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br ACKNOWLEDGMENTS br Introduction Odorant receptors ORs are
2021-10-14
ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed an
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br Factor Xa an enzyme in the coagulation cascade has
2021-10-14
Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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br Discussion Considering cardiovascular risk factors there
2021-10-14
Discussion Considering cardiovascular risk factors, there was a significant difference in prevalence of dyslipidemia in both groups, 57.5% in HIV-infected stroke patients compared to 8.9% in the HIV-uninfected patients. These results are similar to that of Chow et al. who found a dyslipidemia pre
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When studying the potential of HATi for the treatment
2021-10-14
When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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br For some time it was known that membrane bound
2021-10-14
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor Gentamycin Sulfate in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on
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Waldeck Weiermair et al demonstrated that in endothelial
2021-10-14
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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br Materials and methods br Results br Discussion According
2021-10-14
Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 WIN 18446 has been identified within discrete regions of the nervous
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br AUTHOR CONTRIBUTIONS br ACKNOWLEDGMENTS br Introduction C
2021-10-14
AUTHOR CONTRIBUTIONS ACKNOWLEDGMENTS Introduction Chronic neuropathic pain is a common symptom in patients with human immunodeficiency virus (HIV)-1 infection. Glycoprotein 120 (gp120) is an HIV-1 protein that can cause pain behaviors in animal models (Hao, 2013, Nasirinezhad et al., 2015,
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The structure and activity of GLUT has
2021-10-14
The structure and activity of GLUT1 has been most intensively studied in erythrocytes, in which this transporter makes up 10–20% of membrane protein content. Carruthers has shown that, while GLUT1 can exist and transport glucose as monomers, dimers and tetramers, in erythrocytes GLUT1 exists predomi
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Acknowledgments br Introduction The gut
2021-10-14
Acknowledgments Introduction The gut-derived hormone oxyntomodulin (OXM) is a naturally occurring dual agonist of both the glucagon receptor (GCGr) and glucagons-like peptide 1 receptor (GLP-1r). Structurally OXM is the 29 Cytarabine of glucagon with a C-terminal octapeptide tail. Administratio
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MAPK are involved in a large
2021-10-14
MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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Benzamil br Experimental section br Acknowledgements This st
2021-10-13
Experimental section Acknowledgements This study was supported by grants from the National Natural Science Foundation of China (Grants 81673299 and 81273376). Introduction Free fatty acids (FFAs) are important metabolic fuels and those that are polyunsaturated are essential components of t
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With the nitrogen containing heterocycle components and the
2021-10-13
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic TC 14012 receptor (, and ), followed by deprotection by TFA, smoothly provid
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Moving forward to series the energy minimized conformation o
2021-10-13
Moving forward to series , the energy minimized conformation of A 967079 within the binding pocket is quite interesting. The indole-based tail guides the TZD head for a highly-favored interaction with all residues of the H-bonding triad (). In addition, an extra bonding with H449 in the AF-2 helix w
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Over decades a deeper understanding
2021-10-13
Over decades, a deeper understanding of terpene synthases has also permitted enzyme engineering for unnatural substrate acceptance. Novel terpenoids have been successfully synthesized from substrate analogues as by-products from mechanistic investigation (Faraldos et al., 2012; Miller, Yu, & Alleman
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