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Recent studies have also uncovered additional
2020-05-25

Recent studies have also uncovered additional roles for E2 enzymes and E2~Ub conjugates in modulating the activity of deubiquitinating enzymes (DUBs), such as OTUB1 (Juang et al., 2012, Wiener et al., 2013, Wiener et al., 2012). Interestingly, OTUB1 has also been shown to associate and modulate the
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E3330 In light of the overall loss of
2020-05-22

In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. Th
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br Results br Discussion C
2020-05-22

Results Discussion C4 is related to another VACV protein, C16, and the C-terminal domain of C16 also inhibits DNA-PK-mediated DNA sensing via the same mechanism and to a similar level as C4. Moreover, mutagenesis of C16 at the CYC residues equivalent to those in C4 abrogated the C16-Ku interac
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Several authors have been pursuing the aim of finding good
2020-05-22

Several authors have been pursuing the aim of finding good performing organic solvent compatible adsorbers useful in the context of API purification [[10], [11], [12], [13], 22, 23]. For sulfonate GTIs, scavenging nucleophilic resins [22, 23] or molecular imprinted polymers (MIPs) [10] have been exp
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The following is the supplementary data related
2020-05-22

The following is the supplementary data related to this article. Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) to produce phosphatidic 4-DAMP (PA) (Baldanzi, 2014, Goto et al., 2006, Merida et al., 2008, Sakane et al., 2007, Topham and Epand, 2009). To date, ten ma
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WRTs AI AI and AI showed the
2020-05-22

WRTs AI-82/1, AI-9-1 and AI-60 showed the same ST as was published by Dingle et al. in RTS 103, 013 and 097 (Dingle et al., 2011). WRTs 015 and 002 were assigned as WRTs 015-like and 002-like due to slight changes in their CE-ribotyping profiles; however, the ST of WRT 002-like (ST8) was identical t
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br Discussion Nowadays data of uncommon EGFR mutations
2020-05-22

Discussion Nowadays, data of uncommon EGFR mutations are limited, considering that patients carrying these rare alterations are usually excluded from clinical trials. Available survival data of activity of EGFR TKIs on this class of mutations, coming from a small number of usually retrospective s
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br Materials and methods br Results Metabolic
2020-05-22

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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Deregulated Wnt signaling either due to pathway
2020-05-22

Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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br Discussion Our data demonstrate that the bicyclam AMD str
2020-05-22

Discussion Our data demonstrate that the bicyclam AMD3100 strongly interacts with CXCR-4, whereas DS and AR177, two other compounds that also interfere with virus entry into the Gefitinib (and interfere with virus binding), do not. AMD3100 is a unique compound in that it interferes with the chem
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br Pre clinical combination studies using CSF
2020-05-22

Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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In the PTEN loss mouse model
2020-05-21

In the PTEN loss mouse model, deletion of ATG7 gene not only caused an autophagy-deficient phenotype, but also postponed the progression of inoculated prostate tumor [22]. On the basis of these experimental facts, these ATG7 and PTEN related genes were then compared with the 3020 BCR-associated gene
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Introduction It has been well stablished the
2020-05-21

Introduction It has been well stablished the role of CRF in somatic pain regulation (Yarushkina et al., 2011, Yarushkina et al., 2016). However, the effects of CRF in pain relief are controversial and it has been described anti- and pronociceptive effects (Ji et al., 1995, Larauche et al., 2009, Ni
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Our approach relied on measurement of bulk solute diffusivit
2020-05-21

Our approach relied on measurement of bulk solute diffusivity in the three tissue types of interest. Our diffusivity values (Table 3) are on the order of 10−6 cm2/s and are comparable to the PG diffusion coefficient in water at infinite dilution, which is about 10−5 cm2/s at room temperature, as wel
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Moreover the vibrational contributions provide
2020-05-21

Moreover, the vibrational contributions provide a plausible explanation for the missing X′ peaks in the experimental PES for the Er and Tm complexes. The current SO-MCQDPT2 (Fig. 1(k) and (l)) and MCQDPT2 II (Fig. 2(k) and (l)) calculations suggest the appearance of peak splittings for these complex
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