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With the narrow SAR of the tail favouring
2020-10-23
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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The quaternary structure of many of the family B members
2020-10-22
The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and bruton\'s tyrosine kinase receptors) have been actively studied and it has been demonstrated that they can form homodimers/oligomers (Gao et al., 2009; Ng & Chow, 2015; Ng, Lee, & Chow, 201
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Enalapril Maleate receptor In the brain E can modulate the m
2020-10-22
In the brain, E2 can modulate the mitogen-activated protein kinases/extracellular signal-regulated kinases (MAPK/ERK) pathway, which is involved in the formation of different memory types (Atkins et al., 1998, Blum et al., 1999, Schafe et al., 2000). When the MAPK/ERK signaling pathway is activated,
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br Methods br Discussion In a recent
2020-10-22
Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of BI-D1870 synthesis level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard treatment
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There is an opposite opinion indicating that EphB plays
2020-10-22
There is an opposite opinion indicating that EphB plays a role as cancer suppressor. Batlle et al. showed that loss of EphB expression represented a critical step in CRC progression, and CRCs that lacked EphB2 expression have been correlated with more advanced tumour stage, poor differentiation, and
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We elucidated that the ten DGK isozymes
2020-10-22
We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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The first example of a broadly acting antiviral drug is
2020-10-22
The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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br Materials and methods br Results br Discussion The first
2020-10-22
Materials and methods Results Discussion The first DGAT1 gene was described in the mouse in 1998 [28], and a few years later DGAT2 was identified from the oleaginous fungus Mortierella ramanniana[29]. Although both of them are known as the primary enzymes for de novo TAG biosynthesis, they
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br Acknowledgments br Introduction Cysteinyl leukotrienes Cy
2020-10-22
Acknowledgments Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic Arylquin 1 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3
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During the course of our research
2020-10-22
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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To ascertain that the slower migrating
2020-10-22
To ascertain that the slower migrating bands represented phosphorylated CDK5, we performed a phosphatase assay. Lysates of cytochrome p450 inhibitors co-expressing p35 and either WT or D144N CDK5 were immunoprecipitated using an anti-p35 antibody. The immunoprecipitates were then dephosphorylated us
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POE specialises Rogers definition of engineering to systems
2020-10-22
POE specialises Rogers\' definition of engineering [37] to systems engineering as: As such, systems engineering becomes a problem solving exercise, the problem being, given a physical environment E, to find the system S that factor xa inhibitor meets a real-world need N to the satisfaction of a gr
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Sex has been shown to mediate the
2020-10-22
Sex has been shown to mediate the relationship between allelic differences in COMT and behavior (Harrison & Tunbridge, 2008). The COMT promoter region contains 2 estrogen response elements (Xie, Ho, & Ramsden, 1999) that can inhibit the formation of COMT (Jiang, Xie, Ramsden, & Ho, 2003). With regar
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A similar pattern was observed
2020-10-22
A similar pattern was observed for both tissues of P. harpagos, evidencing the absolute predominance of acetylcholinesterase. As observed, no effects were attributed to Iso-OMPA. The hypothesis that the major cholinesterasic form is AChE was reinforced considering the higher hydrolytic activity, whi
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br Conclusion This study demonstrates the
2020-10-22
Conclusion This study demonstrates the presence of functionally viable ET receptors in the surgically extracted tissue from patients with CTEPH. The ET receptor was associated with smooth muscle cells, mainly the contractile phenotype of SMC that surrounds the recanalised cetrimonium bromide and
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