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Initially studies of GPCRs predominantly assessed
2020-01-03

Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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br Materials and methods br Results br Discussion COX mediat
2020-01-03

Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed
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As with all meta analysis this study
2020-01-03

As with all meta-analysis, this study certainly has some limitations. First, our results were derived from unadjusted analyses due to lack of raw data, and lack of further adjusted analyses for age, gender and co-morbidity conditions may impact the reliability of our findings [63]. Second, obvious h
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br Materials and methods br Results br Discussion
2020-01-03

Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th
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The significance of the difference in the
2020-01-02

The significance of the difference in the DDR2 binding specificity towards fibrillar and non-fibrillar collagens is not understood, but may imply differences in biological responses when chondrocytes bind to different collagens in the growth plate. Investigations by Labrador et al. (2001) have shown
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Inappropriate heme metabolism has been linked to
2020-01-02

Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer\'s disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 2
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Cepharanthine receptor We found that the postnatal absence o
2020-01-02

We found that the postnatal absence of norepinephrine yields differing effects depending on noradrenergic receptor type and Cepharanthine receptor region. The density of α1-AR, indicated by [3H]prazosin binding was similar between Dbh+/− and Dbh−/− mice except for a significant increase in hippocam
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Recently naphthoquinone derivatives have shown promising res
2020-01-02

Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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br Conclusion AS SP the first line treatment still
2020-01-02

Conclusion AS+SP, the first-line treatment, still remains highly effective in Pakistan following its introduction in 2007. However, molecular data indicate that SP resistance is being established in Pakistan, although mutations that confer a high risk of SP treatment failure are rare or non-exist
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Preparation of the regioisomeric pyridooxazepinones and was
2020-01-02

Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and SNS-032 chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2.4 mixtu
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br Acknowledgements br Introduction Laryngeal cancers
2020-01-02

Acknowledgements Introduction Laryngeal cancers are the most frequent cancers of the head and neck region and their occurrence is strongly associated with the exposure to cigarette smoke and the consumption of strong alcohols. Almost all laryngeal cancers are squamous cell carcinomas. Usually
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Although PGD was initially considered to
2020-01-02

Although PGD was initially considered to elicit its biological actions through a classical PGD receptor (DP1), later findings suggested that several PGD-mediated actions of eosinophils arise via DP2,, which is also known as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells)
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Ethyl naphthoates a h were successfully
2020-01-02

Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The
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Based on the above we hypothesized that a PROTAC
2020-01-02

Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Our study showed that parental morphine exposure in the
2019-12-31

Our study showed that parental morphine exposure in the adulthood is associated with an increased tendency toward morphine consumption in F1 but not F2 male offspring. Thus, it seems that trans-generational effects of parental morphine consumption disappear in the second generation. In support of ou
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