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Main Text Post translational modifications by ubiquitin Ub a
2021-02-26
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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Ingested folate needs to be chemically modified in order
2021-02-25
Ingested folate needs to be chemically modified in order to become a one carbon donor for cell metabolism. Firstly, folate turns to dihydrofolic flap inhibitor (DHF), it is then converted into tetrahydrofolate (THF) by the dihydrofolate reductase enzyme (DHFR) and finally converted into N5, N10-met
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The compounds were ranked based on
2021-02-25
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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In order to gain further
2021-02-25
In order to gain further insights into the role of peptidases in B. xylophilus, four cysteine proteases highly secreted by B. xylophilus (Cardoso et al., 2016) were selected four further characterisation. Materials and methods Results and discussion Structural prediction and analysis The i
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CaneCPI showed strong inhibitory activity
2021-02-25
CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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In LPS treated BV cells we found that the upregulated
2021-02-25
In LPS-treated BV-2 cells, we found that the upregulated CysLT2R was translocated into the nucleus. The nuclear localization of CysLT2Rs in microglia has not been reported previously. It is known that CysLT1Rs in endothelial Triciribine synthesis translocated to the nucleus in a ligand-independent m
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Currently multiple clinical trials of CSF CSF R targeting ag
2021-02-25
Currently, multiple clinical trials of CSF-1/CSF-1R-targeting agents in combination with standard treatment modalities and immunotherapies are underway (Table 1). In particular, results for combinations with checkpoint blockade inhibitors and other immunotherapeutic approaches are eagerly awaited.
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Magnetic interactions between metal ions are
2021-02-25
Magnetic interactions between metal ions are usually described by superexchange via intermediate ligands. Although the general principles of the superexchange mechanism are essentially the same for d and f ions, calculations of exchange parameters for lanthanides are more difficult than for transiti
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reboxetine mg The underlying assumption of consolidation re
2021-02-25
The underlying assumption of consolidation/re-consolidation is that the reboxetine mg activity initiated during the acquisition trial/re-consolidation trial continues to persist briefly after completion of the trial and it is during this post-trial period that immediate post-trial treatments can inf
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In the horse oviduct the
2021-02-25
In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial Isoxsuprine hydrochloride particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely refl
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To develop antagonists selective for the mouse
2021-02-25
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic Sulindac sulfone () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable ald
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br Conflict of interest br Acknowledgements
2021-02-25
Conflict of interest Acknowledgements This work was supported by the Basic Science Research Program through the National Research Foundation (NRF) funded by the Ministry of Science, ICT & Future Planning (2013R1A1A1076117) and also by the Priority Research Centers Program through the NRF funde
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Due to the high attractiveness of E and E ligases
2021-02-25
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), GDC-0834 (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2005, Marb
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br Conflict of interest br Acknowledgements The authors are
2021-02-25
Conflict of interest Acknowledgements The authors are grateful to laboratory technician Kristina Andersson for expert technical assistance. The authors acknowledge the Swedish Research Council (Grant no. 6834), Region Skåne and Faculty of Medicine, Lund University, for financial support. In
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br DAG kinase activity is confined to specific cell
2021-02-25
DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden
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