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The importance of insulin in controlling
2024-04-19
The importance of insulin in controlling lipolysis and fat mass is further emphasized by mouse models with alterations in the insulin signaling pathway of adipocytes. For example, mice with a tamoxifen-inducible knockout of the insulin receptor in mature adipocytes reveal a substantial decrease of a
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Our in vitro data show that CyaA
2024-04-19
Our in vitro data show that CyaA does not play a critical role in the bacterial adherence to mammalian cells. This observation is in contrast to previous studies that reported a role for CyaA in FHA-mediated adherence of B. pertussis bacteria to the respiratory epithelial Alrestatin [37,38]. This d
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br The role of AMPK beyond energy homeostasis
2024-04-19
The role of AMPK beyond STAT5 Inhibitor receptor homeostasis: regulating metabolism AMPK plays a major role in glucose homeostasis by modulating glucose transport in peripheral tissues [20]. Skeletal muscle, one of the main peripheral tissues involved in glucose uptake and disposal, expresses gl
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The AChR is composed of five homologous membrane spanning
2024-04-19
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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However although in vitro studies in
2024-04-19
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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NBI 27914 hydrochloride Vortioxetine is a multimodal antidep
2024-04-19
Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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Having established the structural requirements
2024-04-19
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Upregulation of ACLY is common in many cancers
2024-04-19
Upregulation of ACLY is common in many cancers (Kuhajda, 2000, Milgraum et al., 1997, Swinnen et al., 2004, Yahagi et al., 2005). This is in part due to the transcriptional activation by SREBP-1 resulting from the activation of the PI3K/AKT pathway in cancers (Kim et al., 2010, Nadler et al., 2001,
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br Mechanisms of GPCR internalization
2024-04-19
Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated FTI 277 HCl (CME) is the best characterized and argua
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The apoptosis promoting Bcl family includes BH
2024-04-19
The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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br COPD As in asthma also in COPD increased
2024-04-19
COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode
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br Experimental procedures br Results br
2024-04-19
Experimental procedures Results Discussion Major depressive disorder is among the leading causes of disability worldwide (Vos et al., 2015). One of the major causal or exacerbating factors of depression is long term stress or psychological trauma (Liu and Alloy, 2010). Dysregulation of the
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Introduction Heterotrimeric G proteins mediate signal transd
2024-04-19
Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s
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The current antifungal pipeline contains several categories
2024-04-19
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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br Alzheimer s disease AD
2024-04-18
Alzheimer’s disease (AD) is an irreversible, age-associated neurodegenerative disorder that is characterized by progressive memory loss and cognitive decline. AD is also the leading cause of dementia, accounting for 5 million cases in the United States and 44 million cases worldwide. In 2015, AD c