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In addition to the ESIs identified that
2019-08-13
In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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The all NTP pyrophosphatase and NUDIX families maintain
2019-08-13
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes
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Several single nucleotide polymorphisms SNPs in humans affec
2019-08-13
Several single nucleotide polymorphisms (SNPs) in humans affect CYP3A expression and activity (Lamba et al., 2002). The CYP3A4 SNP rs2740574 (also referred to as CYP3A4*1B, by The Human Cytochrome P450 (CYP) Allele Nomenclature Database, http://www.cypalleles.ki.se/) is a change in the promoter regi
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In this study we further
2019-08-13
In this study, we further investigated the involvement of CRF1 and CRF2 receptors of the dPAG in the regulation of panic-related responses. For this, we used two animal models that associate escape behavior with panic attacks: the elevated T maze and the electrical stimulation of the dPAG (for a ful
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br Introduction In addition to the canonical
2019-08-12
Introduction In addition to the canonical double stranded structure, DNA can form various higher order structures such as bulges, and various kinds of mismatches, triplexes, to the G-quadruplex (G4). Over the past decades, accumulating evidence has begun to emerge that these non-canonical structu
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Some pyrimidine analogs are substrate based inhibitors that
2019-08-12
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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In this study we investigated the role phenyl
2019-08-12
In this study we investigated the role 17-phenyl tinor (pt)-PGE2 on endothelial barrier function and the underlying molecular mechanism in HMVEC-Ls as well as in a murine model of LPS-induced acute pulmonary inflammation. We found that 17-pt-PGE2 concentration-dependently enhanced endothelial barrie
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SAR302503 Despite the differences in the clustering
2019-08-12
Despite the differences in the clustering abilities of DDR1b versus DDR2 upon ligand administration, we also noted striking similarities in the spatial distribution and phosphorylation of DDR1b-YFP and DDR2-GFP. We show for the first time that in MC3T3-E1 cells, after 4 h of collagen administration,
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br Results br Discussion CCA is a fatal
2019-08-12
Results Discussion CCA is a fatal tumor originating from the intrahepatic bile duct and the prognosis is very poor (Hoyos et al., 2018). CCA is one of the most dangerous primary liver malignant tumors and the most common malignant tumor of the biliary tract worldwide. However, the underlying m
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(-)-p-Bromotetramisole Oxalate A growing number of other pos
2019-08-12
A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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The identification of a gatekeeper mutation
2019-08-12
The identification of a gatekeeper sars-cov also suggests that alternative DDR2 inhibitors may be required to overcome acquired resistance. Additional DDR2 inhibitors that have been isolated include the recently identified alkaloid natural products discoipyrroles A-D and the chemotherapeutic Actino
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Some studies have been conducted on the activities http www
2019-08-12
Some studies have been conducted on the activities of CYP450 [[28], [29], [30], [31]]. For example, Chen et al. reported that low-dose aspirin induced the in vivo activity of CYP2C19 in healthy subjects [30], Krasniqi et al. reported that CYP2C8*3 and CYP2C9*2*3 variants correlated with ibuprofen-in
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It was recently reported that a functional single nucleotide
2019-08-12
It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid Isochlorogenic acid A 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an autosomal
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Moreover the vibrational contributions provide a plausible e
2019-08-12
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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Table gives the list of components
2019-08-12
Table 1 gives the list of components which will be modeled. Transient Voltage Suppressor (TVS) as well as passive elements will be also modeled. For each component, we will choose the EMC (emission and immunity) and transient immunity measurement method adapted to extract the component model. A com
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