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br Results and discussion The
2022-02-08

Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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Aberrant activity of PRC as a result of
2022-02-08

Aberrant activity of PRC2 as a result of over expressed EZH2, has been frequently seen in a wide range of human cancers including breast and prostate tumors [10]. However, leukemia-associated epigenetic aberrations are not fully understood [7]. Herein, we will overview the current knowledge of epige
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Distribution of histamine receptors in the intestines varies
2022-02-08

Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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br Conclusion br Acknowledgments This research was
2022-02-08

Conclusion Acknowledgments This research was funded by Tianjin Health Institution Key Projects, grant number 15KG148” and “Tianjin Medical University General Hospital Youth Incubation Fund, grant number ZYYFY2017029”. I would like to express my heartfelt gratitude to Professor Hongtao Zhang fo
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Several classes of small molecules that
2022-02-08

Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati
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Enzyme parameters obtained for GC
2022-02-08

Enzyme parameters obtained for GC-E variants can further be introduced in kinetic models of phototransduction using computational approaches. A similar approach has been successfully applied in the investigation of disease causing mutations of GCAP1 to simulate rod and cone photoresponses under dise
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Since TgGC resisted several knockout attempts with CRISPR Ca
2022-02-08

Since TgGC resisted several knockout attempts with CRISPR-Cas9, we utilized traditional epitope tagging and an auxin-inducible degron (AID) system (Brown et al., 2017, Brown et al., 2018, Long et al., 2017) to detect and regulate TgGC expression. TgGC localizes to the apical cap region of the plasma
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br Family A Receptors as Promiscuous Sensors for
2022-02-08

Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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GPR shares a amino acid sequence identity in humans
2022-02-08

GPR81 shares a 52% amino 3463 sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capable of act
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Resolving the molecular details of glyco proteome
2022-02-07

Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar
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The main results whose proofs
2022-02-07

The main results, whose proofs depend on the explicit calculation of , include To set our work into the historical context, we note that the transporter category algebras are skew group algebras, and thus are fully group-graded algebras. This work is partially motivated by the papers on fully group
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The MeO CFO phen yl
2022-02-07

The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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br The actions of GLP
2022-02-07

The actions of GLP-1 (9–36) on the vasculature/endothelium The previous sections have ascribed the vascular and/or endothelial actions of GLP-1/GLP-1R agonists to potential direct actions through a canonical GLP-1R, but as mentioned previously, whether VSMCs and ECs express a full-length GLP-1R r
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A frequent complication of SIRS and sepsis is the developmen
2022-02-07

A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal TAK-285 [3] Moreover, it ha
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This excellent tolerability is especially interesting in the
2022-02-07

This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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