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Neurotransmitter transporters are rapidly recycled from and
2021-10-16
Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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In experiments using D to displace binding of specific
2021-10-16
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse PG 01037 dihydrochloride tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fi
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br Experimental br Acknowledgments This
2021-10-16
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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To date types of glucose
2021-10-15
To date, 14 types of glucose transport protein have been discovered, each having its own specific functions with different distributions [33]. Among these, GLUT4 is particularly important for maintaining glucose metabolism homeostasis and insulin sensitivity, since it is involved in glucose transpor
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br Experimental br Results and discussion br
2021-10-15
Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f
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Over recent decades there were three
2021-10-15
Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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KNK437 br Materials and methods br
2021-10-15
Materials and methods Results We examined the cardiac mitochondrial density of HKI and markers of oxidative and metabolic stress in trout exposed to an aerated control exposure, an aerated (normoxic) thermal insult, or a hyperoxic thermal insult. Should mtHK provide a cardioprotective effect i
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br The hedgehog signalling pathway The
2021-10-15
The hedgehog signalling pathway The canonical Hh pathway is a conserved, highly complex signalling cascade, with many players and intricate regulation. However, it can be simplified into four fundamental components: i) the ligand Hh, ii) the receptor Patched (Patch [PTCH1]), iii) the signal trans
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br AURK Functions br Concluding
2021-10-15
AURK Functions Concluding Remarks The AURKs are crucial regulators of cell division; however, little is known about the mechanisms by which these kinases function in meiosis. Recent work has begun to chip away at the specific roles that each of the kinases play; however, as more is uncovered,
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The imidazopyridines and related imidazopyrimidines
2021-10-15
The imidazopyridines and related imidazopyrimidines – and – were constructed from the key amine intermediates – ( X=CH and Ar=2-FPh, X=N and Ar=2-FPh, X=CH and Ar=5-pyrimidine, X=CH and Ar=2-methyl-5-pyrimidine, and X=CF and Ar=2-methyl-5-pyrimidine). These were synthesized a modified Horner–Em
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GSTs have been originally named ligandins because of their
2021-10-15
GSTs have been originally named ‘ligandins’ because of their capacity to bind large ligand molecules (of molecular weight >400 Da) (Oakley et al., 1999). At least three separate 535 2 have been reported for xenobiotics within the H-site; only one is for CDNB (Ralat and Colman, 2004). Usually, the n
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We also explored various nitrogen
2021-10-15
We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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The synthesis of is shown
2021-10-15
The synthesis of is shown in . The ---Boc--diaminopropanoic acid--butyl ester () fragment was synthesized in four steps from Boc--asparagine (). The key step in this synthesis was a Hofmann rearrangement of the terminal carboxamide, which was performed according to the elegant protocol of Zhang tha
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Excessive extracellular glutamate may induce
2021-10-15
Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much
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CAY10499 Several studies have indicated MUC to be
2021-10-15
Several studies have indicated MUC1 to be an effective marker for identifying various malignant tumors, such as gastric, breast, pancreatic, ovarian, gallbladder, uterus, lung, and prostate cancers, as well as for prognostic outcomes [16], [17], [18], [19], [20], [21], [22], [23]. Studies by Kaira e
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