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The experiments reported herein were designed
2022-04-18
The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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To characterize the basic functions of GPR
2022-04-18
To characterize the basic functions of GPR84 in phagocytes, we have utilized the receptor selective antagonist GLPG1205 (a small selective antagonist of GPR84 developed by Galapagos NV [14]) together with ZQ16 (2-(hexylthio) pyrimidine-4,6-diol), a potent GPR84 selective agonist identified in a high
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br Materials and methods br Results and discussion
2022-04-18
Materials and methods Results and discussion Conflict of interest Introduction In the presence of continuous and excessive levels of nutrients, adipocytes become hypertrophic and release several pro-inflammatory adipocytokines such as interleukin-6 (IL-6), monocyte chemoattractant protei
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Because of its excellent GPR potency good hERG
2022-04-18
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, BRD 7552 was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel of
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A high fat maternal diet during the pregestation period and
2022-04-18
A high-fat maternal diet during the pregestation period and extending throughout gestation (including the period of conception) has the propensity of affecting early embryonic development and placentation. Previous investigations have revealed that the preimplantation embryos are generally exposed t
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In order to elucidate the reasons of high efficacy
2022-04-18
In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen Altretamine of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM), while
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The general aim of our in vitro experiments was to
2022-04-18
The general aim of our in vitro experiments was to analyze the patterns of ghrelin and GHSR-1a expression in the mammary glands of dairy goats during pregnancy and to examine the direct effect of ghrelin on cell proliferation in cultured MECs of pregnant dairy goats. For this purpose, we cultured go
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More recently Dal Peraro and coworkers
2022-04-18
More recently, Dal Peraro and coworkers [38] carried out 4 μs CG MD simulations of GS with six randomly placed C9915-55 peptides embedded into a synaptic plasma bilayer model. This lipid raft model was constituted by 32 different Radicicol and cholesterol (54.74%). In this study, the authors observ
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The gene structures of cGalR and cGalR L were determined
2022-04-18
The gene structures of cGalR2 and cGalR2-L were determined by in silico comparison with the chicken genomic DNA sequences retrieved from the Ensembl database. Both cGalR2 and cGalR2-L genes are composed of two coding exons, separated by single introns of 0.9kb (cGalR2) or 3kb (cGalR2-L) locating wit
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TXNIP interacts with various proteins
2022-04-18
TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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Bufalin synthesis Introduction Osteoclasts are large multinu
2022-04-18
Introduction Osteoclasts are large, multinuclear Bufalin synthesis that are responsible for the resorption (breakdown) of bone [1]. Together with osteoblasts, the bone forming cell, they maintain the integrity of the skeleton through constant resorption and repair of bone. Osteoclast precursors of
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ISRIB Natural product based drug discovery can be
2022-04-18
Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in ISRIB binding assays, we used molecular modeling to predict how well these compounds fit t
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br Drug design Over the
2022-04-18
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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Migration chemotaxis and trafficking of leukocytes including
2022-04-16
Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial Dihydrotestosterone (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cel
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According to the experimental data HKI
2022-04-16
According to the experimental data, HKI preferentially binds to the mitochondrial inter-membrane contact sites formed by ANT and VDAC [[5], [6], [7],27], mainly via the VDAC1 isoform [7,8]. These electrogenic contact sites allow application of a part of IMP to MOM by transferring phosphoryl groups f
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