whether these apparently parallel pathways from β-AR to CaMKII-RyR might be related in series. Much of the work leading to the Epac pathway involved measurement of Ca sparks as an index of SR Ca leak, oft
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Two GPCR subtypes of interest in
2021-09-01

Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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br Materials and methods br Results br Discussion In
2021-09-01

Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel
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The estrogen receptor ER dependent signaling
2021-09-01

The estrogen receptor(ER)-dependent signaling pathway plays an important role in bone metabolism by restoring the balance between osteoblastic bone formation and osteoclastic bone resorption [21]. ER has two major isoforms, ERalpha (ER-α) and ERbeta (ER-β), which mediate the effect of estrogen and o
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To overcome problems with the biochemical reconstitution of
2021-08-31

To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a
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br Materials and methods br Results As shown
2021-08-31

Materials and methods Results As shown in Table 1, blood urea nitrogen and serum creatinine levels were significantly elevated at both 1st and 7th days of pyelonephritis, when compared with those of the control group (PIT-901 mg formation or intratubular neutrophils, while tubules showed mild
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