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With LML methyl oxo dihydropyridazin yl piperidin
2022-03-17
With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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GSK has also been used
2022-03-17
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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Another level of complexity within the TGF SMAD and Hippo
2022-03-17
Another level of complexity within the TGF-ß/SMAD and Hippo/YAP/TAZ pathway crosstalks was recently uncovered. TGF-ß induces robust TAZ, but not YAP, protein expression in both mesenchymal and epithelial GGsTop through a SMAD3-independent, p38/MAPK-dependent mechanism that triggers myocardin-relate
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The stability and function of the HIF
2022-03-17
The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m
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br The SRP SR Heterodimer GTPase Tangos
2022-03-16
The SRP/SR Heterodimer: GTPase Tangos Drive Co-Translational Protein Targeting SRP and SR mediate a universally conserved protein targeting pathway responsible for the delivery of 25–30% of newly synthesized proteome to the eukaryotic endoplasmic reticulum (ER) or the bacterial plasma membrane 11
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Urinary hydroxypyrene OHP is a widely used
2022-03-16
Urinary 1-hydroxypyrene (1-OHP) is a widely used biological marker of exposure to PAHs and indicator for internal dose of activated PAHs (Jongeneelen, 1987, Adonis et al., 2003). PAH metabolites may be excreted either as free or as conjugated compounds. When 1-OHP is measured after treating the urin
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Intranasal immunization can induce the activation of IgA
2022-03-16
Intranasal immunization can induce the activation of IgA-secreting plasma cell precursors that are present in NALT and induce IgA antibody-secreting cells; these cells express l-selectin (+), allowing migration to the lymphatic nodes, as well as α4β1 (+), CXCR4 (+), and CCR10 (+), which facilitate m
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We found that most antigenic
2022-03-16
We found that most antigenic regions in GlyT1C are located in the second half of the GlyT1C-terminus, which is in concert with previously published results (Olivares et al., 1994). We however further show that in contrast to epitopes 554–625 which are affected by calcium only minimally, the epitopes
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br Conflict of interest statement br
2022-03-16
Conflict of interest statement Acknowledgments This work was funded in part by a grant from the National Institutes of Health, NIDDK award #DK61425 (to PWS). Introduction The efflux of toxic compounds from the cell by multidrug exporters is an important mechanism for cellular homeostasis a
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Although we showed that RBL H Sc cells took up
2022-03-16
Although we showed that RBL-2H3 Sc98 EDTA took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SERT for
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Glutamate is a ubiquitous principal excitatory neurotransmit
2022-03-16
Glutamate is a ubiquitous principal excitatory neurotransmitter in the Bortezomib that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive disorder, anxious an
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Both anxiety like behavior and
2022-03-16
Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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br Glucose metabolism and diet
2022-03-16
Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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br Acknowledgements br Introduction Ghrelin is
2022-03-16
Acknowledgements Introduction Ghrelin is a potent orexigenic hormone and growth hormone secretagogue mainly derived from the stomach [1], [2], [3], [4], [5]. Other pleiotropic actions of the hormone include those that are glucoregulatory, food reward-enhancing, gastric motility-enhancing, and
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Cartilage and subchondral bone synovial tissue interactions
2022-03-16
Cartilage and subchondral bone/synovial tissue interactions are well-recognized features of joint failure and osteoarthritis[17](seeFig. 1A, B). The intimate mechanical and biological interactions between these tissues are likely to alter the structural organization and function of either tissue. Ho
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