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In normal chow fed mice EP
2021-06-19
In normal chow fed mice, EP4 deficiency also decreased the expression of CYP8B1, the downstream target of CYP7A1. Similarly, knockdown of EP4 with small interfering RNA reduced the expression of CYP8B1 in HepG2 cells. Therefore, it was anticipated that there would be an increased expression of CYP8B
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To study systemic potential of the selected compounds
2021-06-19
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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Repulsive interactions towards undesirable substrates are ar
2021-06-19
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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In a larger study of patients
2021-06-19
In a larger study of 22 patients with nondiabetic proteinuric chronic kidney disease, BQ-123 produced significant natriuresis, resulting from increased renal blood flow. In addition, ETA antagonism reduced blood pressure and proteinuria, and, a new finding, decreased arterial stiffness. However, in
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br Introduction Mammalian proteases comprise both the peptid
2021-06-19
Introduction Mammalian proteases comprise both the peptidases or exopeptidases, which act at the N- or C-terminal positions of polypeptides, and proteinases or endopeptidases, which are capable of cleaving peptide bonds in the central regions of polypeptides. The endopeptidases are classified in
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It is known that cigarette smoke increases the oxidative
2021-06-19
It is known that cigarette smoke increases the oxidative burden in the lungs of mice with emphysema, which leads to oxidative stress [[34], [35], [36]]. However, in addition to cigarette smoke, studies have shown that endogenous oxidative stress is associated with proteolytic GSK2269557 in several
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br Expression and Tissue Functions of DDRs The DDRs are
2021-06-19
Expression and Tissue Functions of DDRs The DDRs are widely expressed in different tissues, both during development and in adult organisms. DDR1 mRNA is found in many tissues in mice and humans, with high levels in brain, lung, kidney, spleen, and placenta (Di Marco et al., 1993, Johnson et al.,
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br Materials and Methods br Acknowledgements
2021-06-19
Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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Erythromycin Our results indicate an OT specific activation
2021-06-19
Our results indicate an OT-specific activation of PKR that inactivates eIF2a and may, by this means, reduce protein translation by utilizing only select sensors and mediators of the UPR (i.e., avoiding significant PERK activation). Interferon is a PKR activator [32] that temporarily subdues cellular
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Circulating NK subsets also show considerable differences in
2021-06-19
Circulating NK subsets also show considerable differences in homing molecules. CD56bright pten pathway express the chemokine receptor CCR7 and L-selectin, which drive their migration to secondary lymphoid organs (Fehniger et al., 2003). In contrast, CD56dim display a high density of CX3CR1 and CXCR1
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In all available E E
2021-06-19
In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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br Are incretins the only mediators of the anti
2021-06-19
Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr
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Recent studies from the literature have
2021-06-19
Recent studies from the literature have identified new ddr1 of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-tolylurea (16d), has e
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br Conclusions The present study demonstrated that CuE posse
2021-06-19
Conclusions The present study demonstrated that CuE possesses strong hepatotoxicity. CuE is not only a mechanism-based inhibitor of human CYP3A4, but also inhibits P-gp activity in vitro. In whole animal studies, CuE induces CYP3A and P-gp after a long-term treatment but inhibits the activities o
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Following the relationship model adopted in this
2021-06-18
Following [20], [22], the relationship model adopted in this Sulbactam work to estimate the time to failure is the Inverse Power Law (IPL): Where L is the SUT life characteristic (e.g. the mean time to failure), s represents the stress level, while k and w are model-related parameters to be defined
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