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Another potential source of variable affinities is inherent
2020-02-10
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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br Methods br Discussion In
2020-02-10
Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of cudc 907 level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard treatment options
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br Materials and methods br Results
2020-02-10
Materials and methods Results Discussion Schistosome cercarial elastase secreted from the acetabular glands of cercariae is recognized to play a critical role in mammalian host skin penetration upon infection. The present study extends the understanding of biochemical and immunological prop
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br Rationale and hypothesis To discover an allosteric
2020-02-10
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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br Significance Our understanding of the ubiquitin biology
2020-02-10
Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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There was a good alignment profile
2020-02-10
There was a good alignment profile between compound 26 (IC50 0.06μM) and MTX (IC50 0.08μM) explaining its activity pattern (Fig. 5a). Fig. 5b clearly indicates a different alignment profiles where carbonyl groups are not on the same side between 25 (IC50>100.0μM) and MTX which is in consistency with
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In order to derive a better understanding of
2020-02-10
In order to derive a better understanding of the results from our SAR study, we utilized Glide to model the binding of the SAR compounds with the non-active site pocket of TS-DHFR shown in C. The majority of models position the phenolic moiety of these compounds within the non-active site pocket, wh
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To date methods for the simultaneous analysis
2020-02-10
To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analys
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Ultimately we decided to investigate the role of
2020-02-10
Ultimately, we decided to investigate the role of Cyp3a in obesity because Hepatic P450 Reductase-null (HRN) mice with no P450 activity show hepatic steatosis with increased Cyp2b10 and Cyp3a11 expression, perturbations in liver size, lipid homeostasis, and increased liver polyunsaturated fatty acid
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Eukaryotic cell cycle machinery is
2020-02-10
Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me
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It has long been known that
2020-02-08
It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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The use of recombinant ER and ER binding
2020-02-08
The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct bgj398 receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein production system used to
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While a growing body of knowledge demonstrates the
2020-02-08
While a growing body of knowledge demonstrates the importance of COX-1 and COX-2 accompanied with neuroinflammation in altitude related conditions. In fact, PGE2 has been widely thought to promote the neuronal inflammation and degeneration in many neurological maladies (Griffin et al., 2013, Jiang a
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The distorted geography on the number
2020-02-08
The distorted geography on the number lines of many pre-service primary teachers in this study also highlights the need to provide them with strong visual models of negative numbers and their ordering. The evidence from Indri\'s interview is that some standard models of negative numbers (e.g., lendi
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On top of the hardware ASTS
2020-02-08
On top of the hardware, ASTS employs Linux SUSE with High-Availability (HA) Extension: a COTS OS provided with two clustering software (Pacemaker Cluster Resource Manager (CRM) and Corosync) responsible for resources orchestration, failure diagnosis, nodes coordination, and fail-over management. The
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