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br Characterization of quantal exocytosis by
2021-12-13

Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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GSK has also been used as PET radiotracer in
2021-12-10

GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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The primary physiological role of the HO system is the
2021-12-10

The primary physiological role of the HO system is the protection of valdecoxib from oxidative stress. These cytoprotective effects are attributable both to the degradation of the pro-oxidant heme and to the positive contribution of the metabolites produced during this degradation, namely CO, BV, a
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To the best of our knowledge this
2021-12-10

To the best of our knowledge, this is the first study to examine functional GSTO1‐1 activity in the cornea. Therefore, comparative data for human or animals is not available. Moreover, we observed the nonspecific degradation of the GSTO1‐1 substrate 4NPG via an unknown mechanism, which was corrected
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Niacin nicotinic acid is widely used
2021-12-10

Niacin (nicotinic acid) is widely used to regulate abnormalities in plasma lipid and lipoprotein metabolism, as evidenced by its potential for reducing atherosclerotic cardiovascular disease risks (Guyton, 1998), due to its ability to reduce circulating triglycerides and apolipoprotein-B containing
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To maintain low Glu concentrations in the synaptic
2021-12-10

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino 69 9 receptor is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, an
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EAATs can transport glutamate aspartate
2021-12-10

EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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br Introduction Anthocyanidins and anthocyanins glycosides o
2021-12-10

Introduction Anthocyanidins and anthocyanins (glycosides of anthocyanidins) are flavonoid phenolic compounds that are among the most common types of plant pigments [1]. They typically are responsible for the red, orange, blue, and violet colors in flowers, fruits, and vegetative tissues [1], [2].
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br Materials and methods br Results br Discussion Several
2021-12-10

Materials and methods Results Discussion Several peripheral hormones that are involved in the central regulation of energy homeostasis, such as leptin, insulin, and amylin [34], [35], [36], [37], [38], cross the BBB by saturable and unsaturable mechanisms. Whether these transport processes
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Acknowledgments This work was supported
2021-12-10

Acknowledgments This work was supported by the Natural Science Foundation of China (Nos. 21602254, 81603194), the Natural Science Foundation of Jiangsu province, China (BK20160767) and National Found for Fostering Talents of Basic Science (NFFTBS, J1310032). Introduction Glucocorticoids (GC) pl
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More recently Serna Marquez and colleagues investigated LA i
2021-12-10

More recently, Serna-Marquez and colleagues investigated LA-induced migration and invasion of MDA-MB-231 breast cancer cells. In this study, LA was shown to induce AKT-2 phosphorylation and cell invasion and migration in MDA cells. LA-induced cell migration was inhibited by siRNA that selectively ta
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This review is an overview on the
2021-12-10

This review is an overview on the ongoing trials involving anti-FGF-FGFR therapies (Wu et al., 2013). Pathway FGFR in cancer A recent study comparing more than 4800 tumor tissue samples has shown that 7.1% of all tumor types have genetic alterations in the FGF-FGFR axis. The aberrations perce
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multidrug resistant In the previous paper we
2021-12-10

In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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br Acknowledgement This research was supported
2021-12-10

Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral NVP-BKM120 Hydrochloride is the most popular administration route due to goo
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SCH is a H R receptor antagonist introduced by
2021-12-10

SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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