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Cabozantinib In addition PK studies on indicate that it
2020-04-09
In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted
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Most remarkably an essentially identical collagen
2020-04-09
Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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br Conclusions br ISG is an
2020-04-09
Conclusions ISG15 is an ubiquitin‐like protein that is induced by treating mammalian ACSF with interferon‐α/β. UbE1L was identified as the E1‐activating enzyme for ISG15 in the course of experiments that demonstrated that the nonstructural or NS1 protein of influenza B virus inhibits ISG15 con
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Main Text Post translational modifications by ubiquitin Ub
2020-04-09
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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Substituents at the C position An oxygen containing
2020-04-09
Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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A surprising second functional effect was found in
2020-04-09
A surprising second functional effect was found in culture experiments. Inclusion of LTD4 reduced the frequency of Fas receptor (CD95) expression. Once again, this effect, although modest, was reversed by a cysLT1 receptor antagonist. The biologic significance of this effect or its mechanism remaine
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Our comparison of all ER iso forms with
2020-04-08
Our comparison of all ERα (iso)forms with ERβ immunostaining suggests that overall ERβ expression is lower than that of ERα isoforms. This contrasts the so far reported data for ERs in the lung, but is not a paradox; in pathology routine, ER positivity is defined stricto senso by nuclear WT ERs. As
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ICT is a product of icariin via the metabolism of
2020-04-08
ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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We also observed reduced insulinotropic
2020-04-08
We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i
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br Introduction Although not fully understood
2020-04-07
Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen
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Some natural products such as curcumin resveratrol
2020-04-07
Some natural products, such as curcumin, resveratrol, and sulforaphane, are known to activate Nrf2 in both in vivo and in vitro experimental models where Nrf2-mediated gene nitric oxide plays a crucial protective role [8]. Under basal conditions, Nrf2 binds to Kelch-like ECH-associated protein 1 (K
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br Introduction Melatonin mainly originates from the pineal
2020-04-07
Introduction Melatonin mainly originates from the pineal gland (Reiter, 1991) and is well known for its physiological functions in the regulation of circadian rhythms (Cajochen et al., 2003) and as a potent free radical scavenger and broad-spectrum antioxidant in mammals (Paradies et al., 2010, T
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The nuclear receptor related protein Nurr NR A is a
2020-04-07
The nuclear receptor related-1 protein, Nurr1 (NR4A2), is a transcription factor that regulates the bcr-abl tyrosine kinase inhibitors of genes critical for the development, maintenance, and survival of dopaminergic neurons (Alavian et al., 2014, Decressac et al., 2013, Dong et al., 2016, Jankovic
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br Acknowledgments We thank Jon Clardy Juan
2020-04-07
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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The V V process of the FPGA development includes
2020-04-07
The V&V process of the FPGA development includes equivalence checking (Huang and Cheng, 1998, Huang et al., 2000, Kuehlmann and Krohm, 1997, Kuehlmann et al., 1995, Burch et al., 1994) as well as the simulation techniques. The equivalence checking can prove that two given designs have the same funct
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