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On the basis of their relative
2022-06-23
On the basis of their relative Glu transport rates and anion currents, EAATs group into two functionally distinct classes, EAAT1–3 being efficient Glu transporters with small associated macroscopic anion currents and EAAT4–5 low-capacity transporters with predominant anion conductance [18]. The diff
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In vitro studies have shown that some antidepressant
2022-06-23
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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am 580 br Acknowledgements br Introduction Benzodiazepine BZ
2022-06-23
Acknowledgements Introduction Benzodiazepine (BZ) treatment is widely used for quick and efficient anxiolytic and sedative responses. However, when the use is extended to longer periods, adverse effects emerge. These include tolerance to the initial drug effect, dependence as revealed by withd
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The molecular identity of RA s target during LTP
2022-06-23
The molecular identity of RA’s target during LTP induction was determined by pharmacological testing. The inhibitory effects of CNQX and niflumic acid on LTP induction remained even in the presence of RA, indicating RA did not affect either the AMPA receptor nor chloride channel (Fig. 2B and D) [26]
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Acarbose and voglibose the classic glucosidase inhibitors we
2022-06-23
Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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A localization of GK to both a cytoplasmic and
2022-06-23
A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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br Conflict of interest statement br Acknowledgements This w
2022-06-23
Conflict of interest statement Acknowledgements This work was supported by the National Health and Medical Research Council of Australia (NHMRC) (project grants [1061044], [1065410] and [1126857], and NHMRC program grant [1055134]); P.M.S. and A.C. are NHMRC Principal and Senior Principal Rese
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The eradication of agonist activity
2022-06-22
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary protease inhibitor cocktail as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could
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The structural similarity software vROCS OpenEye has been ut
2022-06-22
The structural similarity software vROCS (OpenEye) [45] has been utilized by Musumeci et al. [46] to screen the Maybridge [47] HitFinder database (∼14,400 compounds) using Distamycin A (Fig. 3B) as a query. Using the Tanimoto coefficient (Section 6.4) and vROCS's colour scoring (atom/feature similar
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Enhancer of Zeste Homolog EZH is
2022-06-22
Enhancer of Zeste Homolog 2 (EZH2) is a core component of the Polycomb Repressive Complex2 (PRC2) which also includes SUZ12 and EED. PRC2 represses gene transcription through trimethylation of Lys27 of histone H3 (H3K27), and contribute to the maintenance of cell identity, AMD-070 hydrochloride reg
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br Introduction br The histaminergic system in the central n
2022-06-22
Introduction The histaminergic system in the central nervous system The oxytocin antagonist is continually processing information through aminergic systems present in the mammalian CNS such as the serotonergic, dopaminergic, noradrenergic and histaminergic systems which function by projecting
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KX2-391 dihydrochloride Recently the toxicity of TBT was dem
2022-06-22
Recently, the toxicity of TBT was demonstrated at the vascular level in animal models (Nath, 2008), and the results obtained so far suggest that TBT may be a potential risk factor for cardiovascular diseases. TBT is capable to alter the coronary vascular reactivity to estradiol (dos Santos et al.,
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br STAR Methods br Acknowledgments We thank
2022-06-22
STAR★Methods Acknowledgments We thank the TCGA PanCanAtlas Analysis Working Group. This study was supported in part by grants from the NIH (CA175486 and CA209851 to H.L., CA217842 to G.B.M., and CCSG grant CA016672); a grant from the Cancer Prevention and Research Institute of Texas (RP140462
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Classically HIF levels and consequently HIF
2022-06-22
Classically HIF-α levels and consequently HIF transcriptional activity have been associated with hypoxic conditions. However, some years ago, regulation by hormones of HIF transcriptional activity under normoxic conditions was demonstrated. Different stimuli such as heregulin, IGF1 and insulin, amon
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FoxM a downstream target of Gli has been mainly
2022-06-22
FoxM1, a downstream target of Gli, has been mainly related to MK-4827 Racemate mg regulation and cellular proliferation in tumor (Alvarez-Fernandez and Medema, 2013, Halasi and Gartel, 2013, Teh et al., 2002). Especially, FoxM1 is a regulator of G1/S and G2/M transitions and M-phase progression (Wo
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