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FPR activation stimulates multiple signal transduction pathw
2021-10-18
FPR1 activation stimulates multiple signal transduction pathways responsible for various neutrophil functions, such as adhesion, chemotaxis, phagocytosis, fosaprepitant dimeglumine of secretory granules, and superoxide anion radical (O2) production, which contribute to the physiological inflammator
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br Materials and methods br Results br Discussion The distri
2021-10-18
Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta azidothymidine [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adip
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The presence of FBP in
2021-10-18
The presence of FBP2 in nuclei seems to accompany the cells' potential to divide as it has been shown that during differentiation of the satellite cells (myogenic progenitor cells) the amount of nuclear FBP2 decreases and in differentiated myotubes, the localisation of FBP2 is restricted to cytoplas
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Fig C presents the secondary structure arrangement of the
2021-10-18
Fig. 1(C) presents the secondary structure arrangement of the PAS-A and PAS-B domains in both HIF-2α and ARNT. The common scaffold of the PAS domains is a β sheet with numerous flanking α helixes. The PAS-A domains of both HIF-2α and ARNT have A’α, Aβ, Bβ, Cα, Dα, Eα, Fα, Gβ, Hβ, and Iβ from the N t
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Initially the synthesized compounds from were evaluated for
2021-10-18
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic VE-821 having similar termina
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It has been proposed that HCA may
2021-10-18
It has been proposed that HCA1 may be a better target than HCA2 to treat dyslipidemia and to prevent progression of atherosclerosis, because HCA1 is less widely expressed, and HCA1 activation does not result in flushing. However, since the antilipolytic effects mediated by HCA2 appear to be not the
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br Action of GPR in metabolically active tissues In addition
2021-10-18
Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.
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Continuing studies of endocannabinoid ligands at
2021-10-18
Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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In addition researchers studying GPR agonists favor the deve
2021-10-18
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it inos inhibitor is unclear why Sanofi-Aventis chose to terminate collaboration with Metabo
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br TGR Agonists br FXR TGR Dual Agonists In
2021-10-18
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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br Results br Discussion The twin cysteine motif is
2021-10-18
Results Discussion The twin-cysteine motif is an evolutionary conserved motif in all primate lentiviruses except HIV-1 and some strains of SIVcpz according to sequence analysis (Bohl et al., 2013). It is assumed that only those SIVcpz which have lost the twin-cysteines successfully evolved to
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Elevated methylglyoxal levels also contribute to
2021-10-18
Elevated methylglyoxal levels also contribute to carbonyl stress, cytotoxicity, DNA damage, apoptosis and cell death. These mechanisms may be important for normal aging of the nervous system as well as for the development of neurodegenerative diseases such as Alzheimer's and Parkinson's disease wher
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Among the various delivery strategies in the field
2021-10-18
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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Glutamate is a ubiquitous principal
2021-10-18
Glutamate is a ubiquitous principal excitatory neurotransmitter in the inhibitor of apoptosis proteins that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive
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Epidemiological evidence indicates that neuroinflammation pl
2021-10-18
Epidemiological evidence indicates that neuroinflammation plays a pivotal role in pathogenesis of AD (Heneka et al., 2015, Heneka et al., 2013, Holmes et al., 2009, Liu et al., 2016). For example, prolonged treatment with nonsteroidal anti-inflammatory drugs reduces the risk of developing AD (In et
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