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AZD-5438 The first example of a broadly acting antiviral dru
2021-05-27

The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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br Experimental section br Author contributions
2021-05-27

Experimental section Author contributions Acknowledgements Introduction Many TMPyP4 tosylate in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme
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Xenobiotic metabolism primarily occurs in liver which contai
2021-05-26

Xenobiotic metabolism primarily occurs in liver, which contains many enzymes to catalyze the transformation of xenobiotic. Usually, cytochrome P-450s (CYP450s) act as the first response for biotransformation of xenobiotic in organisms. CYP450s generally consist of various subfamily enzymes which can
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a Furthermore the Langerhans cell infiltrate in skin biopsie
2021-05-26

Furthermore, the Langerhans cell infiltrate in skin biopsies from RG7155-treated patients will be analyzed since keratinocyte derived IL-34 was identified as their survival factor (Greter et al., 2012). Microglia, the other macrophage population regulated by neural progenitor and glial cell-derived
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In summary our data demonstrated a biological function
2021-05-26

In summary, our data demonstrated a biological function of cpt1a gene from large yellow croaker. In particular, we indicated the effects of fasting on free carnitine status, CPT1 kinetics, and cpt1a mRNA expression in liver of large yellow croaker. During short-term fasting, the fish liver may have
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We found that E and GEN
2021-05-26

We found that E2 and GEN each has mostly similar effects on recruitment of the epigenetic modulators to the MB-COMT distal promoter (summarized in Table 2). These effects are associated with increased promoter methylation and gene suppression of COMT. It is noted that the array of epigenetic modulat
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br Discussion The use of
2021-05-26

Discussion The use of carp primary cell cultures proved to be a valuable approach to evaluate the piscine immune response. A. hydrophila was a more potent stimulator of NO formation by carp leukocytes compared to commercial LPS often used for leukocyte stimulation (Mustafa and Olson, 1998, Chao e
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More importantly Santagata et al have suggested a
2021-05-26

More importantly, Santagata et al. have suggested a new breast cancer subtyping method according to ER, androgen receptor (AR), and VDR with a higher prognostic value than the ordinarily used method based on ER, progesterone receptor (PR) and Her2 (Santagata et al., 2014). This implies that such com
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The most common pathology associated with FGR is poor
2021-05-26

The most common pathology associated with FGR is poor placental perfusion as a result of abnormal placentation [4]. Placental developmental disorders and insufficient hormone synthesis may lead to FGR [5,6]. However, the exact mechanism responsible for abnormal placental development remains unclear.
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br Significance Ubl post translational
2021-05-26

Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig
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br Halogenases Enzymatic C H activation leading
2021-05-26

Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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It was hypothesized that if modafinil
2021-05-25

It was hypothesized that if modafinil acts primarily via a noradrenergic mechanism, Dbh −/− mice should be non-responsive since they completely lack NE. In contrast, if modafinil acts mainly through DA systems, these mice should be hypersensitive. Modafinil was tested in Dbh −/− mice using both loco
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Cysteine protease inhibitors representing several chemical s
2021-05-25

Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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angiotensin receptor blockers Considering the protumoral fun
2021-05-25

Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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Compounds were screened for their activity against
2021-05-25

Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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