• Determination of relative potency EC by dose response assays

  2019-08-27

  

  Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an

• The assembly and maturation of

  2019-08-27

  

  The assembly and maturation of invadopodia can be initiated by chemical stimuli such as the epidermal growth factor (EGF), as well as the mechanical signals from extracellular matrix (ECM). Upon binding, EGF activates the EGF receptor (EGFR), which further activates several intracellular signaling p

• br Conclusion The results of the current study show

  2019-08-26

  

  Conclusion The results of the current study show that boldness is associated with higher gene expression of drd2a, drd2b and oprd1b in zebrafish males. The results are correlational and additional experiments are needed to clarify the causal role of these receptors in zebrafish behavior. Confl

• br The major regulator of radiation

  2019-08-26

  

  The major regulator of radiation sensitivity Tumor cell resistance to radiation is a big issue for radiation therapy, and a major concern of radiation oncologist. Understanding the regulation mechanism of radiation sensitivity is still a research hotspot. Increased sensitivity to ionizing radiati

• Several authors have been pursuing the aim of

  2019-08-26

  

  Several authors have been pursuing the aim of finding good performing organic solvent compatible adsorbers useful in the context of API purification [[10], [11], [12], [13], 22, 23]. For sulfonate GTIs, scavenging nucleophilic resins [22, 23] or molecular imprinted polymers (MIPs) [10] have been exp

• For the SAR optimization of the right hand side it

  2019-08-26

  

  For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic SQ 29,548 moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by condensati

• Our results also showed that

  2019-08-26

  

  Our results also showed that the highest dose of Astressin2-B increased the rewarding effects of cocaine, since non-defeated animals treated with this dose developed CPP with a sub-threshold dose. We monitored the acute effects of 30 µg/kg of Astressin2-B and found an increase of anxiety in the open

• Assessment of the activity of native and denatured

  2019-08-26

  

  Assessment of the activity of native and denatured TAT-CPG2 after penetration suggests that TAT-CPG2 has been successfully delivered into the cells, and the transduced enzyme is functional inside the cells. The enzyme activity of both native and denatured TAT-fusion proteins in the cultured HepG2 FD

• This work started from the standard version of the CPA

  2019-08-26

  

  This work started from the standard version of the CPA model [17] and investigated its known weaknesses: 1) not meeting the defined critical temperature, 2) missing the temperature dependence of pure component saturated liquid densities, 3) using an α function in the cubic term that can provide unre

• Mass spectrometry has previously been used to examine the pr

  2019-08-26

  

  Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino Demethoxycurcumin kinase analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present stud

• LJI308 clinical Hymenialdisine the most potent inhibitor of

  2019-08-26

  

  Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this LJI308 clinical also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of

• Furthermore in silico physicochemical characters and pharmac

  2019-08-26

  

  Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val

• The present study is the first time to investigate

  2019-08-26

  

  The present study is the first time to investigate the effect of piperine on intestinal sterol transporters and enzymes in the small intestine. NPC1L1 is a sterol transporter responsible for taking up cholesterol from the lumen to enterocytes (Davis et al., 2004). ACAT2 is an enzyme, which esterifie

• The previously described endogenous patterns of IGF induced

  2019-08-26

  

  The previously described endogenous patterns of IGF-1-induced kinase signaling, and resulting interaction between MAPK and PI3K, differ across neuronal sub-types. In R28 retinal neuron-like cells, IGF-1 treatment elicits prolonged activation (at least 80 min) of both PI3K and MAPK (Kong et al., 2016

• The inhibition of FAS by C produces an accumulation

  2019-08-24

  

  The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi

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