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Acidic substituents showed moderate biochemical activity but
2019-09-19
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic wdr5 were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical activi
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br Amygdala microcircuitry and fear learning Recent work has
2019-09-19
Amygdala microcircuitry and fear learning Recent work has begun to dissect functional amygdala circuits that are responsible for the acquisition and expression of fear learning. Ciocchi et al. (2010) identified separable populations of 12198 and within the CeAL that have opposite responses to CS
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Vilazodone Hydrochloride Proof of concept studies with disul
2019-09-18
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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br Acknowledgments br The design of polyaromatic
2019-09-18
Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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DGK is highly expressed in skeletal
2019-09-18
DGKδ is highly expressed in skeletal muscle [7], which is a primary target of insulin for glucose disposal [14]. Notably, Chibalin et al. reported that DGKδ contributes to hyperglycemia-induced peripheral insulin resistance and that decreased protein levels of DGKδ in skeletal muscle attenuated gluc
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In order to validate the ATP competitive mode of
2019-09-18
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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br EBI structure and expression The gene encoding EBI
2019-09-18
EBI2 structure and expression The gene encoding EBI2 was originally identified together with EBI1 (CCR7) as the most highly upregulated gene in Epstein–Barr virus-infected Burkitt\'s lymphoma cells [18]. EBI2 belongs to the rhodopsin-like subfamily of seven transmembrane GPCRs [19]. Although it i
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The presence of a vicious cycle established between tumor pr
2019-09-18
The presence of a “vicious cycle” established between tumor proliferation and paratumor osteolysis plays a crucial role in the development of primary bone tumors [53]. Cancer cells produce soluble factors that activate directly or indirectly via osteoblasts, osteoclast differentiation and maturation
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At one time the biological effects of cAMP
2019-09-18
At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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There may be an interplay of EP
2019-09-18
There may be an interplay of EP2, EP3, EP4 alone, or in combination, with EP1 for the onset of TCDD-induced neonatal hydronephrosis. EP2 and EP4 have been reported to increase AQP2 phosphorylation and membrane trafficking (Li et al., 2009; Olesen et al., 2011). The EP2 and EP4 mRNA concentrations we
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Where a a a and b b b
2019-09-17
Where a, a, a and b, b, b are respectively, repulsive friction constants and attraction friction constants. c represents the quadratic repulsive friction constant and P is critical pressure (bar). CPA equation of state CPA model is an EOS that simply combines a cubic EOS (SRK-EOS) and an associ
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NF B is a family
2019-09-17
NF-κB is a family of protein mediators that regulate various innate and adaptive immune responses [29,30]. The NF-κB family consists of the following five proteins: c-Rel (Rel); p65 (RelA); RelB; p50(NF-κB1); and p52(NF-κB2). It has been confirmed that NF-κB is activated by TNF family cytokines, suc
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br Enzyme activations Activated proteinases can
2019-09-17
Enzyme activations Activated proteinases can unleash a deluge of tissue damage (Zucker et al., 2009). Once activated, the essential enzymes such as serine proteases and cysteine proteases cannot discriminate between self and non-self, burning away self-tissues (Chien et al., 2009, Laskar et al.,
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br Funding This work was partly supported
2019-09-17
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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The absence of the LIG gene in yeasts
2019-09-17
The absence of the LIG3 gene in yeasts has prevented the use of genetically tractable lower eukaryotes, such as Saccharomyces cerevisiae and Schizosaccharomyces pombe, as models to gain insights into the cellular functions of and interplay between the DNA ligases encoded by the LIG1, LIG3 and LIG4 g
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