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br Although there are growing
2022-06-08
Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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In conclusion while class I
2022-06-08
In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides
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It is known that changes in cGMP levels
2022-06-08
It is known that changes in cGMP levels are positively correlated with plant adaptation to environmental stresses. It seems that a novel group of moonlighting kinases with GC activity is particularly involved in response to biotic stress. It was shown that danger-associated molecular pattern (DAMPs)
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Melanocyte stimulating hormone release inhibiting factor Int
2022-06-08
Introduction Soluble guanylyl cyclase (sGC) is a key protein in the regulation of multiple physiological functions in mammalian physiology [1,2]. Upon stimulation by nitric oxide (NO) [3], sGC generates cyclic guanosine monophosphate (cGMP) from guanosine-5′ triphosphate and activates protein kinas
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br Materials and methods br Results
2022-06-08
Materials and methods Results Discussion In this report, we have analyzed the function of an orphan GPCR, and GPR84, using genetically-deficient mice. The expression of GPR84 in the T and D-Mannitol in the spleen prompted us to examine the functional responses of these cells under in vitro
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br Acknowledgements br Introduction Type diabetes is a progr
2022-06-08
Acknowledgements Introduction Type 2 diabetes is a progressive metabolic disorder which is characterised by chronic hyperglycaemia due to relative insulin deficiency, insulin resistance and increased hepatic glucose production [1]. The metabolism of glucose by glycolysis increases the ATP:ADP
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Human GPR hGPR was originally isolated in as an orphan
2022-06-08
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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br Gastrointestinal peptides and intestinal health Gastroint
2022-06-08
Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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br The presence of an
2022-06-08
The presence of an active glyoxalase pathway in an apicomplexan parasite was first reported in Plasmodium falciparum-infected erythrocytes (Vander Jagt et al., 1990). Some years later, glyoxalase I and both glyoxalase II enzymes were characterized in this parasite (Akoachere et al., 2005, Iozef et
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One of the main clinical
2022-06-08
One of the main clinical issues of ABCB1, together with its impact on intestinal absorption, concerns its location at the BBB. Indeed, ABCB1 has been identified in the luminal side of endothelial cells and in the abluminal side of astrocyte endfeet processes of the CNS microvasculature [[36], [37],
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The knowledge that piroxicam competes with
2022-06-07
The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re
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br Discussion and concluding remarks FPR
2022-06-07
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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To investigate an involvement of GPR and
2022-06-07
To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) Biotin-11-dUTP australia were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 c
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br Conclusion In summary a series of novel GPR agonists
2022-06-07
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic ddhC motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent activ
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We then explored the possible mechanisms by which integrin w
2022-06-07
We then explored the possible mechanisms by which integrin α5β1 was involved in the PHEV proliferation process. Normally, the virus activates integrin and induces its downstream protein activation to promote its own invasion and proliferation. Human papillomavirus type 16 (HPV16) binds to heparan su
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