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Raloxifene is a second generation SERM that has tissue
2020-06-19
Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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br Introduction Receptor tyrosine kinases RTKs are criticall
2020-06-19
Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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Interest in the PGE EP pathway is increasing given its
2020-06-19
Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing NU 9056 sale inflammation [15]. The EP4 re
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br Materials and methods br
2020-06-19
Materials and methods Results Discussion In rodent species, CYP2E1 and CYP2B have been implicated in CCl4 metabolism. In this study, we used expressed human CYP2E1 to show that this enzyme is a high-affinity catalyst responsible for low-dose CCl4 metabolism. Studies employing an inhibitory
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OHC is a potent regulator of LXR
2020-06-19
25-OHC is a potent regulator of LXR-mediated pathways, that impact on SKF 83566 hydrobromide lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OHC is
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BRD4770 sale Our study provides proof of principle for dimer
2020-06-19
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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The roles of ginsenoside in E and S proteasome
2020-06-19
The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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Concerning firmness postharvest calcium dips for
2020-06-19
Concerning firmness, postharvest calcium dips for whole fruit have been demonstrated to preserve firmness, cell wall structure (Glenn and Poovaiah, 1990), nutritional quality (Goldberg, 1984) and fruit flavour (Ortiz et al., 2009). Similarly, combinations of calcium treatment (0.5–4%) with packaging
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The serotonin transporter gene encodes
2020-06-19
The serotonin transporter gene () encodes an integral membrane protein that transports serotonin from the synaptic spaces into the presynaptic neurons. The encoded protein terminates the action of serotonin and recycles it in a sodium-dependent way. This protein is a target of psychomotor stimulants
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br Functional significance Defects of the
2020-06-19
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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br Roles for intracellular chloride channels br
2020-06-19
Roles for intracellular chloride channels Specific chloride channel proteins in intracellular membranes Concluding remarks Introduction The sulfonylurea derivative glybenclamide (GLYB) is used as oral hypoglycemic agent to treat non-insulin dependent diabetes mellitus [1], [2]. The antid
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The swelling independent activation of
2020-06-19
The swelling-independent activation of chloride channels by glycerol is proved by our further experiments. When glycerol concentration in the isoosmotic solution was reduced to the micromolar scale or even lower concentration, a Cl− current was still induced. The Cy5 azide mg were not swollen by th
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br Most reported binding data are obtained by performing
2020-06-19
Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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Amphiphilic compounds lower interfacial tension and its biol
2020-06-19
Amphiphilic compounds lower interfacial tension and its biological production often results in a competitive environmental advantage (Darvishi et al., 2011). The reduction of interfacial tension can increase the biologically available surface areas resulting in increased metabolism of insoluble com
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Initial investigations in the heart uncovered Epac
2020-06-18
Initial investigations in the heart uncovered Epac as a positive regulator of myocyte hypertrophy [8], [9]. Concomitantly, Epac has been shown to regulate cardiac Ca homeostasis [8], [10], [11], [12], [13]. Ca is an essential second messenger in the cardiac physiology because its rhythmic variations
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