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Phagocytosis was observed at min after
2022-01-27

Phagocytosis was observed at 60 min after mixing macrophages with microbes (A). The phagocytosis ability (PA) and phagocytosis index (PI) values of the macrophages engulfing the bacteria measured in flow cytometer were shown in histograms (B). Statistical analyses revealed that both the PA and PI va
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br Conclusion and future perspectives The nicotinic acid
2022-01-27

Conclusion and future perspectives The nicotinic Meleagrin receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid and
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br Materials and methods br Results
2022-01-27

Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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MK-8776 The synthesized methoxyamide derivatives were evalua
2022-01-27

The synthesized -methoxyamide derivatives were evaluated for in vitro as GPR119 agonists (, , ) whereas GSK1292263 (II in ) was used as the reference standard. To identify novel sulfone or tetrazole surrogates, diverse functional groups including amide, -sulfonyl amide, hydrazide, -methoxy--methyla
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GPR agonistic activity was evaluated
2022-01-27

GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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br Evasion strategies for enhanced therapeutic outcomes In o
2022-01-27

Evasion strategies for enhanced therapeutic outcomes In order to increase AED penetration into the CNS, several strategies have been developed over the years to overcome the activity of efflux transporters, by inhibiting their function or by regulating their expression. Due to the high relevance
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BCCA occlusion followed by reperfusion injury significantly
2022-01-27

BCCA occlusion, followed by reperfusion injury, significantly increased the brain AT1 and AT2 receptor expression in mice. Reports have demonstrated elevation of AT1 receptor expression in the cerebral WM-1119 during ischemia [34,35]. The gene expression of brain AT2 receptor is increased in both i
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848 synthesis Throughout the last few decades
2022-01-26

Throughout the last few decades, evidence has accumulated indicating that NTTs, whose primary location is the cell surface, are subject to a series of regulatory processes of intracellular traffic to and from the membrane (Robinson and Jackson, 2016; Vaughan and Foster, 2013). In addition, lateral m
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The previous studies focused on the regulation of GK
2022-01-26

The previous studies focused on the regulation of GK activity by nutrients directly or nutritional hormones (Panserat et al., 2014), there was still a lack of studies paid attention to GK both in activity level and transcriptional level. Besides, the GK regulation by dietary NAD+ sale has been defi
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GCK MODY is the most common form
2022-01-26

GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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The eradication of agonist activity in compound was also con
2022-01-26

The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary hydrocort as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize t
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br Experimental section br Results and
2022-01-26

Experimental section Results and discussion Conclusions To summarize, the act of conjugating a ASC ligands to a Ru(II) polypyridyl subunits resulted in a class of excellent DNA binders. A comparison of the DNA binding abilities of the free ASC ligand and the complexes, has revealed that the
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Many extracellular matrix ECM proteins are ligands and
2022-01-26

Many extracellular matrix (ECM) proteins are ligands and regulators of integrin/FAK signaling and are involved in various aspects of cancer progression, including growth, survival, invasion, and metastasis (Lu et al., 2012). Tubulointerstitial nephritis antigen-like 1 (Tinagl1), a secreted extracell
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mitomycin Neuropathic pain NP is a chronic pain caused by
2022-01-26

Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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In the CNS histamine is known to
2022-01-26

In the CNS, 3CAI sale is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of histamine on ne
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