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We also explored various nitrogen substituents
2021-12-10
We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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MRS 1220 br Materials and methods br Results In this
2021-12-10
Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V
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br Investigations br Genetics GLUT is a membrane bound glyco
2021-12-10
Investigations Genetics GLUT1 is a membrane-bound glycoprotein that provides base-rate glucose transport across blood-tissue barriers. It is constituitively expressed in erythrocytes, SR 49059 mg microvessels and astroglia. The gene exclusively associated with GLUT1 is SLC2A1, located on chro
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Compound was obtained as a
2021-12-10
Compound was obtained as a yellow crystal (acetone). And the molecular formula of was established as CHO on the basis of a quasi-molecular ion at / 331.0799 [M+H] (calcd. for 331.0818) in its HR-ESI-MS. Compound showed H and C NMR similar to those of carbachol . However, The H NMR spectrum of c
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Sequences of hexokinases were initially deduced
2021-12-10
Sequences of hexokinases were initially deduced and predicted based on cDNA clones (Andreone et al., 1989, Schwab and Wilson, 1989, Schwab and Wilson, 1991, Griffin et al., 1991, Thelen and Wilson, 1991). Analysis of genome sequence data identified, in Ellipticine to the 4 expected known hexokinase
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In the present study we set out to
2021-12-10
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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br Acknowledgments This work was supported by the
2021-12-10
Acknowledgments This work was supported by the NIH (R01DK103884 to JMZ, R01DK100659 to JKE, and F32DK104659 and K01DK111644 to CMC), the Diana and Richard C. Strauss Professorship in Biomedical Research, the Mr. and Mrs. Bruce G. Brookshire Professorship in Medicine, the Kent and Jodi Foster Dist
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The main consequence of glucose catabolism
2021-12-10
The main consequence of glucose catabolism is the elevation of ATP concentration, which in turn suppresses the ATP sensitive potassium (KATP) channels gating function. The KATP channels are octamers composed of the tetrameric inward-rectifying potassium channels (with Kir6.1 and Kir6.2 subunits), th
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Accumulating evidence suggests that the NGF
2021-12-10
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, melanocortin receptor derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDN
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With LML methyl oxo dihydropyridazin yl
2021-12-10
With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perfor
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A recent novel and important finding is that YAP connects
2021-12-10
A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1
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Spironolactone receptor In human platelets only and isoforms
2021-12-09
In human platelets, only α1 and β1 isoforms of sGC are expressed in equimolar concentrations (3700 copies for β1, and 3500 copies for α1 per platelet) [57] [62]. sGC, is usually a heterodimer and contains heme as cofactor which is required for high-affinity NO binding and stimulation of its activity
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CFTRinh-172 br Introduction The Ras superfamily
2021-12-09
Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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Methylprednisolone Sodium Succinate br Acknowledgments This
2021-12-09
Acknowledgments This publication was supported by NORAD (Norwegian Agency for Development Cooperation) under the NORHED-Program, agreement no. ETH-13/0024. MCM works at the MRC Integrative Epidemiology Unit which receives infrastructure funding from the UK Medical Research Council (MRC) (MC_UU_12
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In this study we also profiled
2021-12-09
In this study, we also profiled the expression of the transporters in wild-type RBL-2H3 cells, RBL-2H3 Sc98 cells, and rat peritoneal mast cells. OCT1 and PMAT were expressed at high levels in both RBL-2H3 Sc98 and RBL-2H3 cells. However, OCT2 and OCT3 were weakly or least detected in RBL-2H3 Sc98 c
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