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Downregulation of tumor suppressors is a major
2020-01-29
Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the PF-5274857 of which is often downregulated or even absent in the majority of human cancers, functions as a phosphatase to
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Due to the high attractiveness of
2020-01-29
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), Thyroid Hormone Receptor Antagonist (1-850) (Davydov et al., 2004, Huang et
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Autoradiography studies have shown cerebellum to
2020-01-29
Autoradiography studies have shown Zoniporide hydrochloride to be devoid of D1-R [40], confirming that this region may serve as reference for estimation of free and non-specifically bound radioligand concentration in tissue (= non-displaceable uptake). In initial human studies using [11C]SCH 23390 a
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Although the implication of DA and
2020-01-29
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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Apart from neutrophil mediated inflammation the production
2020-01-29
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α prod
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TR provides requirements for qualification of commercial PLC
2020-01-29
TR-107330 (1996) provides requirements for qualification of commercial PLC. It uses the criteria of NUREG/CR-6421. EPRI TR-104159 (1995) includes experience about dedicating COTS SW for PLC-based digital systems such as DAFAS (Diverse Auxiliary Feedwater Actuation System) and Emergency Diesel Bus Lo
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Cardiogenesis is enhanced with timely applicati
2020-01-29
Cardiogenesis is enhanced with timely application of Wnt pathway activators and inhibitors. A combination of Wnt/β-catenin signaling pathway activators such as CHIR99021 and inhibitors such as IWP-2 and IWR-1 have been found to be highly efficient cardiomyocyte differentiation protocols [27], [28].
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Since the aggregation of neurotoxic forms of A plays a
2020-01-29
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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Estrogen receptors ERs belong to the third class of nuclear
2020-01-29
Estrogen receptors (ERs) belong to the third class of nuclear receptors (NR3) [23]. Two different forms of ER have been described, ERα and ERβ. They are coded by two distinct genes (ESR1 and ESR2, respectively) containing 8 transcribed exons that give rise to six conserved protein domains: domains A
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br The orphan estrogen related receptor exists as three
2020-01-29
The orphan estrogen-related receptor exists as three subtypes (ERRα, ERRβ, and ERRγ) in the human genome. ERRα is expressed in metabolically active tissues such as muscle and adipose. ERRγ is expressed in the spinal cord and CNS. ERRβ appears to play a role in development, as postnatal expression
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br Experimental section br Acknowledgments
2020-01-29
Experimental section Acknowledgments This work was supported by the National Natural Science Foundation of China (NSFC, Grant No. 81573285 and No. 81602965), the Natural Science Basic Research Plan in Shaanxi Province of China (Program No. 2018JM7071 and No. 2017JQ8002), and the Fundamental Re
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br Materials and methods br Results br Discussion
2020-01-29
Materials and methods Results Discussion Inflammatory signalling and in particular the arachidonic patupilone sale cascade have been suggested as targets for disease modification, optimization of the therapeutic response, and even restoration of pharmacosensitivity (Potschka, 2010). Recentl
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Propylthiouracil receptor Some antioxidants including N acet
2020-01-29
Some antioxidants, including N-acetylcysteine and SOD, have been shown to decrease collagen deposition and protect the lungs in various animal models and even in clinical trials (Chan et al., 2013, Loomis-King et al., 2013, Rafii et al., 2013, Teixeira et al., 2008, Wang et al., 2013). Bleomycin-ind
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Ubiquitin activating enzyme activates ubiquitin
2020-01-29
Ubiquitin-activating enzyme activates ubiquitin by a three-step process with ATP as a cofactor (Chen et al., 2011, Haas and Rose, 1982, Haas et al., 1982). We demonstrated that ATP is required for mRFP-Ub–E1 formation under non-reducing conditions (Fig. 2A). A time course of radioactive ATP product
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Tailoring pharmacological treatment to the genetic backgroun
2020-01-29
Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72
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