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The in vitro cytotoxicity of the prodrugs was
2020-04-13
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., approximately
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In order to assess quantitatively the contribution of the un
2020-04-13
In order to assess quantitatively the contribution of the ung, dug and dut sr9011 to uracil-DNA accumulation in E. coli, we have developed a novel method for measuring uracil residues in DNA that is based on the approach of Kow and co-workers [33] for measuring AP-sites in DNA. The method, which we
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Several large scale clinical studies have set out with the
2020-04-13
Several large-scale clinical studies have set out with the common goal to further understand the cognitive impact of menopause and hormone therapies taken by women (Gleason et al., 2015, Greendale et al., 2011, Karlamangla et al., 2017, Rapp et al., 2003, Shumaker et al., 2003). Only one human study
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Most remarkably an essentially identical collagen
2020-04-13
Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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Herein the interactions of etamicastat nepicastat and
2020-04-13
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the XMD17-109 exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remain
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The V V process of the FPGA development
2020-04-13
The V&V process of the FPGA development includes equivalence checking (Huang and Cheng, 1998, Huang et al., 2000, Kuehlmann and Krohm, 1997, Kuehlmann et al., 1995, Burch et al., 1994) as well as the simulation techniques. The equivalence checking can prove that two given designs have the same funct
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Following the relationship model adopted in
2020-04-13
Following [20], [22], the relationship model adopted in this PRIMA-1 work to estimate the time to failure is the Inverse Power Law (IPL): Where L is the SUT life characteristic (e.g. the mean time to failure), s represents the stress level, while k and w are model-related parameters to be defined f
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br Cholesterol handling in the arterial wall cells
2020-04-13
Cholesterol handling in the arterial wall cells Foam cell formation in the arterial intima is a major hallmark of early-stage atherosclerotic lesions, which is attributed to uncontrolled uptake of modified lipoproteins, excess cholesterol esterification and impaired cholesterol release [44]. As a
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Ten non FH ADH probands
2020-04-13
Ten non-FH ADH probands fulfilled the diagnostic criteria of hyperabsorbers. Table 2 shows the main lipid characteristics of these subjects and of 10 non-hyperabsorber probands used for comparison. There were differences between groups in body mass index, waist circumference and triglycerides. Other
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Several CHK inhibitors have been reported in
2020-04-13
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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The intimate interactions between flavonoids and ER have bee
2020-04-13
The intimate interactions between flavonoids and ERα have been more extensively studied than their ERβ interactions because of the dominant role of ERα in some important diseases (Ye et al., 2018) including breast cancer (more than 80% of human breast cancers are ERα positive) (Turner et al., 2015),
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Although BPA has been proven to cause many health issues
2020-04-13
Although BPA has been proven to cause many health issues such as obesity and neurological toxicity (Rubin, 2011), the effects and mechanisms of BPA on the human tumorigenesis and cancer development are still not well illustrated. In the present study, we found that 10 to 10M BPA significantly promot
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br Effects of culture conditions on drug
2020-04-13
Effects of culture conditions on drug-induced gene Cy3 NHS ester receptor in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that ar
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We first confirmed LPS induction
2020-04-10
We first confirmed LPS-induction of markers known to induce NF-κB signaling in Caco2BB cells, as established for numerous other cell types [31]. We initially selected this approach to monitor NF-κB activation instead of directly monitoring p65 as it is technically straightforward and provides both u
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Abrahamson and coworkers recently demonstrated a distinct
2020-04-10
Abrahamson and coworkers (2009) recently demonstrated a distinct role of the podocyte in preservation and production of mature GBM-components such as α3/4/5(IV)-chains. This group further verified that collagen receptors (integrins) are linked to the TWS119 of podocytes. In accordance to this data,
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