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These observations are of particular interest in
2022-10-02
These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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The current study aimed to understand the
2022-10-02
The current study aimed to understand the roles and the underlying mechanisms of XIST in LSCC, by focusing on the regulation by miR-124-3p, which was previously identified as a target of XIST [12]. We found that the XIST expression is positively correlated with the stages of LSCC in patients. Knockd
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In studies described earlier IRL
2022-10-02
In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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br Drugs approved or in development To date three
2022-10-02
Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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There are many histone H K
2022-10-02
There are many histone H3K9 demethylases, including JMJD1 A, JMJD2 A, JMJD2B, and JMJD2C (Kooistra and Helin, 2012). Considering that EPO YC 1 is regulated by hypoxia, we further analyzed several hypoxia-induced H3K9 demethylases, such as JMJD1 A, JMJD2B and JMJD2C (Beyer et al., 2018; Pollard et al
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br Conflict of interest br Introduction HAT is the founding
2022-10-02
Conflict of interest Introduction HAT1 is the founding member of an expanding class of enzymes known as type B histone acetyltransferases (HATs). HATs are divided into two categories, type A and type B [1]. The type A HATs are nuclear enzymes that acetylate histones in the context of STF 31 a
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The characterization of Da CTSL shows that it
2022-10-01
The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a topotecan phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when secreted by the foregu
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We also examined possible involvement of the NF
2022-10-01
We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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We have previously established the pharmacokinetic profile a
2022-10-01
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in p16 sale and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound
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br Concluding Remarks Given the increasing global
2022-10-01
Concluding Remarks Given the increasing global incidence of metabolic disorders, new drugs that lower body weight and improve glucose tolerance are desperately needed. While we still have a long way to go, GPR55 might be an interesting target to explore, given its expression in numerous metabolic
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Lomustine For molecules with potential for therapeutic
2022-09-30
For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low
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br Materials and methods br Results br Discussion
2022-09-30
Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated Vitamin B12 induced osteogenic effect via Wnt/β-catenin signaling. We found that dose–r
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Metabolism Compound Library synthesis Since the isoflavone e
2022-09-30
Since the isoflavone emerged as privileged scaffold in Hh inhibition, based on molecular modeling predictions and prior studies [17,22], here we designed a number of isoflavones able to interact preferentially with the Smo receptor or the Gli protein. Molecules were synthesized by means of a novel s
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br Materials and methods br Results br Discussion Ghrelin is
2022-09-30
Materials and methods Results Discussion Ghrelin is required for maintenance of glucose homeostasis under fasting conditions, and GHSR-null mice have low fasting blood glucose levels [5], [9]. In this study, we found that restoration of GHSR in nodose ganglion neurons rescued low fasting bl
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In addition to the four classical FGFRs there is an
2022-09-30
In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i
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