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This variant has also been related to
2021-10-12
This variant has also been related to a better treatment response in patients with metastatic colorectal cancer subjected to irinotecan-based chemotherapy (Kweekel et al., 2008). Inheritance of this metabolic variability has also been stated to influence better treatment outcomes in breast cancer pa
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elastase inhibitor Finally LC ESI MS MS
2021-10-12
Finally, LC-ESI-MS/MS was applied to explore the effects of increased fT4 levels 4 and 8 weeks after induced thyrotoxicosis and have revealed an upregulation of proteins involved in blood coagulation, thus providing a clear association [126]. Conclusions Introduction Diabetes mellitus (DM) ha
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G protein coupled receptor GPCR ligands can be classified
2021-10-12
G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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br Acknowledgements This work was supported by Slovak Academ
2021-10-12
Acknowledgements This work was supported by Slovak Academy of Sciences grants VEGA 2/0052/10 and 2/0045/10. Both clinical observations and preclinical studies suggest that hypofunction of -methyl--aspartate (NMDA) receptor is implicated in the pathophysiology of schizophrenia. Thus, therapeuti
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Previously we have shown that the natural flavonoid compound
2021-10-12
Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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br Material and methods br Results br
2021-10-12
Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new BI6727 with different structures have been synthesized in order to cr
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In experiments using D to displace binding
2021-10-12
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse Desfuroylceftiofur tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1,
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It is well known that
2021-10-12
It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling
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To support maximal growth and metabolic function of
2021-10-12
To support maximal growth and metabolic function of major organs, glucose and ASA 404 synthesis are essential. We assessed the plasma levels of glucose and amino acids in LBW and NBW piglets at birth and at day 7 postpartum. Blood glucose levels were influenced by birthweight and age. In this study
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Amsacrine br GLP R expression in the vascular endothelium Im
2021-10-11
GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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Introduction The Hedgehog Hh signaling pathway regulates emb
2021-10-11
Introduction The Hedgehog (Hh) signaling pathway regulates embryonic organogenesis, tissue patterning, and cell differentiation (Armas-Lopez et al., 2017, Ingham and McMahon, 2013). Aberrant activation of Hh signaling pathway contributes to tumor formation and development of various cancers includi
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For the two KO models
2021-10-11
For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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High lipophilicity of seems to cause poor PK profiles First
2021-10-11
High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i
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The involvement of prostaglandins on the effects
2021-10-11
The involvement of prostaglandins on the effects induced by 1-nitro-2-phenylethane is similarly unlikely because vasorelaxation was not changed by indomethacin [20]. The inhibition of adenylyl cyclase with MDL-12330A [21] or cAMP-dependent protein kinase A with KT-5720 [22] also did not interfere wi
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Routine administration of exogenous GC is pertinent during l
2021-10-11
Routine administration of exogenous GC is pertinent during late gestation, particularly in women who are at risk of delivering a preterm infant, aiming at ensuring proper neonatal outcome and survival (Kamath-Rayne et al., 2012). Unfortunately, despite its beneficial roles in foetal survival, variou
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