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Although it has been observed in numerous studies and
2022-02-08

Although it has been observed in numerous studies and by many investigators that intraplatelet cGMP elevation results in platelet inhibition, there are a few papers which proposed a platelet stimulatory role for cGMP when elevated in response to NO donors or PDE5 inhibitors in mouse and human platel
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Decreasing GSK activity has therapeutic benefits in animal m
2022-02-08

Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic GPCR Compound Library injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregu
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O-propargyl-puromycin mg In addition to these effects on met
2022-02-08

In addition to these effects on metabolic function in cardiac cells, this study also demonstrates changes in the expression of hypertrophic genes and proteins subsequent to GPR119 activation. Again this occurred in a distinct pattern dependent on palmitate exposure. Of interest SOCS3 mRNAs were decr
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GPR is a member of the
2022-02-08

GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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Antibiotic treatment suggests that cancer promoting
2022-02-07

Antibiotic treatment suggests that cancer-promoting bacteria arise from the two types of active transport of Grp109a mice. How does the lack of Gpr109a signaling lead to expansion of potentially cancer-promoting bacteria? Is this phenomenon related to improper development of intestinal Treg cells?
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glucokinase inhibitor Studies of human and mouse GPR as asce
2022-02-07

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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Our study has some limitations that should be
2022-02-07

Our study has some limitations that should be considered when the results are interpreted. First, we did not measure the protein levels of Bax and Bcl2, due to time and budget limitations. Although simultaneous measurements of both mRNA and protein levels are complementary for a better understanding
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Homeobox genes can promote oncogenesis through
2022-02-07

Homeobox genes can promote oncogenesis through multiple mechanisms, including gene translocation, loss of heterozygosity, gene amplification, DNA methylation, Nimodipine receptor remodeling, etc. For instance, translocation-mediated fusion of HOXA9 or HOXA13 on chromosome 7p15 with the nucleoporin
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br Discussion and concluding remarks FPR
2022-02-07

Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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Ligand selectivity may directly be
2022-02-07

Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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PD 169316 receptor At the heart of ferroptosis is a process
2022-02-07

At the heart of ferroptosis is a process of lethal lipid peroxidation, which is the oxidative addition of molecular oxygen (O2) to lipids, such as polyunsaturated fatty acyl tails in phospholipids. The first descriptions of such enzymatic reactions were in 1955 by Peterson and colleagues [50] and Ro
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Sequences of HKI and HKII from humans
2022-02-05

Sequences of HKI and HKII from humans were compared to those of the Atlantic salmon to better understand the observation of HKI movement to the mitochondrial fraction in this study, as HKI in mammals is commonly assumed to be mostly passively regulated by product inhibition, with little evidence of
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br Role of dynamin in NPRA
2022-02-05

Role of dynamin in NPRA endocytosis In recent studies using 125I-ANP binding assay and confocal microscopy, we have examined the role of dynamin in the internalization and trafficking of NPRA in a stably transfected HEK-293 GSK 0660 synthesis [69]. Our findings indicated that ANP treatment of hi
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Pharmacologic approaches of inhibiting GSNOR activity have r
2022-02-05

Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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Human GPR hGPR was originally isolated in as an
2022-02-05

Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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