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During the course of our research on mGlu PAMs
2019-09-11
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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Previous studies have demonstrated the
2019-09-11
Previous studies have demonstrated the role of the COMT Val158Met in response to positive and negative emotional stimuli (Bouhuys et al., 1999, Cohn et al., 2009), a fundamental process involved in well-being (Diener et al., 2009a, Diener et al., 1999, Gross and John, 2003). A handful of studies rep
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Based on the above we hypothesized
2019-09-11
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Therefore the relationship between ChEs activity and polymor
2019-09-11
Therefore, the relationship between ChEs activity and polymorphisms in POT1, TERF1, TERT genes were explored in order to screen susceptible biomarkers in this study. Materials and methods Results Discussion However, genetic toxicity induced by OPs has not been fully investigated so far. Ca
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Intriguingly our laboratory has shown that the I F kinase
2019-09-10
Intriguingly, our laboratory has shown that the I638F kinase domain mutant, unlike the L63V and G505 mutants, is incapable of receptor autophosphorylation and activation of its downstream effector SHP-2 when exposed to collagen stimulation. These data indicate that I638F is a loss of function mutati
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ornidazole br Acknowledgements br Introduction Laryngeal
2019-09-10
Acknowledgements Introduction Laryngeal cancers are the most frequent cancers of the head and neck region and their occurrence is strongly associated with the exposure to cigarette smoke and the consumption of strong alcohols. Almost all laryngeal cancers are squamous cell carcinomas. Usually
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br Material and methods br Results
2019-09-10
Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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The two SNPs rs rs presented above
2019-09-10
The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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Our conclusion is in disagreement with that of
2019-09-10
Our conclusion is in disagreement with that of a recent paper by Park et al. [10], which suggests that nitric oxide (NO) inhibition of VHL recruitment occurs by nitrosylation of the 520 cysteine in HIF-1α, and that SNAP does not directly inhibit hydroxylation of HIF peptide by HPH-2. Although this d
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Located on the fore tarsals of the front pair
2019-09-10
Located on the fore-tarsals of the front pair of legs, the Haller’s organ is presumed central to tick chemosensation. Recent genomic, transcriptomic and proteomic investigations have identified several families of transmembrane proteins in the forelegs of ticks that are likely involved in olfactory
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Where does this transfer process
2019-09-10
Where does this transfer process occur? The maternal side of the placenta is textured and spongy looking. The surface has 20–30 distinctive compartments named cotyledons, inside of which are the chorionic villi that form the principal functional structural unit of the placenta. These villi are compl
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The genetic asymmetries between parental
2019-09-10
The genetic asymmetries between parental genomes are also the subject of genetic conflict theory. This concept proposes that paternally inherited imprinted genes “extract” nutrients from the mother during gestation. By contrast, maternally inherited genes counteract the effect of paternal genes (Con
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MI has been detected in wastewater at
2019-09-10
3MI has been detected in wastewater at concentrations of 640–700 μg L−1 (Hwang et al., 1995) and up to 20 mg L−1 in decaying algal water environments (Peller et al., 2014). It is likely that 3MI accumulation in fish might be due to the degradation of endogenous amino acids. The presence of this che
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As in our earlier observations
2019-09-10
As in our earlier observations, the PTPN22 SNP affected the appearance of β-cell autoimmunity, but in contrast to our earlier report, only a borderline effect of the PTPN22 SNP on the progression to clinical disease was observed in the current analysis [22], [27]. The finding of an effect of the PTP
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br Materials and methods br Results
2019-09-10
Materials and methods Results Discussion The investigation of oxysterols is highly complex and challenging, arising not only from the large number of molecules in this family, but also due to their low abundance in biological systems compared to cholesterol and their susceptibility for auto
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