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QSAR based on the D structures of ligands plays
2021-01-19

QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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br Results and discussion br Conclusion
2021-01-19

Results and discussion Conclusion A new series of 2-mercapto-quinazolin-4-one analogues is designed and synthesized to possess electron withdrawing or donating functional groups (Cl or CH3O) at position 6- or 7-, 4-methoxyphenyl function at position 3. The 2-mercapto function is used to connec
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br Materials and methods br Results br Discussion In general
2021-01-19

Materials and methods Results Discussion In general, CI symptoms are often visible only after the chilled products have been removed from coolstore to a warmer temperature (Schirra and Cohen, 1999). However, in the present work, 'satsuma’ mandarin fruit stored at 2°C showed chilling symptom
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DMOG synthesis Ligand binding RTK activation induces the end
2021-01-19

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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The in vitro cytotoxicity of the prodrugs
2021-01-19

The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximatel
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The effect of the simple dopaminergic tonic phasic model on
2021-01-19

The effect of the simple dopaminergic tonic/phasic model on cognitive processing has been investigated by a few studies (Nolan et al., 2004; Rosa et al., 2010). Rosa et al. (2010), using a Stroop task that requires different levels of cognitive flexibility and stability, observed an association betw
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In mouse lung arsenite enhances the formation of cigarette
2021-01-19

In mouse lung, arsenite enhances the formation of cigarette smoke-induced 8-oxodeoxyguanine (Hays et al., 2006) and BaP-induced DNA adducts (Evans et al., 2004). Moreover, arsenite inhibits the repair of BaP-induced DNA adducts in human lung carcinoma A549 Canagliflozin (Schwerdtle et al., 2003), i
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Our finding that VEGF A induced downregulation of
2021-01-19

Our finding that VEGF-A induced downregulation of EphB4 is VEGFR2 dependent (Fig. 4A) is not surprising because VEGFR2 is the primary signaling receptor of VEGF-A in EC [34]. However, our finding that VEGF-A induced upregulation of dll4 Spermine NONOate is not inhibited by VEGFR2 inhibition suggest
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Parecoxib Sodium Given the molecular pharmacology and in vit
2021-01-19

Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma
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Enzyme mimics belong to a type of rising catalysts which
2021-01-19

Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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br Summary and perspectives In
2021-01-19

Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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Since the dideoxy analogues and
2021-01-19

Since the 1,2-dideoxy analogues, and , served as substrates for TgTCEA and TgTCEB, respectively, with the higher affinity (lower ) and lower turnover number (lower ) than their authentic substrates, PosA and PosB (such trend was more evident on analogue for TgTCEB than on analog for TgTCEA), an i
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In general we observed that the enolase gene
2021-01-19

In general, we observed that the enolase gene with highest mRNA levels was TVAG_043500, under all three iron concentration conditions. mRNA levels for this gene are very similar in normal and iron rich cultures (73.9 and 78.1 fold change, respectively), and higher in iron depleted cultures (118.3 fo
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In our study the TIP P model is
2021-01-19

In our study, the TIP3P model is applied for water, AMBER99sb force field [24] is used to describe three types of EGFR, including the wild type (PDB: 2ITY) [25], its mutant G719S (PDB: 2ITO) [25] and mutant T790M (PDB: 3IKA) [26]. The force field of Tubemoside molecule is parameterized with optimize
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Recent results from our group found that SPMs not
2021-01-19

Recent results from our group found that SPMs, not only play a part in terminating inflammation, but also have a physiological role in conjunctival goblet bay 41 to maintain ocular surface health in the absence of disease. Amongst the SPMs that are effective in the conjunctiva are resolvin D1 (RvD1
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