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As previously stated the most
2021-04-29
As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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Previous studies reported that NE and MHPG are deeply involv
2021-04-29
Previous studies reported that NE and MHPG are deeply involved in depression and that NE reuptake inhibitors are approved for use in patients with depression (for review, see [2]). We found increased hippocampal content of NE and MHPG in the CORT-treated CRTH2−/− mice (Fig. 3). In the hippocampus, a
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Next our exploration shifted to modifications
2021-04-29
Next, our exploration shifted to modifications at the lateral chain of the benzoquinone nucleus (SAR 2). Considering that the CK2 inhibitory activity is favoured by the presence of the -Ph-4-NO2 (SAR 1), the subsequent analogues were investigated with this moiety retained. The influence of the side
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IT-901 br Discussion Cytomegalovirus CMV is a
2021-04-28
Discussion Cytomegalovirus (CMV) is a herpes virus that causes primary infection in normal hosts and re-activation infection in compromised hosts with impaired CMI, e.g., organ transplants. Following primary infection, which may be severe, CMV becomes latent in lymphocytes. Reactivation may occur
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R 59-022 Research done thus far supports the
2021-04-28
Research done thus far supports the hypothesis that MPA has detrimental effects on cognition, alone and in combination with estrogen; there are other FDA-approved progestogens that satisfy the uterus opposing effects that have not been cognitively profiled. An important goal to aid women's health is
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Introduction Neuropathic pain occurs in approximately one
2021-04-28
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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The optimization of the lead
2021-04-28
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic GSK1210151A moiety with other functional groups led to loss of functional activity against EP4 receptor. A
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VU 0364439 synthesis br O GlcNAc transferase OGT belongs to
2021-04-28
O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t
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br Acknowledgements br Introduction Endothelial cells consti
2021-04-28
Acknowledgements Introduction Endothelial tie2 constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile roles in mainta
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Downregulation of tumor suppressors is a major factor
2021-04-28
Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the Propidium iodide mg of which is often downregulated or even absent in the majority of human cancers, functions as a phosp
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br Discussion The regulation of
2021-04-28
Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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br Materials and methods br Results br Discussion br
2021-04-28
Materials and methods Results Discussion Conflict of interest Introduction Dopamine-β-hydroxylase (DβH) deficiency is a rare autosomal recessive disorder characterized by the congenital absence of DβH, the enzyme converting dopamine to noradrenaline in sympathetic nerve terminals and
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Industrial fermentation aims to produce valuable products fr
2021-04-28
Industrial fermentation aims to produce valuable products from cheap feedstocks by utilizing diverse microbial functions through aerobic or anaerobic fermentation [[8], [9], [10]]. During anaerobic fermentation, the reducing power is mostly directed to product synthesis rather than being oxidized, r
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Having generated synthetic cytokines and synthetic cytokine
2021-04-27
Having generated synthetic cytokines and synthetic cytokine receptors, the logical next step has been to design fully synthetic cytokine/cytokine receptor systems, modifying either cytokine/cytokine receptor binding interfaces or cytokine-unrelated combinations of substances and their binding domain
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CysLTs trigger contractile and inflammatory
2021-04-27
CysLTs trigger contractile and inflammatory processes through the specific interaction with cell surface receptors belonging to the rhodopsin family of the G protein-coupled receptor (GPCR) genes. Until now, two receptor subtypes have been cloned, namely CysLT1 and CysLT2[8]. In particular, when the
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