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vorapaxar Most enzymes involved in the addition and removal
2020-06-17

Most vorapaxar involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 ligases (Ernst
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In normal cells the apoptotic stimuli lower the expression
2020-06-17

In normal cells, the apoptotic stimuli lower the expression level of antiapoptotic proteins by increasing turnover rate and preventing the constant degradation of proapoptotic proteins. Thus, the dysregulation of anti-/pro-apoptotic proteins will confer the survival of cancer thz1 via enhancing the
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It is currently believed that acute morphine
2020-06-17

It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ
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In this report we evaluate if
2020-06-17

In this report, we evaluate if this molecular mechanism is used universally by high-fidelity DNA polymerases during the replication of DNA lesions that are structurally distinct from abasic sites. This was approached by quantifying the kinetic parameters for the incorporation of modified and non-nat
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Our approach relied on measurement of
2020-06-16

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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Then the mechanisms responsible for BPA induced up regulatio
2020-06-16

Then the mechanisms responsible for BPA induced up regulation of ERRγ were further investigated. Recent studies indicated that Akt and MPAK can modulate the protein levels and transcriptional activities of ERRγ (Heckler et al., 2014, Sun et al., 2014). Previous studies also indicated that BPA can ac
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EC barrier dysfunction triggered by inflammatory mediators
2020-06-16

EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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Since the initial identification of
2020-06-16

Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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br Acknowledgments We thank Jon
2020-06-16

Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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Piperlongumine The CysLT receptor antagonist BayCysLT RA sig
2020-06-16

The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear Piperlongumine into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Barret e
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br Materials and methods br Results br Discussion Recently
2020-06-16

Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p
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To our knowledge this study is the
2020-06-16

To our knowledge, this study is the first to construct a whole-body transcriptome of D. variabilis. Most of the data currently accessible in NCBI are derived from a midgut EST database consisting of 1679 transcripts (Anderson et al., 2008) and about 20,000 mRNA sequences from the testis-vas deferens
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GDC-0994 NPC L NPC Niemann Pick C
2020-06-16

NPC1L1 (NPC1 [Niemann-Pick C-like-1]-like intracellular cholesterol transporter) is the rate-limiting transmembrane transporter for cholesterol GDC-0994 from the intestinal lumen, and it mediates the absorption of both dietary and biliary cholesterol., , NPC1L1 is the target of the cholesterol-lower
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Introduction Ewing sarcomas primitive neuroectodermal tumors
2020-06-15

Introduction Ewing sarcomas/primitive neuroectodermal tumors (ES/PNETs) are relatively infrequent but the second most common sarcoma of the bone next to osteosarcoma. Nearly 80% of them occur in persons younger than 20years. Most of them arise from the bone, but 10 to 20% of them from soft tissue.
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What does this mean for
2020-06-15

What does this mean for cancer therapy? We found that components of the de novo pyrimidine synthesis pathway rarely mutate in cancer, clearly showing its importance. In our experimental models, the pathway, including DHODH itself, was primed to respond when the block in CoQ redox-cycling was removed
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