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Given the potency enhancing effect of the butyl group this
2020-01-23
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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ROS generation is crucial for
2020-01-23
ROS generation is crucial for NETs release upon both physiological or pathogenic stimuli [16,30]. In our study, we further verified this conclusion by demonstrating that SRA stimulation by Poly I enhanced intracellular ROS levels while scavenging of ROS by anti-oxidant agents effectively abolished t
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br Experimental br Results and discussion br
2020-01-23
Experimental Results and discussion Conclusions The fungus Mucor circinelloides MUT44, previously shown to have ene-reductase activity [11], possesses ten genes coding for putative ene-reductases belonging to the Old Yellow Enzymes family. Since the reduction of CC double bonds is one of th
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br Experimental Procedure br Acknowledgment
2020-01-23
Experimental Procedure Acknowledgment This work was supported by Ministry of Education, Singapore (MoE Tier-2) grant (R-154-000-625-112) and R154-000-A72-114 (AcRF Tier 1 grant) respectively. We acknowledge the Advanced Photon Source Beamline 24-ID-C, Argonne National Laboratory, USA. D.N. is
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br Results br Discussion The ubiquitin system
2020-01-23
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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Historically covalent drugs have had great success e
2020-01-23
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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br Introduction Addiction to opioids
2020-01-23
Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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In contrast irinotecan has shown
2020-01-22
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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br Restenosis after angioplasty remains a remarkable challen
2020-01-22
Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle rho inhibitor (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migrate
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Organometallic compounds exhibited remarkable potential for
2020-01-22
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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If the unwanted objects detected by OpenComet
2020-01-22
If the unwanted objects detected by OpenComet are manually deleted, and then the DNA (%) in tail is computed, the performance of the present method can be compared more effectively. Therefore, performance of OpenComet is analysed in two ways as Approach 1 and Approach 2. Approach 1, considers the DN
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To understand more clearly how these activities are combined
2020-01-22
To understand more clearly how these activities are combined in the heterotrimeric enzyme and to understand more clearly how DNA alkylation might effect DNA helicase activity, we summarize the relevant features of the structure of RecBCD determined in the presence of DNA. The RecB and RecC subunits
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With regard to the DGATs we have found
2020-01-22
With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C.
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There is an increase in small fruit
2020-01-22
There is an increase in small fruit consumption especially berries in recently. Because small fruits are rich sources of both anthocyanins and phenolic compounds. These chemicals have been found in Vaccinium corymbosum in high levels. Research on small fruits is of vital importance for human nutriti
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DL-α-Hydroxyglutaric acid disodium salt synthesis Cancer has
2020-01-22
Cancer has been linked to both genetic and epigenetic changes. Epigenetic modifications, mainly DNA methylation at CpG dinucleotides, affect the regulation of gene transcription without altering the gene\'s sequence. Short sequences rich in CpG dinucleotides (i.e., CpG islands) are often found in th
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