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Although the presence of histamine secreting bacteria
2022-06-30

Although the presence of histamine-secreting bacteria has been well documented in foods, their presence within the human gut microbiota has not been investigated in detail. We recently performed an analysis of fecal samples from 161 volunteers to quantify the presence of bacterial HDC, using primers
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In conclusion re evaluation of HER
2022-06-30

In conclusion, re-evaluation of HER2 status is necessary to determine the appropriate use of anti-HER2–targeted therapy beyond disease progression. EGFR and c-met amplification, as well as PIK3CA mutation, are rarely associated with acquired resistance. Our results highlight the importance of formal
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br Heme oxygenase inhibitors Historically the first class of
2022-06-30

Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron Sulfo-NHS-LC-Biotin of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for bindi
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As a possible back up to Sch
2022-06-30

As a possible back-up to Sch 503034 (), we explored inhibitors that contained alternative electrophiles to ketoamides. Boronic acids have been extensively investigated as possible electrophiles that could react with nucleophilic serine in the context of developing inhibitors of thrombin receptor and
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The observed glucose intolerance and elevated fasting blood
2022-06-29

The observed glucose intolerance and elevated fasting blood glucose in this study is in consonance with earlier study (Ferris and Kahn, 2012). These have been the common features of GC exposure and are not unexpected. Previous researches that reported IR during GC exposure have shown controversy con
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In summary we have designed and optimized a new
2022-06-29

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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Indacaterol Maleate br Regulation of gonadotropins by GnRH G
2022-06-29

Regulation of gonadotropins by GnRH GnRH is released from the hypothalamus, and its release pattern is known to be pulsatile. That is, the pulse frequency and amplitude of GnRH release vary physiologically during reproductive cycles in females, and differentially stimulate the production and rele
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GHSR A s have high levels of constitutive activity and
2022-06-29

GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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Moreover after the initial bleaching
2022-06-29

Moreover, after the initial bleaching of the fluorescent molecules in the targeted cell exposed to laser illumination, the neighboring reservoir fluorescent probes are expected to give in return new fluorescent ones if the cells are coupled together by gap junction channels. This supposes that the
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The focused set of cyclopentapyrazoles
2022-06-29

The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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The focused set of additional pyrazole analogs allowed the
2022-06-29

The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro su
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Determination of enzyme activity differs
2022-06-29

Determination of enzyme activity differs from other analytical procedures. In this ER 27319 maleate case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic
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br Conflict of interest br Acknowledgments The research was
2022-06-29

Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be
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Focal adhesion kinase FAK is a
2022-06-29

Focal adhesion kinase (FAK) is a non-receptor type tyrosine kinase that can further cooperatively interact with receptor tyrosine kinase signaling to regulate adhesion, migration, survival, proliferation, polarization, and differentiation [12]. Following activation, phosphorylated extracellular regu
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Cyclopamine a steroidal alkaloid type secondary metabolite f
2022-06-28

Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas
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