• Compounds and possessed relatively low clogP

  2019-11-04

  

  Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.

• Soon after the discovery of ET

  2019-11-04

  

  Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).

• Determination of relative potency EC by

  2019-11-04

  

  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

• Damage of PE HD due

  2019-11-04

  

  Damage of PE-HD due to both mechanisms is usually considered to emerge from a local stress concentration in the material, leading to the initiation of a crack, which subsequently propagates further through the material, and finally leads to macroscopic failure. In this process, crack growth occurs o

• Tropical theileriosis is caused by the apicomplexan

  2019-11-04

  

  Tropical theileriosis is caused by the apicomplexan parasite Theileria annulata which is transmitted by a tick vector from the genus Hyalomma in cattle (Echebli et al., 2014, Li et al., 2014). Theileria parasites invade the leukocytes by sporozoites secreted from the vector, schizonts mature into me

• br Methods br Results br Discussion

  2019-11-04

  

  Methods Results Discussion With this study, we provided evidence that acriflavine can interfere with EMT and UPR, two well-described pathways associated with cancer aggressiveness. And, because drug resistance is also clearly associated with the mesenchymal state [36], blocking of the epith

• Lymphocyte mobility and homing is modulated by the chemoattr

  2019-11-04

  

  Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21

• Modulating protein stability specifically inhibiting ubiquit

  2019-11-04

  

  Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here

• Our previous work has demonstrated that

  2019-11-02

  

  Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi

• A previous study suggested that DARs and octopamine tyramine

  2019-11-02

  

  A previous study suggested that DARs and octopamine/tyramine receptors (OARs/TARs) have close pharmacological properties (Beggs et al., 2011). Their relationships were also supported by phylogenetic analyses (Balfanz et al., 2005, Hauser et al., 2008, Wu et al., 2014), indicating that some of DAR an

• DGK is also involved in cell

  2019-11-02

  

  DGKδ is also involved in cell differentiation. Previously, to investigate the physiological roles of DGKδ, DGKδ-deficient mice have been generated. On the basis of the analysis of DGKδ-deficient mice, Crotty et al. reported that DGKδ regulates the epidermal growth factor receptor (EGFR) pathway by a

• In this study using REMD with

  2019-11-02

  

  In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).

• br Results Table shows demographics and clinical features

  2019-11-02

  

  Results Table 1 shows demographics and clinical features of subjects with obesity and controls. Before surgery five obese were diabetic, only one on glucose-lowering therapy; three obese were dyslipidemic and assumed lipid lowering medications. Lathosterol levels were significantly higher in pati

• In the present study it

  2019-11-02

  

  In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including CARIPORIDE recep

• The changes in the chemokine

  2019-11-01

  

  The changes in the chemokine receptors CCR-5 and CXCR-4 in women and men with PTSD are completely different. In the group of women with PTSD alone the level of this Melatonin increased six times, whereas, in women with APD and PTSD, the level of the receptor CCR-5 was eight times higher than in the

14152 records 914/944 page Previous Next First page 上5页 911912913914915 下5页 Last page