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Concerning the molecular mechanisms underlying transcription
2022-03-28

Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1
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br Discussion In the present paper it was
2022-03-28

Discussion In the present paper it was shown for the first time that the conjugation of ethacrynic Clofazimine and glutathione catalyzed by GSTP1-1 stereospecifically forms one of the diastereoisomers of the glutathione conjugate (EASG). Chemical conjugation results in formation of a mixture of b
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br Conclusion br Conflict of interest br References
2022-03-28

Conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Free fatty acids (FFAs) are essential nutrients that contribute to various cellular functio
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94 8 Ning et al showed that
2022-03-28

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Recently higher grade varicoceles have been reported to be
2022-03-28

Recently, higher-grade varicoceles have been reported to be associated with higher nocturia levels [20], and we observed an interesting phenomenon in which the urine volume/water intake ratio dramatically increased in the rat model of experimental left varicocele (ELV); the decreases in hypothalamic
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In parallel we were also preparing and evaluating
2022-03-28

In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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br Discussion The GlyR is responsible
2022-03-28

Discussion The GlyR is responsible for mediating much of the neuronal inhibition in the brainstem and spinal cord, although these receptors are also found in a number of higher brain regions (Baer et al., 2009, Jonsson et al., 2012, Jonsson et al., 2009, Lynch, 2004). A variety of structurally-di
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Tetrazole is one of the most commonly used
2022-03-28

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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Introduction The brain contains abundant fatty acids which s
2022-03-28

Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev
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The role for noggin in telencephalic
2022-03-28

The role for noggin in telencephalic development and also adult neural stem cell expansion and differentiation has been debated, and noggin has been suggested to exert diverse effects in these events (Bachiller et al., 2000, Bonaguidi et al., 2008, Colak et al., 2008; de Chevigny et al., 2008, Li et
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Fourthly the distribution sites after i c v injection
2022-03-26

Fourthly, the distribution sites after i.c.v. injection of FAM-ghrelin(1–7)-NH2 were explored in mice using the technologies of fluorescence labeling. The green fluorescence of FAM-ghrelin(1–7)-NH2 was strongly distributed in these structures of lateral ventricle, lateral septal nucleus, dorsal part
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Bile acids BAs are critical
2022-03-26

Bile acids (BAs) are critical for facilitating the Silydianin of dietary lipids and lipid-soluble vitamins in the intestines [6], [7]. At physiological levels, BAs function as signaling molecules and activate specific nuclear receptors [farnesoid X receptor (FXR), pregnane X receptor, and vitamin D
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Growing evidence supporting the anti inflammatory and tissue
2022-03-26

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 Results and discussion br Conclusions As described above
2022-03-26

Results and discussion Conclusions As described above, the SAR study based on compound 1 led to the identification of compound 4 as an ideal inhibitor. An enzyme level investigation showed that 4 is a more potent and selective FGFRs tyrosine kinase inhibitor than is Ponatinib. In addition, the
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Recent research has focused on
2022-03-26

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty 5(S),6(R)-7-trihydroxymethyl Heptanoate receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells,
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