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A selected set of these new derivatives
2024-12-31
A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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br Selective Androgen Receptor Modulators SARMs The AR and
2024-12-30
Selective Androgen Receptor Modulators (SARMs) The AR and its endogenous ligands, androgens, are important for development and maintenance of muscle and bone, secondary sexual organs, and development of other tissues (Mooradian et al., 1987). Although androgens are important for normal developmen
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br Materials and methods br Results br Discussion
2024-12-30
Materials and methods Results Discussion Intracellular metabolic pathways of sugar, such as glycolysis and TCA cycle, provide material and energy for the synthesis of other substances, including amino acids. Thus, the content of sugars and their metabolic pathways are important for amino AD
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We start with a basic description
2024-12-30
We start with a basic description of the MT-SGL model. Consider a multi-task learning (MTL) setting with k tasks. Let p be the number of covariates, shared across all the tasks, and n be the number of samples. Let denote the matrix of covariates, be the matrix of responses with each row correspond
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Cells have developed strategies aiming to enhance both the e
2024-12-30
Cells have developed strategies aiming to enhance both the efficiency of proteins with chaperone activity as well as their overall antioxidant capacity to maintain proteostasis under oxidative stress conditions (Miyata et al., 2012). For instance, 2-Cys peroxiredoxin is an abundantly expressed, anti
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br Endoplasmic reticulum protein ERp binds to AdipoR
2024-12-30
Endoplasmic reticulum protein 46 (ERp46) binds to AdipoR1 in HeLa cells ERp46 is localized in the ER and is suggested to act as a chaperone. About 20% of endogenous ERp46 are found at the plasma membrane suggesting that this protein may have additional functions. ERp46 interacts with TNF-alpha ce
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Regenerative mechanisms often require reemployment of
2024-12-30
Regenerative mechanisms often require reemployment of pathways used during development in the embryonic and postnatal periods (Waschek, 2002). PACAP has diverse neurodevelopmental and growth factor-like effects (Botia et al., 2007; Vaudry et al., 2009; Waschek, 2002; Watanabe et al., 2016) and it is
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Among the enzymes involved in adenosine metabolism adenosine
2024-12-30
Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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Given the powerful and ubiquitous nature of adenosine action
2024-12-30
Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl
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AMPK modulates changes in lipid metabolism via the
2024-12-30
AMPK modulates changes in lipid metabolism via the regulation of fatty CCG-100602 oxidation and cholesterol synthesis in the liver. The key enzymes involved include ACC and HMGCR [27,28]. Both participate in the rate-limiting steps of fatty acids and cholesterol synthesis and are inactivated on phos
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Streptomycetes are a group of filamentous Gram positive soil
2024-12-30
Streptomycetes are a group of filamentous Gram-positive, soil-inhabiting bacteria which have captured enormous screening interest because of their ability to produce and secrete a variety of triclabendazole and extracellular proteins [7]. Among the diverse antibiotics produced by Streptomycetes are
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On the basis of the
2024-12-30
On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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br Funding br Introduction l Dihydroxyphenylalanine l DOPA i
2024-12-30
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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The syntheses of a and
2024-12-27
The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each Cytokine signali
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br Exocytosis of GLUT by autophagy br Conclusion br
2024-12-27
Exocytosis of GLUT4 by autophagy Conclusion Conflict of interest Ethics statement Antigen processing and presentation Adaptive immune response has to be instructed to identify and eliminate specific pathogens or foreign entities defined by their antigenic determinants. Processed antig