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br FREE FATTY ACID RECEPTOR
2022-03-10
FREE FATTY ACID RECEPTOR 1 (GPR40) G-PROTEIN-COUPLED RECEPTOR 120 CONCLUSION Free fatty Imeglimin hydrochloride receptors whose natural ligands are identified as FFAs having various lengths have been reported. They act as novel nutrient sensing receptors independent of PPARs and FABPs, and
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An azabicyclic compound named S a
2022-03-10
An azabicyclic paricalcitol synthesis named S 38093, (4-[3-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)propoxy]benzamide), was introduced by Servier with H3R antagonist and inverse agonist activity (Sors et al., 2017). The compound contains all the drug-likeness criteria owing to its physi
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Anti apoptotic Bcl proteins have become attractive targets f
2022-03-10
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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Ikaros utilizes chromatin remodeling to activate or repress
2022-03-10
Ikaros utilizes amg 232 remodeling to activate or repress the transcription of its target genes (Su et al., 2004). Ikaros directly associates with histone deacetylases HDAC1 and HDAC2 and can recruit them to the upstream regulatory elements of its target genes (Kim et al., 1999, Koipally et al., 19
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Selection of the month br Fibrosis br Liver protection
2022-03-09
Selection of the month Fibrosis Liver protection device Non-alcoholic steatohepatitis Genetic metabolic liver disease Hepatitis C virus (HCV) infection Hepatitis B virus (HBV) infection Cirrhosis Regeneration Introduction Upon catalysis by hepatic and bacterial enzymes, c
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As preclinical toxicity and efficacy
2022-03-09
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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br Materials and methods br Results and
2022-03-09
Materials and methods Results and discussion We recently found that the GlyT1 N-terminal and C-terminal sequences could be modified by phophorylation, or partially lost under pathological conditions by calcium-dependent proteolysis (Baliova and Jursky, 2005, Baliova and Jursky, 2010). While re
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The neurobiological mechanisms underlying DHK induced NOR le
2022-03-09
The neurobiological mechanisms underlying DHK-induced NOR learning and memory impairments remain unclear. Accumulated evidence shows that astrocyte-neuron lactate shuttle is of crucial important in synaptic plasticity and memory formation, and regulation of neuronal gene expression related to synapt
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The transport of glutamate by EAAT
2022-03-09
The transport of glutamate by EAAT2 from the extracellular fluid into either astrocytes or endothelial cells is an unfavorable and energy-consuming process. This energy is provided by a coupled co-transport of three sodium ions, one proton, and one glutamate molecule in the counter-transport of one
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Tight junctions regulate the transfer of
2022-03-09
Tight junctions regulate the transfer of ions as well as small molecules across endothelial barriers (Li et al., 2015). We also investigated whether resistin affects tight junctions, which play an important role in the conformation of polarized endothelial barriers (Matsuzaki et al., 2010). A previo
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Cx is a phosphoprotein that is predominantly phosphorylated
2022-03-09
Cx43 is a phosphoprotein that is predominantly phosphorylated in the control state. Cx43 can be phosphorylated by a number of kinases and dephosphorylated by protein phosphatases such as PP1 and PP2A [6], [10]. Posttranslational phosphorylation of Cx43 is thought to influence intercellular coupling
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In this study we describe the expression
2022-03-09
In this study, we describe the expression of galr2a and galr2b in zebrafish embryos using whole-mount in situ RNA hybridization. To further analyze the distribution of GALR2b and its interactions with galanin, we generated Tg(galr2b:egfp) zebrafish, which express EGFP under the control of a galr2b p
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Nano biocatalyst prepared by assembling an
2022-03-09
Nano-biocatalyst, prepared by assembling an enzyme on nanomaterial (NM) carriers is an emerging innovation in the field of nanobiotechnology. Some of the advantages of using NM as supports in PU-H71 synthesis to conventional porous supports are effective enzyme loading due to large surface area wit
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br ACKNOWLEDGMENTS br Introduction Odorant
2022-03-09
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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entacapone After the successful development of molecular tar
2022-03-09
After the successful development of molecular targeted drugs in lung adenocarcinoma, substantial efforts have been made to provide similar targeted drugs in lung squamous-cell carcinoma. Because FGFR gene alteration is the most frequent occurrence in squamous-cell carcinoma, targeted therapies for F
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