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br Conclusion CSF R may contribute
2019-09-02
Conclusion CSF-1R may contribute to limitation of targeted therapies by providing EGFR-bypassing signals that support proliferation. Multi-kinase inhibitors such as cabozantinib are available, and agents targeting CSF-1R are in clinical trials, however, at present, as inhibitors of tumor-associat
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bromocriptine mesylate and Ethyl naphthoates a h were succes
2019-09-02
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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Experiment B CP during fear acquisition
2019-09-02
Experiment 4B: CP154,526 during fear acquisition normalizes fear-potentiated startle and prevents exacerbation of contextual conditioned fear in SERT−/− rats. As genotypes differed markedly in basal fear acquisition, drug effects could differ strongly between genotypes. Therefore, all effects in th
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The enzyme cyclooxygenase COX or prostaglandin endoperoxide
2019-09-02
The enzyme cyclooxygenase (COX) or prostaglandin endoperoxide H synthase (PGHS) is the key enzyme in the conversion of arachidonic dna-pk inhibitor (AA) into prostaglandins (PGs) [1]. In 1991, researchers found that there were two isoforms of this enzyme called COX-1 and COX-2 with independent genes
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Therapeutic options targeting intrahepatic resistance are ve
2019-09-02
Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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br Materials and methods br Results br Discussion
2019-09-02
Materials and methods Results Discussion The main finding of the present study is that selective ETA and dual ETA/ETB receptor blockade markedly improve endothelium-dependent vasodilatation in patients with type 2 diabetes and vascular complications. The magnitude of improvement did not dif
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br Steroid biosynthesis br Steroid hormone metabolism in
2019-09-02
Steroid biosynthesis Steroid hormone metabolism in breast cancer Conclusion Steroid hormones elicit their biological actions primarily by binding to steroid receptors such as the ER, AR, PR and GR. Although classical breast cancer diagnostic panels assess the expression of the ER and PR, as
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Exposure to UV instead of DMBA also produced a
2019-09-02
Exposure to UV instead of DMBA also produced a sloughing and angiogenic response in transgenic, but not WT, mice, indicating that the epidermis of the BK5.EP4 mice has a much lower apoptosis threshold than WT mice, as suggested by others (Chun and Langenbach, 2007). Overall, these studies suggest th
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Regarding eicosanoid production iPLA VIA appears in general
2019-09-02
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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Our research has demonstrated that the absolute bioavailabil
2019-09-02
Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin
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We postulate that OT contained in milk
2019-09-02
We postulate that OT contained in milk during early postnatal development causes a mild enteroprotective preconditioning of the ER (Fig 9). This is perhaps akin to a mechanism shown by others [50], [51], [52], which is characterized by selective activation of the IRE1a/XBP1/eIF2a (via PKR) UPR pathw
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The kinase activity of DNA PKcs
2019-09-02
The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], lgk974 IV [62], and XLF
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Importantly piPolB holds a great promise for developing nove
2019-09-02
Importantly, piPolB holds a great promise for developing novel biotechnological applications. For instance, in vitro activities of piPolB, namely, strand displacement and faithful, processive DNA polymerization, can be harnessed for efficient primer-independent whole-genome amplification, whereas th
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DGK type I http www apexbt
2019-09-02
DGKη1 (type II DGK) has a separated catalytic domain [10], [13], whereas the domains of DGKα, ε and ζ are not split [1], [2], [3], [4], [5]. Therefore, the structural difference may cause the distinct affinity for DG among these isozymes. Because other type II DGKs (η2, δ1, δ2 and κ) also have the s
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High throughput screening HTS of
2019-09-02
High throughput screening (HTS) of the AstraZeneca umi 2 clinical collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) an
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