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The allosteric site of class C receptors is generally locate
2024-03-27
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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In addition to connecting high ARG levels with
2024-03-26
In addition to connecting high ARG1 levels with DNMT3A/TET2 mutations in MDS/CMML patient biopsies, we also wanted to address the cell type demonstrating elevated ARG1. Following our mouse work, we hypothesized that overexpression of this protein would be found in myelomonocytic O-propargyl-puromyci
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Acarbose mg Due to anatomical and physiologic characteristic
2024-03-26
Due to anatomical and physiologic characteristics of the eye, administration of ophthalmic medicines is difficult and many studies showed that only approximately 5% of the administrated dose are absorbed by intraocular tissues, making the treatment unfeasible for diseases located in posterior segmen
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Here we found that AMPK directly phosphorylates
2024-03-26
Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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br Materials and methods br Results
2024-03-26
Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following
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br Perspective AA LA and other PUFAs
2024-03-26
Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path
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Interestingly intermittent high doses of AKT inhibitors have
2024-03-26
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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Interaction between AhR and ligands leads to AhR transformat
2024-03-26
Interaction between AhR and ligands leads to AhR transformation (Fig. 1), characterized by a rapid receptor nuclear translocation and the formation of AhR/Arnt complex and the release of the chaperone proteins. Following AhR transformation, the AhR/Arnt complex binds to its cognate DNA consensus seq
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br Role of OCT in histamine clearance Histamine is a
2024-03-26
Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for
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The excellent potencies selectivities and improved PK
2024-03-26
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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br Conclusion br Conflict of Interest br Author Contribution
2024-03-26
Conclusion Conflict of Interest Author Contributions Acknowledgements This work was supported by a research grant (SR/50/AS-14/2012) from the Department of Science and Technology, New Delhi, India to CMC and CSIR Senior Research Fellowship (09/013(0339)/2010-EMR-I) to SB. Introduction
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As we previously observed in the NSFT
2024-03-26
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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br Materials and methods br Results br Discussion This study
2024-03-26
Materials and methods Results Discussion This study demonstrates that treatment with a selective adenosine kinase inhibitor ABT-702, thereby enhancing extracellular adenosine, can provide partial protection from age-related hearing loss in C57BL/6J mice. Chronic treatment with ABT-702, comm
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Though we have proved that
2024-03-26
Though, we have proved that VA could suppress hepatic gluconeogenesis, the mechanisms of VA on gluconeogenesis in vivo and in vitro remain unclear. AMP-activated protein kinase (AMPK), which is called an energy receptor enzyme, is widely expressed in liver and other tissues [23]. AMPK has become ano
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br Conflict of interest br Ethics committee br Introduction
2024-03-26
Conflict of interest Ethics committee Introduction Severe combined immunodeficiency due to adenosine deaminase deficiency (ADA-SCID) is characterized by impaired function and differentiation of T, B, and natural killer (NK) cells. Non-immunological abnormalities may also occur, including fa
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