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Most remarkably an essentially identical collagen binding mo
2019-11-02
Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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Most xenobiotics undergo biotransformation before
2019-11-02
Most xenobiotics undergo biotransformation before being excreted. Such biotransformation is classified into two phases. In the first phase, the lipophilic substrate is oxidized by the cytochrome P-450 (CYP450) enzyme system, which introduces a single oxygen TPMPA into the molecule (Moutou et al., 1
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In the case of high fidelity polymerases we propose that
2019-11-02
In the case of high-fidelity polymerases, we propose that water is used to achieve negative selection against nucleotide binding. With specialized DNA polymerases, we propose that nucleobase desolvation plays a different yet important role in allowing these enzymes to replicate damaged DNA. In this
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It is well known that CysLTs
2019-11-02
It is well known that CysLTs exert potent contractile action on human bronchial smooth muscles through activation of CysLT1 receptors. Indeed, in vitro antigen-induced contraction of passively sensitized human bronchial tissue is markedly suppressed by a pre-treatment with CysLT1 receptor antagonist
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In humans individual differences in prefrontal dopamine
2019-11-02
In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia
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br The modulation of ER from
2019-11-02
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective DGAT-1 inhibitor receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity,
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br Methods br Results br Discussion MEN is a potent
2019-11-01
Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3
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ASC-J9 Under optimized assay conditions very low concentrati
2019-11-01
Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO ASC-J9 membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little specific binding
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br Materials and methods br Results
2019-11-01
Materials and methods Results and discussion Conclusions In the present study, we have shown the important role of miR-204-5p in C2C12 myoblast differentiation. Overexpression of miR-204-5p inhibited myogenic differentiation and decreased the formation of slow-twitch myofibers, whereas miR-
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br Author Contributions br Acknowledgments br Introduction O
2019-11-01
Author Contributions Acknowledgments Introduction Osteoporosis is a common bone disease that frequently leads to disruption of the alveolar and systemic bones with age. Novel osteoanabolic strategies to treat osteoporotic bone loss or augment fracture repair efficiently are desired. Since b
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Proof of concept studies with
2019-11-01
Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d
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Regarding the mechanism of action of CRF
2019-11-01
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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Anisomycin br Acknowledgments This research was
2019-11-01
Acknowledgments This research was supported by grants from the Ministerio de Ciencia e Innovación (Grants SAF/FEDER 2010-17907; 2013-49076-P), Spain, Red de trastornos adictivos (RETICS RD12/0028//0003, Instituto de Salud Carlos III, Spain) and Fundación Séneca (15405/PI/10, Región de Murcia, Spa
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This study has several limitations First despite
2019-11-01
This study has several limitations. First, despite the relatively large number of participants for a pharmacological neuroimaging study, sample sizes for examining the modulation of THC effects by COMT eukaryotic initiation factor were small. Therefore, these particular findings should be interpret
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Over the last decade numerous studies have
2019-11-01
Over the last decade, numerous studies have evaluated the acute, short-term, and medium-term impact of pulmonary vasodilators on Fontan physiology.23., 24., 25., 26., 27., 28., 29., 30., 31. Although different mct2 inhibitor of medications have been evaluated, phosphodiesterase-5 (PDE-5) inhibitors
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