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Having taken a step back from affinity to gain better
2023-08-28
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br Materials and methods Bacterial strains and growth condit
2023-08-28
Materials and methods Bacterial strains and growth conditions. Escherichia coli TOP10 and E. coli BL21Star (DE3) (ThermoFisher, Waltham, MA) were grown at 37 °C in Luria broth (LB) or LB-agar containing kanamycin (50 μg/ml). Bioinformatic analyses. The amino inos inhibitor sequence of Rv2477c wa
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Since obesity appears to impact leptin and adiponectin level
2023-08-28
Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic s
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The regulation of gene expression by glucocorticoids can
2023-08-28
The regulation of gene expression by glucocorticoids can be mediated either by the canonical mechanism that involves the interaction of the glucocorticoid receptor (GR), a transcription factor activated by the hormone, with glucocorticoid response element (Ye et al., 2007), or by the non-canonical m
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br Findings br Discussion br Conclusions Midwives were
2023-08-28
Findings Discussion Conclusions Midwives were more likely to provide effective antimalaria services (including two doses of IPT during the second and third trimesters of pregnancy) to pregnant women if Conflict of interest Authors’ contributions Funding Acknowledgements Resea
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br Acknowledgements We thank the National Natural Science
2023-08-28
Acknowledgements We thank the National Natural Science Foundation of China (41576156), Shandong Province Science and Technology Development Plan (2015GSF121045), Yantai Science and Technology Development Plan (2015ZH078), and the Public Science and Technology Research Funds Projects of Ocean (No.
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br Conclusions Our study confirms that N terminal
2023-08-28
Conclusions Our study confirms that N-terminal mutations can affect Aβ fibril and oligomer formation, despite lying outside the core amyloid region of Aβ. Of the three factors that may influence Aβ-mediated toxicity (primary structure of Aβ, assembly structure and cellular responses), our results
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Adenosine can modulate neutrophil bactericidal functions
2023-08-26
Adenosine can modulate neutrophil bactericidal functions. A dual regulatory effect has been reported for adenosine on phagocytosis. Indeed, the activation of A1 receptors augments this process, while the stimulation of A2A receptors was found to reduce the phagocytic activity of neutrophils [89]. In
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The purpose of the present study is
2023-08-26
The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos
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Molecular docking is widely used to predict
2023-08-26
Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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Many metalloenzyme inhibitors consist of two chemical compon
2023-08-26
Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino igf 1 inhibitor residues that form the substrate-binding site of the metalloenzyme. The MGB i
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Plasma apelin levels predict the major cardiovascular event
2023-08-26
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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The physiologic conditions and signaling mechanisms that reg
2023-08-26
The physiologic conditions and signaling mechanisms that regulate apelin secretion and APLNR expression in malignant tissues appear to be multifactorial. Previous studies have shown that hyperplastic and neoplastic cholangiocytes secrete a variety of hormones, peptides, and growth factors that help
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br Perspectives br Acknowledgments This investigation was su
2023-08-26
Perspectives Acknowledgments This investigation was supported by a Research Grant 2010/01385-5 from FAPESP (Sao Paulo Research Foundation, Brazil). P.F.S. was recipient of a CNPq (National Council for Scientific and Technological Development, Brazil) productivity grant. R.F.A. was recipient o
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Analysis of the enzyme activity expressed as
2023-08-26
Analysis of the enzyme activity, expressed as rate of product formation per unit serum volume (20μl), between the diagnostic groups revealed that ApB activity was significantly decreased in the patient group both at recruitment and after 13months when the substrate concentration used was 1.5mM (pthe
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