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Since our new compound Fex could be a new FXR
2022-04-01

Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 Retigabine dihydrochloride with transwell experiment
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Studies on FXR knockout mice demonstrated
2022-04-01

Studies on FXR knockout mice demonstrated that FXR activity is necessary to maintain a proper integrity of intestinal tight junction [18]. HF diet-induced bowel dysfunction impaired FXR activity and affected fecal BA profile. Generally, it augmented the concentration of secondary BAs in the colon e.
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The current study identified the presence and
2022-03-31

The current study identified the presence and location of all four histamine receptors in the GI tract of 6 healthy adult dogs. Although no clinical signs of GI disease were noted, mild inflammation was noted in at least one section of the GI tract in all dogs based on WSAVA guidelines. Interpretati
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br Trifluoromethylketones This group of
2022-03-31

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc sphingosine in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif
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The replacement of the P butyl urea
2022-03-31

The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P
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Human immunodeficiency virus type HIV is responsible for the
2022-03-31

Human immunodeficiency virus type 1 (HIV-1) is responsible for the propionitrile pandemic; notification is compulsory in Brazilian blood banks since 1988. From 1980 to 2016, the Brazilian MH reported 882,810 HIV/AIDS cases, with 52.3% in the southeast region. HIV/HCV co-infection has been associate
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NPxY was recognized as the
2022-03-31

NPxY was recognized as the first short signal sequence motif in the cytoplasmic domain of membrane receptors and proteins with critical roles in internalization and trafficking of receptor molecules [130]. Including LDL receptor, beta-1 integrin, megalin, beta-amyloid precursor protein, EGF receptor
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The identity of organelles is defined by a
2022-03-31

The identity of organelles is defined by a particular set of molecules present on their surface. Most organelles in the endomembrane system (i.e., endoplasmic reticulum, Golgi apparatus, endosomes, and lysosomes) carry Rab GTPases (hereafter referred to as Rabs), which serve as binding platforms for
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The mode of action of m Tyr has
2022-03-31

The mode of action of m-Tyr has not been fully recognized. The primary/basic mechanism of action of m-Tyr is thought to be associated with the incorporation of this NPAA into the structure of proteins resulting in formation of dysfunctional proteins [11], [12]. m-Tyr is incorporated into proteins in
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Several studies have sought a cross relationship between com
2022-03-31

Several studies have sought a cross-relationship between commensal bacteria-derived metabolites and the Gprs (Blad et al., 2012). Gpr81 is expressed primarily in adipocytes, and hence, lactate-Gpr81 interaction inhibits lipolysis (Cai et al., 2008, Liu et al., 2009). Lactate reduced inflammation by
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br Introduction Atherothrombosis is associated with the pres
2022-03-31

Introduction Atherothrombosis is associated with the presence of a low-grade, subclinical smoldering inflammatory response [1]. Several inflammatory markers, among them high-sensitive C-reactive protein (hs-CRP) [2], the erythrocyte sedimentation rate (ESR) [3], fibrinogen concentrations [4], int
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Through the analysis of various
2022-03-31

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic rapamycin buy motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering
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br Genetic rescue of GluR A dependent spatial working memory
2022-03-31

Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific cdk7 of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schmitt et al., 2005). This ge
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5-Methoxy-UTP br Materials and methods br Results br
2022-03-30

Materials and methods Results Discussion Importantly, we observed that treatment with DA3-CH could reduce the pathophysiological processes in the hippocampal CA1 area after SE. At present, the unimolecular dual incretin receptor agonist has been developed as a treatment for type 2 diabetes,
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Newt GHS R a proteins expressed
2022-03-30

Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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