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However despite medicinal chemistry efforts lead to consider
2022-07-26

However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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br Introduction The signaling molecule nitric
2022-07-26

Introduction The signaling molecule nitric oxide (NO) plays an essential role in vessel homeostasis by initiating vasodilation [1], [2], [3]. After biosynthesis in endothelial cells, NO diffuses into the subjacent smooth muscle layer to reach its target enzyme, soluble guanylyl cyclase (sGC, EC 4
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To solve the atomic structures of several individual domains
2022-07-26

To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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The Scribble complex localizes to the leading edge in
2022-07-26

The Scribble complex localizes to the leading edge in response to integrin engagement. There, Scribble controls the activation Rac and PAK via the Rac GEF β-Pix (Bahri et al., 2010), which is required for collective cell migration (Omelchenko et al., 2014). However, on the rear edge, Scribble can be
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The use of antiinflammatory agents
2022-07-26

The use of antiinflammatory agents has been suggested as a potential treatment in HF. One strategy targeted tumor necrosis factor (TNF) in HF,, but the negative results of the clinical trials have been discouraging., Other clinical trials have attempted to suppress proinflammatory cytokine product
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FR 236924 synthesis Selected GSNOR inhibitors were assessed
2022-07-26

Selected GSNOR inhibitors were assessed for potential off-target activity with a panel of 54 transmembrane and soluble receptors, ion channels, and monoamine transporters. Off-target effects were estimated from the percent inhibition of receptor radio-ligand binding in the presence of 10μM of test c
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br Methods br Results br Discussion
2022-07-26

Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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The hypothesis that genes involved in type diabetes evolved
2022-07-26

The hypothesis that genes involved in type 2 diabetes evolved under changing selective pressures and may carry the signature of natural selection motivated us to describe patterns of sequence variation at CAPN10 and GPR35 in human populations. An initial population genetics study reported an unusual
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Recently a G protein coupled receptor GPR a was identified
2022-07-26

Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Mechanistic studies have suggested that the benefits of niacin therapy may result from the activation of GPR109a located on adipocytes. Recent experiments have shown that niacin activation of GPR109a re
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The importance of FXR FGF signaling in
2022-07-26

The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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br Funding M I is supported by European Research Council
2022-07-26

Funding M.I. is supported by European Research Council (ERC) Consolidator Grant 725038, Italian Association for Cancer Research (AIRC) Grant 19891, Italian Ministry of Health (MoH) Grant GR-2011-02347925, Lombardy Foundation for Biomedical Research (FRRB) Grant 2015-0010, the European Molecular B
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Sephin1 In contrast to UDG SMUG exhibits dramatically
2022-07-26

In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of contam
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A group of small molecule
2022-07-25

A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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We detected the FFAR protein
2022-07-22

We detected the FFAR2 protein with a molecular mass of about 50 kDa, which is comparable to the main band detected in pigs (Li et al., 2014) but different from the calculated size based on the sequence (Wang et al., 2009). The size difference can be explained, at least in part, by glycosylation site
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br Characterization of quantal exocytosis by amperometry A
2022-07-22

Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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