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The in vitro cytotoxicity of the prodrugs was assessed in
2020-01-16
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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br Author contribution br Acknowledgements We
2020-01-15
Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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Most enzymes involved in the
2020-01-15
Most BVT 2733 synthesis involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 ligase
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Proof of concept studies with disulfiram
2020-01-15
Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d
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br Experimental Procedures DNA synthesis reagents were
2020-01-15
Experimental Procedures DNA synthesis reagents were purchased from Glen Research (Sterling, VA). A solution of 0.1 M triethylamine acetate (TEAA) (pH 6.5) was used as HPLC buffer A, and HPLC-grade acetonitrile from Oceanpak (Sweden) was used as HPLC buffer B. All other chemicals were obtained fro
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Organometallic compounds exhibited remarkable potential
2020-01-15
Organometallic compounds exhibited remarkable potential for the development of new cancer drugs not only due to the direct cytotoxicity but also to the drug targeting and active anticancer immune response ability [4]. Among the organometallic compounds, ferrocene is one of the most well-known compou
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br Results br Discussion Thus
2020-01-15
Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh
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Treatment related adverse events have been
2020-01-15
Treatment-related adverse events have been a serious issue in clinical application. Severe toxicity has been reported in clinical trials using antibody blockade of CSF-1R (20 mg/kg), PD-1, and CTLA-4.29, 30, 31 However, apparent side effects were not observed in our study with PLX3397 treatment alon
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Nevertheless of the different types of
2020-01-15
Nevertheless, of the different types of scoring systems so far proposed, each of these [14], [29], [30] considered some aspects that could describe the fibrotic evolution, though none provided a quantitative assessment. Calvaruso et al. [8] showed that CPA had a better histological correlation with
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A further quandary concerning rediscoveries arises in habita
2020-01-15
A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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However the Moon is not the
2020-01-15
However, the Moon is not the only possible source for space resources. Asteroids, in particular near-Earth asteroids (NEAs), can provide an alternative source for propellant and other materials, sometimes at lower cost. There are an expected 4000 NEAs that require less propellant (delta-V) per trip
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br Materials and methods br Results
2020-01-15
Materials and methods Results Discussion Persimmon tannin has been reported to have the bile acid binding ability in vitro (Matsumoto et al., 2011) and hypolipidaemic effects in animals (Matsumoto et al, 2008, Zou et al, 2012). Our previous study also proved that persimmon tannin promoted t
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Although further experiments are needed
2020-01-15
Although further experiments are needed to determine definitively whether D–ETB receptor heterodimers exist, for example, by using fluorescence resonance EDC.HCl transfer analysis or co-immunoprecipitation of receptors, the results of the study by Zeng and colleagues appear to indicate that D–ETB r
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In particular EphB has been one of the
2020-01-15
In particular, EphB4 has been one of the most studied receptor of the Eph family: inhibition of EphB4 expression using interfering-RNA or antisense oligonucleotides inhibited proliferation, survival and invasion of PC3 prostate cancer Ac-YVAD-CHO synthesis in vitro and in vivo. Inhibition of EphB4
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Among the down regulated genes were several
2020-01-15
Among the down-regulated genes were several of interest. Coronin2a (Coro2a), a component of the nuclear receptor co-repressor complexes, contributes to de-repression of inflammatory response genes (Huang et al., 2011). Mill1, an MHC family member expressed in hair follicles, represses wound healing
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