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A compound structurally similar to PF has been developed
2022-10-10
A H-Lys(Ac)-OH.HCl receptor structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-yl
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The repurposing of well characterized
2022-10-10
The repurposing of well-characterized and well-tolerated drugs in order to treat illnesses for which they were not originally intended has emerged as an attractive alternative to a long and costly process of drug development. Repositioning antihistaminergic ligands seems a promising idea given that
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br Material and methods br Results and discussion Unlike man
2022-10-10
Material and methods Results and discussion Unlike many fruits such as bananas and tomatoes, known as climacteric fruits, in which ripening is regulated by a burst of 5-Ethynyl-2'-deoxyuridine biosynthesis and an increase in respiration, pepper fruits, which do not follow this pattern, are ca
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GPR GPR GPR GPR and
2022-10-10
GPR80, GPR81, GPR82, GPR93 and ψGPR79 all shared identities to P2Y GPCRs or P2Y-like oGPCRs. Previously, at least three different nucleotide receptor phenotypes have been observed in mammalian tissue, including GPCRs activated by c1 v1 c2 v2 nucleotides (e.g. P2Y1 and P2Y11), uridine nucleotides (e
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Notably we observed that GPR
2022-10-10
Notably, we observed that GPR35 activation induced by PA, an in vivo GPR35 agonist [6], significantly decreased DAI, colon weight, and histological score, while increasing colon length in mice with DSS-induced colitis. Furthermore, fibronectin and integrin α5 were co-localized with GPR35 on the colo
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In conclusion the present study demonstrated that peripheral
2022-10-10
In conclusion, the present study demonstrated that peripheral nerve exposure to HIV gp120 increased the expression levels of the P2Y12 receptor in DRG SGCs and enhanced mechanical and thermal hyperalgesia in rat models. Up-regulation of the P2Y12 receptor in DRG SGCs further promoted the release of
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telomerase inhibitor br Conflict of interest br CRediT autho
2022-10-10
Conflict of interest CRediT authorship contribution statement Magdalena Olga Ciechanowska: Conceptualization, Data curation, Investigation, Methodology, Project administration, Writing - original draft. Magdalena Łapot: Formal analysis, Investigation, Methodology. Marek Kowalczyk: Writing - re
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MLN 2480 sale Our experimental results demonstrated http www
2022-10-10
Our experimental results demonstrated marked variability in antioxidant defenses and oxidative damage in Crassostrea gigas between the visceral mass and the gill after the treatments by rifampicin and verapamil through determining the changes of the activity of SOD and POD and MT content. It has bee
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histone methyltransferase Resolving the molecular details of
2022-10-10
Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar
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Glucocorticoid is a major regulator of body s response to
2022-10-09
Glucocorticoid is a major regulator of body's response to stress (Armario, 2006). Repeated injections of the glucocorticoid corticosterone (CORT) in mice have been shown to produce an animal model of depression (Zhao et al., 2008). Further study of this phenomenon suggested that prolonged CORT expos
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br The interrelationship between obesity and galanin Numerou
2022-10-09
The interrelationship between obesity and galanin Numerous studies revealed that obesity and galanin may promote each other. On the one hand, galanin may increase the possibility of obesity of subjects via boosting their appetite and food intake. Acute injection with galanin or its agonist, galan
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Fatty acids are also known to
2022-10-08
Fatty acids are also known to activate G-protein coupled receptors (GPCRs). LCFAs activate the GPCRs for free fatty thrombopoietin receptor agonist (FFA)1 and FFA4 (Briscoe et al., 2003; Hirasawa et al., 2005), whereas SCFAs activate FFA2 and FFA3 receptors, which are expressed in bovine neutrophil
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Our previous study had shown that silencing FFAR expression
2022-10-08
Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β RKI-1447 [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved in the anti-li
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During the activation of the coagulation cascade
2022-10-08
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium Neurotensin synthesis on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly
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br Materials and methods br
2022-10-08
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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