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The current research also analyzed the association of this
2022-04-22
The current research also analyzed the association of this polymorphism with HCV genotype 1-related hepatic steatosis by gender. Even though the allele and genotypes of this polymorphism an increased the risk of HCV-related hepatic steatosis, neither allele nor genotype frequency of this polymorphis
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To identify structurally novel autophagy inhibitors a medium
2022-04-22
To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 ic losartan potassium stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected
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Moreover we have demonstrated that internalization and
2022-04-22
Moreover, we have demonstrated that internalization and subcellular trafficking of NPRA, using IF staining (IFS) and co-IP of plasma membrane, endosomal, lysosomal, and recycling endosome markers to follow intracellular trafficking and signaling by confocal IF microscopy (CIF) and immunoblotting (IB
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Interestingly myorelaxation and the stimulation of cGMP
2022-04-22
Interestingly, myorelaxation and the stimulation of cGMP production are properties also reported for sGC stimulators, such as YC-1 and BAY 41–2272 (i.e., indazole compounds that were discovered in the 1990s) [35]. They relax aortic ring contractions induced by phenylephrine, and their effects are si
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Glutathione transferases GST have been discovered in
2022-04-22
Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To d
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Glycogen synthase kinase GSK a serine threonine kinase has b
2022-04-22
Glycogen synthase kinase-3 (GSK-3), a serine/threonine kinase, has been confirmed to be involved in some biological processes in NaCl or wound-treated plants (Chen et al., 2003, Hai et al., 2001, Jonak et al., 2000). NO has been recently recognized as a vital signaling compound in plants. The NO don
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Screening of the compounds allowed for a number
2022-04-22
Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detr
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Starting from commercially available dioxaspiro decan ol was
2022-04-22
Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an cyclin dependent kinase catalyzed deprotection efficiently gave . A - enriched mixture of (
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G protein coupled receptor GPCR ligands can be classified as
2022-04-22
G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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GnRH receptor GnRH R levels are elevated in decidualized
2022-04-22
GnRH receptor (GnRH-R) levels are elevated in decidualized stromal cells, suggesting a function for the GnRH–GnRH-R pathway in the early implantation events. Both GnRH and GnRH-R have been shown to be present in preimplantation embryos and the fallopian tubes at both mRNA and protein levels (). Two
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Active compounds and were further tested and EC
2022-04-22
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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br Methods br Results br Discussion Significant alterations
2022-04-22
Methods Results Discussion Significant alterations in the expression of genes related to the glutamatergic system have been shown in several experimental models of epilepsy; however, in most studies focused on acute changes or modifications in expression, these were investigated during the
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Animal studies have shown that various antidepressant treatm
2022-04-21
Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key KN-93 regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate the negative feedba
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The focused set of cyclopentapyrazoles
2022-04-21
The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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The focused set of additional pyrazole analogs allowed the
2022-04-21
The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro
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