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Recently naphthoquinone derivatives have shown promising
2020-04-14
Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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A range of inhibitors were therefore synthesized containing
2020-04-14
A range of inhibitors were therefore synthesized containing either carboxylic ARP 100 or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Analysis of
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The study reported here had the primary goal to compare
2020-04-14
The study reported here had the primary goal to compare the methylation of HPV late genes with methylation of the DAPK promoter, and with histological or cytological diagnoses among high-risk patients that were referred to a colposcopy clinic based on abnormal cervical cytology. Based on the literat
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Ligand binding RTK activation induces the
2020-04-14
Ligand binding (RTK activation) induces the endocytic internalization of RTKs, and this has been demonstrated for CSF-1R [15], [16], [17]. Endocytosed RTKs are targeted to the lysosome, which we and others have established to be dependent on ubiquitination via CBL-family and recognition by ESCRT com
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Both anxiogenic and antinociceptive effects produced by
2020-04-14
Both anxiogenic and antinociceptive effects produced by CRF seem to be selective for the CRF1 receptor, since intra-dPAG microinjection of ASV 30, a CRF2 receptor antagonist, altered neither the anxiety nor the antinociception response. Intra-dPAG ASV 30 was also unable to prevent the anxiogenic (ob
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Models and theories The CPA equation of
2020-04-14
Models and theories The CPA equation of state is composed predominantly of two parts: physical item and the association item based on the thermodynamic perturbation theory [21], [22], [26], [27]. The physical item is used to represent intermolecular physical interaction, usually representing the SR
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Recent studies showed that the
2020-04-14
Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-
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In addition PK studies on indicate that it displays
2020-04-13
In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted
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Enzyme activity loss during the hydrolysis process has tradi
2020-04-13
Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important
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A growing body of data
2020-04-13
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream Thiamet G synthesis molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the c
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To predict levels of SCF assembly Liu
2020-04-13
To predict levels of SCF assembly, Liu et al. (2018) first quantified the remaining necessary kinetic parameters and derived a model in combination with known functions and concentrations of components. The model agrees astonishingly well with many experimental observables. In terms of SCF assembly,
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With a favorable spectrum of
2020-04-13
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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MTT results show that both pancreatic
2020-04-13
MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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Due to its several industrial applications the recombinant p
2020-04-13
Due to its several industrial applications, the recombinant production of collagen and all its derivatives as gelatins has been pursued for many years in different biological systems as mammalian Amikacin australia (Toman et al., 1999), tobacco plants (Ruggiero et al., 2000), silkworms (Tomita et a
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icrt Yu et al also reported that extracting consortium
2020-04-13
Yu et al. [24] also reported that extracting consortium of hydrolytic enzymes from sludge flocs performs better than costly single purified commercial enzyme. Thus, it is concluded from the above cited literature analysis that only few studies have been reported on extraction of enzymes from waste s
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