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The effect of ET activity on the
2020-11-13

The effect of ET-1 activity on the development of experimental pulmonary fibrosis has also been examined by other investigators. One study found that repeated administration of Bosentan, an ERA used to treat pulmonary arterial hypertension (PAH), significantly decreased bleomycin-induced pulmonary f
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Judging from the densitometric analysis of
2020-11-13

Judging from the densitometric analysis of the Western blots, CYP2E1 protein was expressed, although at very low levels, by PT cells. This corresponds to previous observations [10], showing that CYP2E1 was expressed in the PT, although expression was higher in the distal tubule. Testosterone 6β-hyd
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br A brief history of RBR
2020-11-13

A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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EBI and its ligand s
2020-11-13

EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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DIDS br Multi subunit RINGs There are RING
2020-11-13

Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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In the context of E ligase drug discovery
2020-11-13

In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 Azi
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In the past few years
2020-11-13

In the past few years we and others have reported that GLP-1 may also be secreted by sub-populations of alpha Pyridoxal 5 phosphate in human pancreatic islets (Marchetti et al., 2012, Ellingsgaard et al., 2011), which could contribute to beta cell function and survival (Marchetti et al., 2012, Elli
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br Introduction As a strong analgesic morphine is often
2020-11-13

Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft
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Experimental studies offer a means of developing an empirica
2020-11-13

Experimental studies offer a means of developing an empirical basis for the development of forensic protocols in the investigations of specific crime types [12]. Such an evidence hydroxychloroquine sulfate for ICST cases will help enable the identification of situations when there is likely to be r
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Studies of Jelski and Szmitkowski show
2020-11-13

Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between gamma secretase inhibitors of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH and ALDH activi
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LTD and LTC cause contraction in
2020-11-13

LTD4 and LTC4 cause contraction in the rat stomach and these contractions are sensitive to CysLT1 receptor antagonists (Goldenberg and Subers, 1983, Miura et al., 1992, Miyata et al., 1995). However, effects of other leukotrienes in the gastric contraction and inhibitory effects of potent, selective
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In addition to the blockade of airway smooth muscle contract
2020-11-13

In addition to the blockade of airway smooth muscle contractions, CysLT1 receptor antagonists also exerted a potent anti-inflammatory effect at this level. The oral administration of MEN91507, Pranlukast, Montelukast, and Zafirlukast also produced a long-lasting inhibition of leukotriene D4-induced
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On the other hand the
2020-11-13

On the other hand, the IL-8 promoter activity induced by the signalling cascade of the CysLT1-G300S receptor is higher than that of the WT receptor. The chemokine IL-8 is mainly involved in the recruitment and activation of neutrophils and we have previously shown that this chemokine gene is a targe
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Previous studies reported that combined administration
2020-11-13

Previous studies reported that combined administration of licorice/GL and TWHF/TP showed reduced toxicity and equal or even potentiated therapeutic efficacy when treating arthritis (YS et al., 2006, YS et al., 2008, Zhang et al., 2007). Our findings that GL reduced exposure to TP in rats confirmed t
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Within the Class II receptors
2020-11-13

Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem tazemetostat of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely related, as are D
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