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In the a first in vitro indication
2021-10-21
In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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According to the World Health Organization
2021-10-21
According to the World Health Organization, the average global intake of fat has increased by 20 g per person over the last half-century [21]. However, not all fats are the same and it is now well established that saturated and unsaturated fats, as well as trans fats, can act in opposing ways to inf
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Growing evidence supporting the anti inflammatory and tissue
2021-10-21
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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br General features of FGFRs and inhibitors br Conclusion Gi
2021-10-21
General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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Importantly HDACi mediated effects are cell and HDAC specifi
2021-10-21
Importantly, HDACi-mediated effects are cell and HDAC specific; different effects and outcomes have been observed in different cell types, targeting different HDAC isoforms. While HDACi exhibit a strong proapoptotic potential in human leukemia bioactive 19, 20, 21, 22, they have a limited ability t
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Stability of DBS over the day time
2021-10-21
Stability of DBS over the 60-day time points was encouraging, with a maximum of 0.1 log10 IU/mL degradation from the day 1 value (Supplementary Fig. 1 and Supplementary Table 3). Discussion This study evaluated the sensitivity and specificity of the Aptima HCV Dx assay for HCV RNA detection from
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G protein coupled receptor kinases GRKs are
2021-10-21
G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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A repertoire of cytotoxic payloads is increasing among
2021-10-21
A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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Unlike the bacterial SRP pathway for which the
2021-10-20
Unlike the bacterial SRP pathway for which the energetics, kinetics, and structure of almost every intermediate have been characterized, multiple questions remain for the GET pathway (Figure 3, marked with ‘?’). First, the targeting pathway demands distinct activities of Get3 before and after substr
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One important aspect about GSK inhibitors is their effect on
2021-10-20
One important aspect about GSK-3 inhibitors is their effect on pluripotency of Taurine [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of events preserv
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As well as the above studies Meier and coworkers
2021-10-20
As well as the above studies, Meier and coworkers used TUG-891, alongside omega-3 fatty acids, to show a potential role for FFA4 in inhibiting proliferation of DU145 prostate cancer cells [68]. Given that these cells express both FFA4 and FFA1 and the current view that TUG-891 may not be sufficientl
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More recently NMR techniques have been
2021-10-20
More recently, NMR techniques have been used to monitor K+ () fluxes in isolated rat hearts. These reveal an increased rate of passive efflux of from Langendorff-perfused hearts at 20°C compared to 36°C or 10°C (Gruwel, Kuzio, Xiang, Deslauriers, & Kupriyanov, 1998). Similar experiments assessed th
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Akt mTOR signaling pathway is a major
2021-10-20
Akt/mTOR signaling pathway is a major negative regulator of autophagy, via modulating ULK1 complex. It is well established that Inhibition of mTOR by deprivation of nutrients or growth factors, led to dephosphorylation of ULK1, ULK2, and Atg13 in human cells, which is a key step for ULK1 complex ass
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The molecular formula of was determined
2021-10-20
The molecular formula of 2 was determined to be C20H26O5 on the basis of HRESI (−) MS data at m/z 345.1705 [M–H]− (calcd 345.1702 for C20H25O5). Detailed analysis of the 1H and 13C NMR data of 2 revealed similar fragments compared with desoxyarticulin (Faini et al., 1987) except for an additional hy
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br METHODS br RESULTS br Discussion Numerous
2021-10-20
METHODS RESULTS Discussion Numerous studies have proposed various hypotheses and models to explain how neuroinflammation could contribute to the chronic fatigue, postexertional fatigue, and cognitive deficits observed in patients with ME/CFS.12, 13, 14, 15 Although neuroimaging studies have
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