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QSAR based on the D structures of ligands plays
2021-04-14
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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Besides degrading cholesterol the cholesterol degradation pa
2021-04-14
Besides degrading cholesterol, the cholesterol degradation pathway also offers a route to obtain useful starting materials for the production of steroid drugs and hormones. Indeed, steroids are among the most marketed pharmaceuticals with about 300 approved steroid drugs [15] and a worldwide market
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To date the role of CRF and CRF
2021-04-14
To date, the role of CRF and CRF1+ neurons within the amygdala in the expression of anxiety-like behavior and conditioned fear, and the place where these cell populations fit into the fear-related microcircuitry already identified in the CeA, have not been fully characterized. Recent evidence suppo
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Population genetic summary statistics for five super and sub
2021-04-14
Population genetic summary statistics for five super- and 26 sub-populations, including haplotype and diplotype frequencies (analogous to allele and genotype frequencies), observed (Ho) and expected (He) heterozygosities, pairwise genetic distances, and tests for detection of departures from Hardy W
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It is very important to decide what
2021-04-14
It is very important to decide what the best time of NIR laser irradiation is for the optimized PTT. So the best way is to monitor the biodistribution of the nanoparticles in various tissues (specially, in tumors) temporally and spatially after iv injection. Based on the combined functions of therap
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Compounds and possessed relatively low clogP
2021-04-14
Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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Several studies have demonstrated that
2021-04-13
Several studies have demonstrated that αSyn specifically associates with lipid rafts (Cole et al., 2002), raising the possibility that the perturbation of rafts can affect the aggregation and phosphorylation of αSyn (Fortin et al., 2004). Schneider et al. (2010) described the potential involvement o
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Historically covalent drugs have had great
2021-04-13
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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As the angular structure of compound
2021-04-13
As the angular structure of compound cannot be differentiated from the linear structure by H NMR spectroscopy, a NOESY NMR experiment was performed to unambiguously characterize the regioselectivity of the final compound. In the linear compound , a signature correlation between the proton of the t
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In the present study we
2021-04-13
In the present study, we implemented the dendritic RCA-induced formation of amplifying DNAzyme catalytic labels strategy for sensitive and accurate assay of MTase activity and the detection of DNA methylation. In comparison with the traditional RCA process, the proposed strategy achieved high amplif
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Previous studies from our lab looked at the effect
2021-04-13
Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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The most common adverse events in relation to udenafil
2021-04-13
The most common adverse events in relation to udenafil treatment are headache and facial flushing; other possible adverse events are febrile sensation, dyspepsia, and visual disturbances. No severe adverse event related to udenafil has been reported thus far. The adverse event rate recorded in the p
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br Methods br Results and discussion br Conclusions br Confl
2021-04-12
Methods Results and discussion Conclusions Conflict of interest Acknowledgment The research is supported by the National Natural Science Foundation of China (Grant No. U1603285). Overview of the MAPK pathway The mitogen-activated protein kinases (MAPK) pathway, often known as a ca
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Increased leukocyte trafficking and infiltration of the vasc
2021-04-12
Increased leukocyte trafficking and infiltration of the vascular wall are thought to provide a key stimulus for SMC activation and subsequent neointima formation in response to vascular injury [19], [20]. The essential trigger regulating the accumulation of leukocytes in the vessel wall is the upreg
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br Acknowledgements This study was financially supported
2021-04-12
Acknowledgements This study was financially supported by the National Special Research Programs for Non-Profit Trades (Agriculture) (Grant No. 201303045) and the Basic Foundation for Scientific Research of the State-level Public Welfare Institutes of China (Grant No. 2013JB10). Introduction L
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