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Recently several dual GLP GIP receptor
2021-11-18

Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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FFA expression was also noted
2021-11-18

FFA4 expression was also noted to be upregulated in eight human CRC cell lines. Compared to two normal colon cell lines with relative one-fold expression of FFA4, CRC cell lines HCT116 (3.5-fold higher), Colo205 (3-fold), Caco-2 (2.2-fold), HT-29 (2.3-fold), RKO (2.8-fold), DLD-1 (2.9-fold), SW480 (
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In the current study we report the properties of
2021-11-18

In the current study, we report the properties of P. anserina mutants carrying mutations in a gene encoding the bi-functional enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFK-2/FBPase-2). This enzyme catalyzes two opposite reactions (Pilkis et al., 1995, Rider et al., 2004): synthesi
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DZNep is a PRC inhibitor that
2021-11-18

DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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In C elegans KDM A appears
2021-11-18

In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene
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Studies of human and mouse GPR
2021-11-18

Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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Lipid sensing GPCRs as therapeutic targets G protein
2021-11-18

Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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Despite the rapid development of
2021-11-18

Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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In summary we have designed and optimized a new
2021-11-17

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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LPC OMe LPC LPC and OMe LPC were shown
2021-11-17

LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated ursolic aci
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In both families GPR A mRNA
2021-11-17

In both families, GPR109A mRNA in kidney fat was positively correlated with NEFA as a tendency. A positive correlation between this fat depot and insulin was observed in lean-type cows. In fat-type cows, mesenteric GPR109A mRNA correlated positively with insulin and negatively with urea on a moderat
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A-740003 Ginger derived glycoproteins contain a variety of f
2021-11-17

Ginger-derived A-740003 contain a variety of functional components, including specific phenolic compounds, purine compounds, and bioactive polysaccharides. Moreover, glycoproteins belong to the glycoconjugates, which combine some of the properties of polysaccharides and proteins. It has been reporte
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br Introduction L Glutamate is one of the
2021-11-17

Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of Thiamet G mg functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated concent
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FFAR is highly expressed not only
2021-11-17

FFAR1 is highly expressed not only in β cells but also in α xylometazoline receptor (Segerstolpe et al., 2016), which gives the interesting perspective that 20-HETE may function both as an autocrine and as a paracrine regulator of islet cell function (Figure 1A), i.e., acting in symphony with the m
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The molecular identity of RA s target during LTP
2021-11-17

The molecular identity of RA’s target during LTP induction was determined by pharmacological testing. The inhibitory effects of CNQX and niflumic acid on LTP induction remained even in the presence of RA, indicating RA did not affect either the AMPA receptor nor chloride channel (Fig. 2B and D) [26]
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