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The synthesis of compounds a
2021-01-29
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of Moxidectin 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were o
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N acetylation by N acetyltransferase NAT is an important
2021-01-29
N-acetylation by N-acetyltransferase (NAT) is an important metabolic pathway for some substances, and there are 2 functional NAT isoforms in humans—NAT1 and NAT2. Studies of etamicastat in healthy subjects showed an extensive N-acetylation of etamicastat to the inactive metabolite BIA 5-961, and a l
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Previous synthetic lethal screening efforts Cox et
2021-01-29
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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br Disclosures br Introduction The presence of anti
2021-01-28
Disclosures Introduction The presence of anti-viral T-cell immunity is crucial for effective and sustained protection against Cytomegalovirus (CMV) following allogeneic stem cell transplantation (alloSCT) [1]. In vitro and in vivo T-cell depletion (TCD) via addition of the anti-CD52 monoclonal
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AON successfully alleviated the myotonic phenotype in DM
2021-01-28
AON successfully alleviated the myotonic phenotype in DM model mice [18], [23]. To screen for an optimal AON sequence, we used 25-mer phosphorothioate 2′ O-methyl RNA molecules that covered the exon 6B or exon 7A. Unexpectedly, AON 7A (+63−8) which covers the boundary of intron 7A and exon 7A enhanc
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EP EP and EP receptor expression on HMVEC L was
2021-01-28
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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The ultrafiltration approach has been used to
2021-01-28
The ultrafiltration approach has been used to measure equilibrium BIEs for a number of enzyme systems, including BCA Protein Quantitation Kit hexokinase (Lewis and Schramm, 2003a, Lewis and Schramm, 2003b), thymidine phosphorylase (Birck & Schramm, 2004), purine nucleoside phosphorylase (Murkin, Ty
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BS-181 Nimodipine is an L type calcium channel
2021-01-28
Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si
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A recent study revealed that in human glioma
2021-01-28
A recent study revealed that in human glioma cells, DNA-PKcs interacted with the regulatory γ subunit of AMPK and positively regulated AMPK phosphorylation and activation under glucose-deprived conditions. This suggested that DNA-PK is an important regulator of AMPK activation in response to energy
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Besides chemopreventive effects against oxidative DNA damage
2021-01-28
Besides chemopreventive effects against oxidative DNA damage we evaluated the protective effects of the three Hypericum sp. and isolated compounds against alkylating DNA damage induced by MMS in HT29 cells. Human exposure to alkylating agents, from different sources, occurs in a continuous way and i
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br Conflict of interest br Acknowledgements This
2021-01-28
Conflict of interest Acknowledgements This work was supported by the Biotechnology Research Center, China Three Gorges University, Yichang, China (No. 2016KBC05), the National Natural Science Foundation of China (No. 31370600 and 31300508), the Zhejiang Science and Technology Major Program on
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br Materials and methods br Results br Discussion We confirm
2021-01-28
Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc
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The inhibition of FAS by C produces an accumulation of
2021-01-27
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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Within the cluster of North African populations the Sousse
2021-01-27
Within the cluster of North African populations the Sousse population sample is somewhat different from the other six populations. One has to analyze more in depth the reasons of this isolation that has been shown by other genetic studies (Fadhlaoui-Zid et al., 2015). It seems that the particular ge
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To avoid the difficulty of the nonsmooth
2021-01-27
To avoid the difficulty of the nonsmooth constraints, a sequence of smooth problems by using smoothing functions have been progressively approximated this nonsmooth problem. To date, there have been many smoothing functions, such as perturbed Fischer–Burmeister (FB), Chen–Harker–Kanzow–Smale (CHKS),
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