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TRAM 39 The quaternary structure of many of the family
2020-02-11

The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and TRAM 39 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). Harikumar, Pin
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Compounds that interact with MDR can do so by
2020-02-11

Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant MDL 800 and there was no observed reduction
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For radiochemotherapy it is well known that mitotic cell
2020-02-11

For radiochemotherapy, it is well known that mitotic cell death and apoptosis present the major cell death modes. More recently, autophagy-dependent cell death has been described to occur upon radiochemotherapy (Daido et al., 2005, Song et al., 2017). This form of regulated cell death depends on com
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As the primary model we selected LDL receptor knockout
2020-02-11

As the primary model we selected LDL-receptor knockout mice because these resemble the human plasma lipoprotein profile more closely. Currently, genetic models with reduced milk cholesterol content, which mimic cholesterol-free formula feeding, are unavailable. Thus, instead of modifying milk choles
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Plerixafor 8HCl br Materials and methods br Results To inves
2020-02-11

Materials and methods Results To investigate the effect of 17βE on cell proliferation in the human renal tubular epithelia, BrdU uptake was measured in HRTEC primary and 3D-HRTEC cultures, allowing determination of the DNA replication rate. Representative microphotographs show BrdU uptake in H
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Introduction Psoriasis is a chronic recurrent and
2020-02-11

Introduction Psoriasis is a chronic, recurrent and inflammatory skin disease, and it is characterized by erythema, skin hyperplasia, scales, and hyperproliferation of keratinocyte [1]. It is reported that the psoriasis occurrences are about 3% worldwide [2], but the number varies depending on ethni
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Our recent discovery M P
2020-02-10

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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br Chagas disease Chagas disease an NTD
2020-02-10

Chagas disease Chagas disease, an NTD caused by the protozoan Trypanosoma cruzi, affects 8–10 million people globally. More than 10,000 deaths are caused by the disease each year, and nearly 70 million people are susceptible to infection (Manne-Goehler, Umeh, Montgomery, & Wirtz, 2016). Chagas di
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A neurotoxic syndrome called Intermediate syndrome has been
2020-02-10

A neurotoxic syndrome called “Intermediate syndrome” has been described after acute cholinergic crisis, which has been interpreted as the result of pre- and postsynaptic disruptions of neuromuscular transmission (Senanayake and Karalliedde, 1987). Other toxic effects with unknown molecular targets
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Cell swelling stimulates the release
2020-02-10

Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino gemsa receptor taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activa
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Bioinformatics analysis for genes encoding
2020-02-10

Bioinformatics analysis for genes encoding proteins (ESR1, IL6, TERT, DNMT3B) showed that NF-kB is one of the transcription factors that might be regulating their expression, especially for IL6, TERT and DNMT3B genes. Previous studies have demonstrated that PA induces NF-kB activation, thus increas
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br Introduction Fibroblast growth factors FGF
2020-02-10

Introduction Fibroblast growth factors (FGF) are a family of 18 secreted ligands that bind to four receptor tyrosine kinase (RTK) FGF receptors (FGFR1–4). The interaction of FGFs with their cognate receptors results in the activation of a number of downstream signaling pathways, including the MAP
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Regarding eicosanoid production iPLA VIA appears in general
2020-02-10

Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele
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Herein in continuation of our interest in designing new
2020-02-10

Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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As for antiviral activity eight
2020-02-10

As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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