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br All platelet agonists acting
2022-05-04

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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Spermine NONOate Glutathione transferases GST have been disc
2022-05-04

Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To da
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Waldeck Weiermair et al demonstrated that
2022-05-04

Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp
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Introduction Although G protein coupled receptor GPR
2022-05-04

Introduction Although G-protein-coupled receptor 55 (GPR55) was considered a cannabinoid receptor, it differs phylogenetically from cannabinoid type 1 (CB1) and type 2 (CB2) receptors as it lacks the classic cannabinoid-binding pocket (Baker et al., 2006). GPR55 is sensitive to an array of cannabi
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As part of our discovery efforts searching for
2022-05-04

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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In recent large clinical studies AIM
2022-05-04

In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic nociceptin receptor to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secon
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Stattic mg Molecular properties as well as metabolic
2022-05-04

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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EGTA Over expression of Glo can suppress inflammatory
2022-05-04

Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial EGTA [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen expression
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Additionally increased GLO gene expression protein
2022-05-04

Additionally, increased GLO1 gene expression, protein expression, and activity have been reported in a variety of cancers, including breast,22, 23, 24 pancreatic, melanoma, and prostate.27, 28, 29 Vince and Daluge proposed that inhibitors of GLO1 could serve as anti-tumor agents, by increasing conce
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Taking into account abovementioned vitamin D deficiency effe
2022-05-04

Taking into account abovementioned, vitamin D3 deficiency effects on synaptic neurotransmission can be considered as targeting both Ca2+-independent and Ca2+-dependent processes. Ca2+-independent action of vitamin D3 deficiency is associated with a decrease in the expression of glutamate and GABA tr
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The developed method was used to
2022-05-04

The developed method was used to quantify RBC membrane transport of the anomers of three monofluorinated analogs of glucose in a modified medium designed to provide stable metabolic properties of the cells over the lifetime of the experiment. This allowed us to evaluate the specific interaction (spe
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A localization of GK to both a
2022-05-04

A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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A localization of GK to both a
2022-05-04

A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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It is notable that pharmacological or genetic inhibition of
2022-05-04

It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin con
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br Introduction Connexins are transmembrane proteins that al
2022-05-04

Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent Oligomycin A receptor via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nutrients to the e
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