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Because of its excellent GPR
2022-08-04
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Go 6983 was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel of
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br The glycine transporter GlyT was originally identified as
2022-08-04
The glycine transporter 1 (GlyT1) was originally identified as a member of the solute carrier family 6 of sodium- and chloride-dependent neurotransmitter transporters . GlyT1 is expressed in the central nervous system and in peripheral tissues; mainly in erythroid cells, from erythroblasts in the
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LFFs associating with green algae utilize polyols therefore
2022-08-04
LFFs associating with green algae utilize polyols; therefore, we hypothesize that at least one polyol transport system is conserved in LFFs and it is required for the lichenization events that occur widely and independently in Ascomycota. Thus, the present study aimed to first evaluate phylogenetic
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Regarding the causative diseases of ES patients with unknown
2022-08-03
Regarding the causative diseases of ES, patients with unknown cause and those with encephalitis had significantly higher CSF levels of diacerein against GluN2B-NT2 and GluN2B-CT than the disease controls, but patients with genetic disorder and those with cortical dysplasia showed no significant dif
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br Acknowledgements The authors are grateful
2022-08-03
Acknowledgements The authors are grateful for funding provided by the Health Research Council of New Zealand. Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, fa
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In this study our result suggests that exogenous GR agonist
2022-08-03
In this study, our result suggests that exogenous GR agonist DEX and GR inhibitor RU486 can affect dopaminergic neurotransmitters in the brain. Pituitary adenylate cyclase-activating polypeptide (PACAP), an endogenous neuropeptide, can regulate the synthesis and release of catecholamine. McArthur et
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The biological actions of ghrelin are
2022-08-03
The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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This study compared PMS ascorbate and t
2022-08-03
This study compared PMS+ascorbate and t-BHP in terms of their effects on the volume-dependent parameters of normal human RBCs. Incubation with both oxidative systems resulted in the RBC density and osmotic resistance distribution shifts. Clotrimazole or Са2+ added into the medium, as well as high ex
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Initially we carried out gap FRAP
2022-08-03
Initially, we carried out gap-FRAP experiments using the two-photon configuration of the confocal microscope. A SR101-positive astrocyte was targeted and a 5 × 5 μm square area was exposed to a laser illumination (5 flashes of 5 s each during 25 s). This procedure resulted in a bleaching of this ast
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br Concluding remarks br Introduction The hair cells of vest
2022-08-03
Concluding remarks Introduction The hair in turn of vestibular organs detect linear and rotational head movements, providing sensory information that is essential for normal postural and visual reflexes. Most vestibular hair cells are produced during embryonic development, but they can be lost
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We next investigated whether pharmaceutical inhibition of th
2022-08-03
We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not signifi
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br Introduction Isoprenoid structures play
2022-08-03
Introduction Isoprenoid structures play an essential role in biology and over 30,000 natural products of this class are known (Greenhagen et al., 2003). Like other animals, insects require these compounds for many disparate processes, including electron transport (e.g., ubiquinones), protein glyc
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Macrophage populations are prominent in active IBD Strober a
2022-08-03
Macrophage populations are prominent in active IBD (Strober and James, 1986) as compared to healthy donors. Further, percentages of macrophages are increased in DSS-induced colitis (Grose et al., 2001, Ogawa et al., 2004). IBD is also linked to an influx of neutrophils and depletion of neutrophils b
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Smoking is strongly and consistently associated with periodo
2022-08-03
Smoking is strongly and consistently associated with periodontitis in the general population. In our study we detected a similar pattern in patients with HIV infection: smokers had a higher DPSI score compared to non-smokers. The exact cause of smoking as a risk factor for periodontitis in the gener
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Here we report the kinetics of inhibition of the MYST
2022-08-03
Here, we report the kinetics of inhibition of the MYST HAT family member KAT8 by MG149, and a calculation of the inhibitory constant Ki of MG149 for KAT8. The inhibition of HATs by MG149 could be correlated to inhibition of histone acetylation in murine PCLS upon MG149 treatment, as determined by a
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