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br Clinical potential of ET
2020-06-11
Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]
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Most xenobiotics undergo biotransformation before
2020-06-11
Most xenobiotics undergo biotransformation before being excreted. Such biotransformation is classified into two phases. In the first phase, the lipophilic substrate is oxidized by the cytochrome P-450 (CYP450) enzyme system, which introduces a single oxygen Anisodamine synthesis into the molecule (M
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LY83583 The Kaempferia parviflora extract met
2020-06-11
The Kaempferia parviflora extract met the criteria for a non-competitive interaction with CYP1A1 based on the decrease of Vmax and unchanged Km. The high Ki value and low IC50, as well as the high Km value was indicative of the weakness of the interaction between the Kaempferia parviflora extract an
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The EGFR belongs to the ErbB family of
2020-06-11
The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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Introduction Cholesterol plays a pivotal
2020-06-11
Introduction Cholesterol plays a pivotal role as a constituent of biological membranes and as a precursor for vitamins, hormones and bile acids. Accordingly, its production, distribution, and elimination must be tightly regulated at the cellular and organismal level. Accordingly, dysregulated chole
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Interestingly we observed that T D islet cells have lower
2020-06-11
Interestingly, we observed that T2D islet c75 have lower DPP-4 expression, as compared to ND cells (Fig. 1, Fig. 2). Previously, a reduced activity of this peptidase was observed in human T2D islet lysates (Omar et al., 2014). As mentioned above, GLP-1 is also produced by islet cells (alpha cells i
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br Introduction br Sphingolipid metabolism Sphingolipids are
2020-06-11
Introduction Sphingolipid metabolism Sphingolipids, are fundamental constituents of all eukaryotic membranes and their metabolism is carried out by a broad array of anabolic and PD 0332991 with ceramide as their hub (for a review, (Hannun and Obeid, 2018)). Ceramide can be formed by multiple
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br Non cyclic nucleotide EPAC regulators
2020-06-10
Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su
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SGX523 Accumulating evidence suggests that certain
2020-06-10
Accumulating evidence suggests that certain abnormal emotional traits, such as impulsive aggression and cluster B personality, are associated with suicidal behaviors (Currier and Mann, 2008, Mann et al., 2009, Rujescu et al., 2007, Turecki, 2005). Impulsive aggression appeared to be associated with
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In conclusion our data represents a step
2020-06-10
In conclusion, our data represents a step forward in terms of clarifying the role of I/D polymorphism of ACE and VNTR polymorphism of eNOS and G1793A, C677T and A1298C polymorphism of MTHFR in pathophysiology of psoriasis in Pakistani patients. It will help in better understanding of the disease pro
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br Significance Our understanding of the
2020-06-10
Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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br Conflict of interest br Acknowledgements The authors
2020-06-10
Conflict of interest Acknowledgements The authors are grateful to laboratory technician Kristina Andersson for expert technical assistance. The authors acknowledge the Swedish Research Council (Grant no. 6834), Region Skåne and Faculty of Medicine, Lund University, for financial support. In
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It is currently believed that acute morphine administration
2020-06-10
It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ
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br Results and Discussion br Materials
2020-06-10
Results and Discussion Materials and Methods Acknowledgements Introduction Inorganic pyrophosphate is generated as a by-product in several enzymatic reactions in cells. These reactions include DNA and RNA synthesis, activation of fatty acids and amino acids, as well as synthesis of the c
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br Acknowledgments br Introduction Cysteinyl leukotrienes
2020-06-10
Acknowledgments Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic FDA-approved Drug Library and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, includi
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