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Another important new result that has
2019-11-29
Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f
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br A brief history of
2019-11-29
A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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ON-01910 Intriguingly one E residue may serve as a molecular
2019-11-29
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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WES and validation by Sanger sequencing in PNGS
2019-11-29
WES and validation by Sanger sequencing in PNGS-252 revealed an apparent homozygous c.4C>G missense alteration (GenBank: NM_014176.3), resulting in the amino 3254 substitution p.Gln2Glu (Figure 1A). This mutation must be very rare, because this is not listed in the NHLBI Exome Sequencing Project or
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lxr agonist A An optimized BEI SEIscore based on
2019-11-29
(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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In contrast DGAT does not interact
2019-11-29
In contrast, DGAT1 does not interact with mitochondria and LDs but can form dimers and tetramers [76]. It has been reported that the hydrophilic N-terminal region of DGAT1, which is not required for acyltransferase activity, has the roles in regulating enzyme activity and the formation of dimers and
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G007-LK Apart from its high affinity the selection of GW
2019-11-29
Apart from its high affinity, the selection of GW2580 as G007-LK lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensive
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As shown in Figs a
2019-11-29
As shown in Figs. 3(a) and (b), with the SO effect, the absolute values of the VDEs change by at most 0.19eV. Table 1 also shows that the observed peak splitting energies in the Sm-Ho complexes were reproduced even without the SO effect. Considering its significant importance in the electronic struc
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Since the aggregation of neurotoxic forms of A
2019-11-29
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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In a recent report Yoshihara
2019-11-29
In a recent report, Yoshihara and colleagues (2016) used transcriptomes derived from freshly isolated islets of 2-week-old neonatal, 6-week-old young adult, or 12-week-old adult mice to interrogate how maturation is regulated to acquire glucose responsiveness. The authors observed that estrogen-rela
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In conclusion we designed novel E inhibitors based on the
2019-11-29
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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br Materials and methods br
2019-11-29
Materials and methods Results Discussion The nitric oxide generating enzymes of the NOS family comprise three isoforms: nNOS, iNOS and eNOS [31]. Expression of eNOS is mainly found in endothelial b-AP15 where it physically promotes vasodilation [32]. Conversely, evidence also indicates tha
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It was demonstrated that ET signaling is
2019-11-29
It was demonstrated that ET-1 signaling is the primary axon guidance mechanism that accounts for sympathetic innervation of the sinoatrial node and myocardium in the developing mouse heart [11]. In this article, we will review the findings relating to the basic profiles; i.e. molecular features of
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br Funding br Disclosure of
2019-11-29
Funding Disclosure of interest Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic disease characterized by extensive deposits of the extracellular matrix (ECM) that can impair the architecture and function of the lungs (Cavazza et al., 2010). Imbalance between the prolifer
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MTT results show that both pancreatic cell lines were
2019-11-28
MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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