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br Acknowledgments I thank Takeshi Sakaba for critical readi
2022-10-02

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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In conclusion re evaluation of HER status is
2022-10-02

In conclusion, re-evaluation of HER2 status is necessary to determine the appropriate use of anti-HER2–targeted therapy beyond disease progression. EGFR and c-met amplification, as well as PIK3CA mutation, are rarely associated with acquired resistance. Our results highlight the importance of formal
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Also the decrease in adipocyte cAMP
2022-10-01

Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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br Glycoengineering br The Omics perspective The publication
2022-09-30

Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO dub ubiquitin for improved glycoprotein product
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opioid receptor antagonist The dopamine substrate currents I
2022-09-30

The dopamine substrate currents (IDA – IControl) were determined at different holding potentials (IV curves) in transfected HT22 cells (Fig. 5A). The plot for HT22 cells transfected with DAT exhibited the typical behavior of dopamine transporter currents (Ingram et al., 2002; Sonders et al., 1997),
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br Dysregulation of glutamate transporter expression and fun
2022-09-30

Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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The glucocorticoid GR complex exerts wide spread cellular ef
2022-09-30

The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of
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Receptors for glucagon Gcgr GLP
2022-09-30

Receptors for glucagon (Gcgr), GLP-1 (Glp1r), and GLP-2 (Glp2r) are G-protein coupled receptors (GPCRs) belonging to class B-1 (secretin receptor-like) family of GPCRs (Harmar, 2001, Fredriksson et al., 2003). The mammalian Gcgr, Glp1r, and Glp2r genes, together with the cysteine protease for the re
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The Hedgehog Hh pathway is linked to the development
2022-09-30

The Hedgehog (Hh) pathway is linked to the development of several types of epithelial cancers (Rubin and de Sauvage, 2006). A paracrine mechanism has been implicated in CAF activation, with Hh ligands secreted by cancer cells activating the glioma-associated transcription factors (Gli) in surroundin
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Homeobox genes can promote oncogenesis through multiple mech
2022-09-30

Homeobox genes can promote oncogenesis through multiple mechanisms, including gene translocation, loss of heterozygosity, gene amplification, DNA methylation, Amikacin remodeling, etc. For instance, translocation-mediated fusion of HOXA9 or HOXA13 on chromosome 7p15 with the nucleoporin gene NUP98
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Moreover intestinal chronic inflammation is a promoting fact
2022-09-30

Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic Purvalanol B cou
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br Role of FPRs in regulating
2022-09-30

Role of FPRs in regulating the inflammatory response Annexin I is a glucocorticoid-regulated protein possessing both pro- and anti-inflammatory activity that might be mediated, in part, by FPR activation [35]. Expressed in a variety of cell types, annexin I is particularly abundant in neutrophils
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More direct evidence of a
2022-09-29

More direct evidence of a role for Hat1 in the acetylation of newly synthesized histone H4 has come from a number of recent studies that have shown that Hat1 is responsible for at least a portion of the acetylation that occurs on histone H4 lysines 5 and 12 in the pool of cytosolic histones. In chic
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Compared to the other histamine receptor subtypes the
2022-09-29

Compared to the other NVP-AEE788 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) and
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br Materials and methods br Results Estimations of OMP gener
2022-09-29

Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of Eltrombopag concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fracti
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