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An interesting question is why RhoF has such
2021-12-08
An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino Chlorocresol receptor mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF
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After establishing improved GSNOR potency some of the
2021-12-08
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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Previously we reported that the
2021-12-08
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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Introduction Gestational diabetes mellitus GDM is
2021-12-08
Introduction Gestational diabetes mellitus (GDM) is one of the most common complications associated with pregnancy [1]. Approximately 7.6% of pregnancies in the United States are complicated by GDM [2,3], which significantly increases the mother's risk of developing type 2 diabetes (T2D) later in l
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br Genetic manipulation variation of the
2021-12-08
Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors
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We are aware that the
2021-12-08
We are aware that the classical biochemical view is centered on the local concentrations of specific ion and molecules rather than on cell electric potentials. However, important downstream processes can be influenced by acting locally on these potentials because they regulate the conductance of the
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DS2 synthesis br BA induced activation of
2021-12-08
BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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br ACKNOWLEDGMENTS br Introduction Odorant receptors ORs are
2021-12-08
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 ACKNOWLEDGMENTS br Introduction Odorant receptors ORs are
2021-12-08
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 a
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Trifluoromethyl ketones and fluorophosphates were
2021-12-08
Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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Chicoric acid CA is a di acylated hydroxycinnamoyl tartaric
2021-12-07
Chicoric Ivabradine HCl (CA) is a di-acylated hydroxycinnamoyl tartaric acid ester [12] found in a variety of plant species, especially within the Astereceae family [13]. Of interest for this study, Sonchus oleraceus and Bidens pilosa plants, from Astereceae family, were used. Both S. oleraceus and
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br Introduction Histamine stored in mast cells and
2021-12-07
Introduction Histamine stored in mast cells and basophils has been recognized as one of the most critical mediators in allergic reactions and plays an important role in eliciting the nasal symptoms of allergic rhinitis, such as sneezing, nasal itch, pain, rhinorrhea, and congestion [1], [2]. It i
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10537 The finding of histamine action on ASICs also raises
2021-12-07
The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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br Histamine and glycaemia Histamine is involved in a wide
2021-12-07
Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of PF-573228 and diabetes date back to the 1950s. Since that time the involvement of histamine in diab
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HER genotype was determined in breast cancer tissue of
2021-12-07
HER2 genotype was determined in breast cancer tissue of 73 breast cancer patients. As previously reported, Ile655Val and Ala1170Pro genotypes measured in breast cancer tissues were available for 71 and 69 breast cancer patients, respectively. Briefly, 77.5% (55/71) of patients were homozygous for th
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