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br Materials and methods br Results br
2021-09-27

Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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br Conflict of interest br Acknowledgements This work
2021-09-27

Conflict of interest Acknowledgements This work was funded by the University of Turin (ex60% 2014), World Wide Style Project (WWS; University of Turin/Fondazione CRT) and University of Florence (ex60% 2014). ACR and AP designed the study; AP, EB and IO conducted the literature search and analy
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It has been well established that triazophos is
2021-09-27

It has been well established that triazophos is a classic resurgence-inducing insecticide favoring N. lugens population growth by fecundity stimulation, with enhanced contents of soluble sugar, crude fat, soluble protein content of fat body and ovary, glucose and trehalase activity but reduced treha
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Considering that TGF plays a pivotal role in inflammation
2021-09-27

Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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The second approach to optimizing
2021-09-27

The second approach to optimizing microsomal stability in this series involved the strategic positioning of steric bulk along the tether as a means of encumbering the access of oxidative enzymes to the methylene bridge. This approach has been employed in other P2-P4 macrocyclic inhibitors of NS3/4A
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br Methods br Results br Discussion Peptide therapeutics rep
2021-09-27

Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succe
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si cid br NO GC pathway and implications
2021-09-27

NO-GC-1 pathway and implications for glaucoma Direct in vivo measurement of NO in the eye is not yet feasible. However, measurement of nitrate and nitrite levels are routinely used as markers for the activity of NOS and the production of NO radicals [98]. Several studies in human glaucoma patient
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In this study we demonstrate that HHcy upregulated
2021-09-27

In this study, we demonstrate that HHcy upregulated the expression of GSNOR in T cells. As a result, GSNOR induced denitrosylation of Akt in Hcy-activated T cholecystokinin receptor in vivo and in vitro, which contributed to vascular inflammation and susceptibility to atherosclerosis in GSNOR-/-Apo
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Using embelin and its analogs as surrogate GPR agonists we
2021-09-27

Using embelin and its analogs as surrogate GPR84 agonists we discovered that GPR84 couples to G12 and G13 signaling pathways in addition to Gi, linking receptor function to Rho/Rac signaling and modulation of the cytoskeleton. In primary human macrophages, GPR84 activation leads to Gβγ signaling, Er
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br Conflict of interest statement br Acknowledgments The
2021-09-27

Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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Previously we reported that the inhibition
2021-09-27

Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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br Results br Discussion br Materials and Methods br
2021-09-27

Results Discussion Materials and Methods Introduction Deoxyribonucleic Vidofludimus (DNA) is among the most important biopolymers in living organisms alongside carbohydrates and proteins. DNA is a linear polymer consisting of four types of nucleobases, deoxyribose, and phosphate. The ba
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Oxipurinol In this study with the use of
2021-09-27

In this study, with the use of 13C515N2-labeled glutamine, we observed that 13C515N2-labeled glutamine produces a wide range of NAAG isotopologues and its precursors: NAA and glutamate. The NAAG production from glutamine is consistently more elevated in MYC-ON lymphoma and OVCAR4 compared to MYC-OFF
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GLP is released in response to ingestion of
2021-09-26

GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty GSK2636771 receptor 4 (FFA4/GPR120) as a potential 7TM receptor involved in
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Recently Bristol Myers Squibb and Merck
2021-09-26

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic tankyrase derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists
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