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br Conflict of interest br Introduction The
2024-07-16
Conflict of interest Introduction The Piezo proteins, Piezo1/FAM38A and Piezo2/FAM38B, are multi-pass transmembrane proteins that have been identified as mechanically-activated (MA) homomultimeric, pore-forming ion channels [1,2]. Piezo1 is broadly expressed with its highest expression in blad
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To confirm a role of OCT in
2024-07-16
To confirm a role of OCT3 in corticosterone-induced potentiation of cocaine-primed reinstatement, we examined the interaction of corticosterone and cocaine in the reinstatement of cocaine conditioned place preference (CPP) in wild type mice, and transgenic OCT3-deficient mice. These mice express a t
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Adiponectin also works on AdipoR inducing extracellular Ca i
2024-07-16
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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AdipoRon acts on the anti diabetic effects of adiponectin ex
2024-07-16
AdipoRon acts on the anti-diabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively [23]. AdipoR activation is a promising treatment for diabetes, nonalcoholic fatty liver disease, and cardiovascular disease, demons
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The activation of the A
2024-07-16
The activation of the A2BR subtype triggers different intracellular metabolic pathways, often linked to the activation of adenylyl cyclase and increased levels of intracellular cAMP (Lynge et al., 2003, Bernareggi et al., 2015). The nAChR-channel kt 4 mediated by the cAMP/PKA pathway was reported t
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Further analysis sought to understand the mechanism associat
2024-07-16
Further analysis sought to understand the mechanism associated with the autotaxin-mediated increase of miR-489-3p in circulation. Based upon sequence complementarity, DIANA TarBase predicted miR-489-3p targets MAPK2K1, or MEK1, an oncogene widely dysregulated in cancer (Fig. 4A). To test this relati
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br The Molecular Machinery of Autophagy and Regulation by
2024-07-16
The Molecular Machinery of Autophagy and Regulation by Sphingolipids Sphingolipid-Mediated Autophagy in Cancer: Dr. Jekyll and Mr. Hyde Autophagy is an evolutionarily conserved stress response that typically promotes survival and antagonizes apoptosis. However, excessive autophagy was found to
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In this review we will present the traditional and
2024-07-16
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Hyperactivity of the hypothalamus pituitary
2024-07-15
Hyperactivity of the hypothalamus-pituitary-adrenal (HPA) axis, which is well described in MDD (Pariante and Lightman, 2008, Marques et al., 2009), is also observed in AD and results in increased glucocorticoid (GC, cortisol in primates) levels in blood and CSF (Davis et al., 1986, Martignoni et al.
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Negative regulation of AR expression by
2024-07-15
Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as
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integrin inhibitor In our study the expression levels
2024-07-15
In our study, the expression levels of adiponectin and its receptors in the uteri, conceptuses, and throphoblasts were determined by the stage of early pregnancy. Therefore, it could be hypothesized that the adiponectin system is regulated by the local hormonal milieu. Hormonal regulation in the ute
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-07-15
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Our published data showed that in mouse heart the protein
2024-07-15
Our published data showed that, in mouse heart, the protein level of WDR1 was highest during the embryonic stage, but became progressively decreased to a constant level from birth to adulthood (Yuan et al., 2014), indicating an important role of WDR1 in embryonic heart development. However, function
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br Conflict of interest br Financial support br Acknowledgme
2024-07-15
Conflict of interest Financial support Acknowledgments This work was supported by the Japanese Millennium project. We thank all members of the Center for Genomic Medicine of RIKEN and Dainippon-Sumitomo Pharma Co., Ltd. for supporting this study. We are also grateful to members of the Hiros
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Based on the improved characteristics of the mutant ECDs
2024-07-15
Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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