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A general synthetic pathway to these tricyclic
2022-08-19
A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methyl
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br Acknowledgments This publication was supported
2022-08-19
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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ARQ 197 receptor Selection of the month br Fibrosis
2022-08-19
Selection of the month Fibrosis Liver protection device Non-alcoholic steatohepatitis Genetic metabolic liver disease Hepatitis C virus (HCV) infection Hepatitis B virus (HBV) infection Cirrhosis Regeneration Introduction Upon catalysis by hepatic and bacterial enzymes, c
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To this end we evaluated novel D analogs for selectivity
2022-08-18
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell BCATc Inhibitor 2 receptor systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (
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enzastaurin The discovery that GLUT in the microvasculature
2022-08-18
The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting enzastaurin function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an important link to the unfavora
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calcifediol The primary requirements of an ideal bioprobe fo
2022-08-18
The primary requirements of an ideal bioprobe for glucose transporter-mediated bioimaging include high specificity, sensitivity as well as low cytotoxicity [18]. According to these concepts, we recently reported the simple amide linked glycoconjugates which containing cyanine fluorophores (Cy3 and C
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Nuclear export of GK has been reported to
2022-08-18
Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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Introduction Human pathogenic Leishmania protozoa comprise
2022-08-18
Introduction Human pathogenic Leishmania protozoa comprise 20 different species that are distributed throughout the world and cause the disease leishmaniasis [1]. Transmission primarily occurs through the bite of a female sand fly and clinical manifestations of the disease span from cutaneous lesio
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Two pathways have emerged to explain
2022-08-18
Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an
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GHSR A s have high
2022-08-18
GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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More polar substituents introduced on the position of the
2022-08-18
More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m
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We hypothesize that HBO increases GABA activity at the GABAA
2022-08-18
We hypothesize that HBO2 increases GABA activity at the GABAA receptor via a nitric oxide dependent mechanism. Blotting for the phosphorylated β3 subunit of the GABAA receptor should theoretically be increased when there is more GABA activity at the receptor (McDonald et al., 1998). We expected that
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br Experimental br Results and discussions br Conclusion br
2022-08-18
Experimental Results and discussions Conclusion Notes Introduction The noncanonical DNA structures that is, i-motif [[1], [2], [3], [4], [5], [6], [7], [8], [9]] and G-quadruplex [[10], [11], [12], [13], [14]] have recently been carefully studied using either experimental or computati
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There are many kinds of neurological disorders
2022-08-18
There are many kinds of neurological disorders and neuropsychiatric diseases, like stroke, dementia, schizophrenia and so on. Among these disorders, the most important reason for choosing depression in our study is that FXR has already been demonstrated to regulate the function of CREB, which is cl
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Initially the synthesized compounds from were evaluated
2022-08-17
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic Tivozanib mg having similar t
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