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In the present study we tested
2021-11-15

In the present study, we tested α-glucosidase and tyrosinase inhibitory effects of the methanol extract from lower stems and Granzyme B Inhibitor Z-AAD-CH2Cl of Q. coccifera (1) as well as the isolated compounds [lyoniresinol-9-O-β-xylopyranoside (2) and lyoniresinol-9-O-β-glucopyranoside (3), cocc
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Genomic studies have afforded new insight into the influence
2021-11-15

Genomic studies have afforded new insight into the influence of ARQ 621 structure on GR binding. An important clue came from genome-wide mapping of chromatin structure using DNase I hypersensitive site sequencing (DNase-seq), and comparing the locations of open chromatin to GBSs [10]. DNase-seq in
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Somatostatin analogues are among the first peptide based dru
2021-11-15

Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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Neuregulin/Heregulin-1β (NRG-1β/HRG-1β), human recombinant p
2021-11-15

The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) Neuregulin/Heregulin-1β (NRG-1β/HRG-1β), human recombinant protein synthesis (also known as the SeHCAT retention test). SeHCAT test involves the use of a syntheti
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Preliminary explorations focused on the linker of Table Lill
2021-11-15

Preliminary explorations focused on the linker of 2 (Table 1). Lilly reported that the methylene between the phenyl and the piperidyl group was metabolically susceptible to N-dealkylation, so we replaced the methylene with a carbonyl moiety to block the metabolic site [23,48] (Fig. 2). In addition,
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Similar to in vitro data in vivo studies
2021-11-15

Similar to in vitro data, in vivo studies have also revealed modulation of TLR4-induced inflammatory responses by AEA. The proposed AEA reuptake inhibitor AM404 has been shown to attenuate TLR4-induced increases in plasma levels of IL-6 and IL-1β, the latter effect mediated by CB1 receptor activatio
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Distribution of histamine receptors in the intestines varies
2021-11-15

Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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In recent years the Hippo signaling pathway has
2021-11-15

In recent years, the Hippo signaling pathway has emerged as an important regulator balancing cell proliferation and differentiation [[5], [6], [7]]. The pathway components, first described in the fruit fly Drosophila melanogaster, are highly conserved across different phyla [6]. The signaling pathwa
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Several studies have also shown that HK may be an
2021-11-15

Several studies have also shown that HK2 may be an important downstream SMIP004 of the PI3K/AKT/mTOR signaling pathway and may contribute to the development of cancer [15]. In our previous study, we found AKT2 expression was positively correlated with HK2 expression in primary colon cancer specimens
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While the binding of HK to VDAC
2021-11-15

While the binding of HK1 to VDAC1 is strong and continuous, the binding of HK2 to VDAC1 is much weaker, and alternates between a cytoplasmic and a mitochondrial-bound states (John et al., 2011). This dynamic process is regulated by the metabolic and energetic requirements of the fda approved and pro
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GW9662 receptor TRAPP Transport Protein Particle complexes s
2021-11-15

TRAPP (Transport Protein Particle) complexes share a common core architecture and function in GW9662 receptor and autophagy (Kim et al., 2016). In yeast, the core complex has GEF activity for the Rab1 ortholog Ypt1. The larger TRAPPII and III complexes include regulatory subunits implicated in memb
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Barthi et al previously showed that curcumin inhibits
2021-11-15

Barthi et al.[43] previously showed that curcumin inhibits IKK complex activity and thus IκBα phosphorylation as well as the p65 nuclear translocation. Those data are in agreement with our results obtained by gel shift assays using GSTP1-1 promoter and consensus NF-κB probes. Moreover, luciferase ac
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br Lysophosphatidylinositol LPI LPI is
2021-11-12

Lysophosphatidylinositol (LPI) LPI is a subspecies of lysophospholipid consisting of inositol as its head group, one glycerol molecule and one acyl chain (Piñeiro and Falasca, 2012). The biosynthesis of this lipid starts from Phosphatidylinositol (PI) and is catalysed by the enzymes phospholipase
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Human GPR hGPR was originally isolated in as an
2021-11-12

Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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In this study we describe the
2021-11-12

In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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