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With the nitrogen containing heterocycle components and the
2022-03-30
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic Chloramphenicol (, and ), followed by deprotection by TFA, smoothly provided
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br Acknowledgments We apologize to the researchers who
2022-03-30
Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Dave Primm (Department of Surgery, University of Texas Southwestern Medical Center) for his critical reading of the manuscript. This work was supported by grants from the US National Institu
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By measuring the accumulation of unprenylated Rap
2022-03-30
By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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The above mentioned studies are
2022-03-30
The above-mentioned studies are especially important since the structural alterations of the peritoneum during peritoneal dialysis are very similar to vascular and tissue alteration seen in diabetes. The tissue alterations during long-term peritoneal dialysis include a thickening and replication of
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br Discussion The aim of the present study
2022-03-30
Discussion The aim of the present study was to extend the list of ASIC ligands and to check if histamine receptors ligands can also affect ASICs. The novel finding is that not only histamine but also thioperamide, 1-metylhistamine and Nα-methylhistamine are active ASIC1a potentiators, while other
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br STAR Methods br Acknowledgments We thank P
2022-03-30
STAR★Methods Acknowledgments We thank P. Adler, V. Riechmann, N. Tapon, E. Knust, the Vienna Drosophila RNAi Center, the Australian Drosophila Research Support Facility (www.ozdros.com), the Bloomington Drosophila Stock Center, and the Developmental Studies Hybridoma Bank for D. melanogaster s
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br Introduction The signaling molecule
2022-03-30
Introduction The signaling molecule nitric oxide (NO) plays an essential role in vessel homeostasis by initiating vasodilation [1], [2], [3]. After biosynthesis in endothelial cells, NO diffuses into the subjacent smooth muscle layer to reach its target enzyme, soluble guanylyl cyclase (sGC, EC 4
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Having identified initial leads and further lead optimizatio
2022-03-29
Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Refametinib derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chl
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(S)-Methylisothiourea sulfate br Conclusions Beta cell speci
2022-03-29
Conclusions Beta cell-specific expression in human islets of DGCR2, GBF1, GPR44 and SerpinB10 has not previously been described, although the proteins have partly been characterized in other contexts not related to beta (S)-Methylisothiourea sulfate or diabetes. DGCR2, GPR44 and SerpinB10 were n
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br Conclusion The wild study reports seasonal
2022-03-29
Conclusion The wild study reports seasonal variations in reproductive physiology, behavior and tachykinin plasticity at different age stages in wild-caught Mongolian gerbils. The gerbils in breeding seasons have more mature sexual development, higher exploratory behavior, higher novelty preferen
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br Reaction mechanism The dissimilarity between monofunction
2022-03-29
Reaction mechanism The dissimilarity between monofunctional and bifunctional glycosylases is that the monofunctional glycosylases removes the substrate base, leaving an intact AP site while the bifunctional glycosylases have an additional lyase activity. This intrinsic lyase activity is present i
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In insects structural cuticular proteins CPs
2022-03-29
In insects, structural cuticular proteins (CPs) play important roles in determining the diverse physical properties of the cuticle, depending on developmental stages, as well as different body regions, as a result of interactions with other CPs and the structural biopolymer chitin [4]. Many studies
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Molecular dynamics studies have proved
2022-03-29
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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br Materials animals and methods br Results
2022-03-29
Materials, animals and methods Results Discussion This study presents mice with a missense point mutation in R258 of FFAR1 that has functional consequences. Firstly, in islets of Ffar1R258W/R258W mice, both the physiological agonist palmitate and the synthetic agonist TUG-469 were unable to
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Introduction Glucose is the most important energy carrier
2022-03-29
Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula
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