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br FXR Agonists Azepinol b indole hEC nM
2022-08-09

FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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ace inhibitor Glycine regulates several brain functions and
2022-08-09

Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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HU 308 receptor Diabetes induced damage results in periphera
2022-08-09

Diabetes-induced damage results in peripheral nerve pathology that HU 308 receptor correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studies, and perip
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MicroRNA or miRNA is group of RNA molecule of about
2022-08-09

MicroRNA, or miRNA, is group of RNA molecule of about 22 nucleotides without protein-coding function. MicroRNAs are widely distributed in plants, animals and even some viruses and participant in both normal physiological and pathological processes by post-transcriptional regulation of gene expressio
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Multiple mechanisms have been suggested by which
2022-08-09

Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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Q-VD(OMe)-OPh Neither GIP nor GIPR SNPs were associated with
2022-08-09

Neither GIP nor GIPR SNPs were associated with occurrence of fractures in the OPRA cohort (Table 4). Discussion The basis for this study lies in the role of glucose-insulinotropic peptide (GIP) hormone in the regulation of insulin secretion as well as its anabolic effect on osteoblasts and inhib
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In a previous paper we demonstrated immunohistochemically th
2022-08-09

In a previous paper, we demonstrated immunohistochemically the Wnt-C59 mg of GHSR-1a in acrosomes and peripheral region of spermatid heads as well as in acrosomes of the spermatids undergoing spermiation [19]. The present study was undertaken to demonstrate the GHSR-1a expression in rat epididymal
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Following optimization chemicals which were
2022-08-08

Following optimization, 31 chemicals, which were considered as the skin sensitizers and non-sensitizers in LLNA studies, were studied for their potential of β-galactosidase suppression (Table 2). The detailed information on test chemicals used were given in Table 1. With optimum cell densities, E. c
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Prior to proceeding to the main
2022-08-08

Prior to proceeding to the main tests, essential conditions were optimized. At first, we tested whether the parameters that were successful in inducing LacZ gene for the production of β-galactosidase enzymes in E. coli culture system in our previous study would be sufficient to induce LacZ gene in t
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br Materials and methods br Results The
2022-08-08

Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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The presence of FBP in
2022-08-08

The presence of FBP2 in nuclei seems to accompany the cells' potential to divide as it has been shown that during differentiation of the satellite cells (myogenic progenitor cells) the amount of nuclear FBP2 decreases and in differentiated myotubes, the localisation of FBP2 is restricted to cytoplas
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Our results are consistent with the hypothesis that reduced
2022-08-08

Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral 2211 synthesis as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts. A re
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The exact mechanism by which N BPs
2022-08-08

The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs
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br Acknowledgements We thank Dr Bhushan Nagar and Dr Albert
2022-08-08

Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery
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Two typical properties of Gi
2022-08-08

Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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