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A key inciting event in atherosclerosis is the deposition
2020-04-13

A key inciting event in atherosclerosis is the deposition of circulating low-density lipoprotein (LDL) in the subendothelial space of major arteries. In the subendothelium, native LDL is no longer protected by circulating antioxidants and is oxidatively modified to oxidized LDL (OxLDL) [5]. OxLDL is
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As part of a program to explore the
2020-04-13

As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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Substituents at the C position An oxygen containing substitu
2020-04-13

Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-04-13

Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead tyrosine kinase receptor 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the
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28170 In this study new and more extended tables of
2020-04-13

In this study, new and more extended tables of parameters were estimated for pure fluids and binary mixtures that are relevant to biodiesel systems. Also, calculations for glyceride systems will be shown, which is a topic not investigated before with the CPA model. As before [21], [22], [23], [24],
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The performance of the qCPA approaches is
2020-04-13

The performance of the qCPA approaches is similar with regards to the derivative properties of CO2 and for mixtures of CO2+self-associating compounds. For CO2+n-alkanes the four-parameter versions of qCPA both perform somewhat better than the three-parameter version. Nevertheless this modest improve
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Functional studies revealed that these ESR mutations
2020-04-13

Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea
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br Molecular genetics Based on the
2020-04-13

Molecular genetics Based on the genetic mutations associated with their development, sarcomas are subdivided into two distinct classes. One class is composed of tumors bearing complex karyotypic abnormalities with no particular pattern. The second class, which includes Ewing sarcoma, encompasses
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The optimization of the lead compound was
2020-04-13

The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Annexin V-Cy3 Apoptosis Kit Plus moiety with other functional groups led to loss of functional activity
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Dehydroandrographolide mg Multiple protein species are known
2020-04-13

Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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In the phase I AURA trial patients with
2020-04-10

In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for Evans Blue tetrasodium salt 19 deletion
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br Conclusions This study showed that in EOC
2020-04-10

Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC fexofenadine hydrochloride with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed a
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Cysteine protease inhibitors representing several chemical s
2020-04-10

Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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In a cell based functional assay the
2020-04-10

In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC
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To determine the time course
2020-04-10

To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour Chlorpropamide were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, suggesting th
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