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Recently a lot of synthetic FFA agonists containing
2022-01-06
Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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These observations are of particular interest in
2022-01-06
These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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A great number of proteins entering the nucleus
2022-01-06
A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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Before discovery of their histone demethylase function the J
2022-01-06
Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tail
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The overall response rate to afatinib is comparable
2022-01-06
The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an
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br Manganese based imaging probes br Imaging of vesicular mo
2022-01-05
Manganese-based imaging probes Imaging of vesicular monoamine transporter 2 (VMAT2) Imaging of sulfonylurea receptor 1 (SUR1) In mammals, insulin secretion is mediated by the membrane potential of pancreatic β-cells. Increases in glucose levels lead to blocking of ATP-sensitive potassium ch
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br Acknowledgements This work was financed by the projects
2022-01-05
Acknowledgements This work was financed by the projects “Mejora Genética del Almendro” (MINECO-Spain, AGL2017-85042-R), “The molecular mechanisms to break flower bud dormancy in fruit trees” to RS-P within the Villum Young Investigator Program and by the VILLUM Research Center for Plant Plasticit
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For another the N terminal
2022-01-05
For another, the N-terminal sequence of native glucagon is highly conserved, and positions 8, 9, 16 and 18 are noteworthy in maintaining glucagon activity [18], [20], [21]. It also achieves a degree of selectivity from its C-terminal residues, and a significant contribution is made by the C-terminal
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In order to test whether the
2022-01-05
In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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Considering the conformational preferences of the SRSRY sequ
2022-01-05
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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The ability to metastasize is the defining character of a
2022-01-05
The ability to metastasize is the defining character of a cancer and the leading cause for resultant mortality. It is hypothesized that a rare subset of cancer cells, often operationally referred to as “cancer stem cells” (CSCs), are responsible for sustaining cancer metastasis and recurrence [1]. T
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In conclusion we have shown that the
2022-01-05
In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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EPZ-6438 Another property shared between Hat p
2022-01-05
Another property shared between Hat1p and Rtt109p is a transient or substoichiometric interaction with Asf1p. Asf1p is necessary for the acetylation of histone H3 lysine 56 by Rtt109p. However, they do not appear to form a stable complex [22], [24], [27], [84], [90]. Surprisingly, the original type
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Finally we investigated increasing basicity as a way to impr
2022-01-04
Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, Biotin-16-dCTP demonstrated significant improvement of values of solubility for the two media, especia
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K-7174 australia FPG had no consistent activity in reducing
2022-01-04
FPG-2 had no consistent activity in reducing G→T transversions. Gao and Murphy [2] earlier reported that FPG-2 had a limited amount of activity in vitro on depurinated, UV-treated, and methylene-blue-treated DNA (but not on 8-oxo-G-containing oligonucleotides). FPG-2 contains the N-terminal domain a
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