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The first hint that GLP might
2021-08-16

The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the
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We recently described the benzoxazin one
2021-08-16

We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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Cdc which is involved in filopodium formation
2021-08-16

Cdc42, which is involved in filopodium formation, and Rac1, which is involved in lamellipodium formation, engage in cross-talk with one another [25,26,30,31]. In general, filopodium formation precedes lamellipodium formation, and filopodium formation (Cdc42 activity) suppresses lamellipodium formati
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orbifloxacin synthesis br Conclusion CSF R may contribute to
2021-08-14

Conclusion CSF-1R may contribute to limitation of targeted therapies by providing EGFR-bypassing signals that support proliferation. Multi-kinase inhibitors such as cabozantinib are available, and agents targeting CSF-1R are in clinical trials, however, at present, as inhibitors of tumor-associat
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The on target in vitro pharmacology of was
2021-08-14

The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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In this study we observed alterations in mRNA levels of
2021-08-14

In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased Trigonelline when the sensitization condition was established. Similarly, CRF2 receptor incr
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The anticholinesterase activities of all
2021-08-14

The anticholinesterase activities of all subfractions derived from EtOAc extract were detected and summarized in . Fraction 5 and its resulting subfractions (5B, 5C, 5D, 5C3, 5C4, 5D3, and 5D4) were found to show attractive activities. Subsequently, ten compounds (–) were obtained from these active
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br Experimental Procedures br Author Contributions
2021-08-14

Experimental Procedures Author Contributions M.M. and M.T. designed and supervised the study. S.I. conducted the analysis on NOG-rd mice. H.-Y.T., M.F., and T.M. conducted and analyzed MEA. S.I., H.-Y.T., and M.M. performed 3D image analysis. N.K., T.K., M.G., and R.T. planned and established
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It remains unclear how LINE RNA Nucleolin Kap are
2021-08-14

It remains unclear how LINE1 RNA-Nucleolin-Kap1 are targeted to the Dux cluster. LINE1-Nucleolin-Kap1 may have other interacting partners with DNA binding specificity. For example, YY1 has been implicated in targeting a repressive complex containing Nucleolin to the human DUX4 cluster (Gabellini et
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monensin Omar Farha and coworkers have
2021-08-14

Omar Farha and coworkers have recently successfully employed metal-organic frameworks (MOFs) to tackle these limitations while retaining the essential characteristics of an immobilization material. MOFs consist of metal ions, or small clusters thereof, coordinated with organic ligands. MOFs are high
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The prospects of the use of this novel
2021-08-14

The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to NMS-E973 synthesis through the endosomal compartment [47] or through non-endocytotic pathways [48],
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Glycolysis is important to maintain the vital functions of T
2021-08-14

Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its NMS-1286937 metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress from host ce
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The activity of cysteine endopeptidases involved in
2021-08-14

The activity of cysteine endopeptidases involved in the germination of caryopses is generally regulated at two levels: the hormonal induction of synthesis by gibberellins (Drzymała et al., 2008) and a putative regulation of activity by phytocystatines (Kiyosaki et al., 2007, Martinez et al., 2009),
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The HEV vaccine developed based
2021-08-13

The HEV vaccine, developed based on p239 particles, is of good efficacy, immunogenicity and safety, and was licensed in China in 2012. p239 (aa 368–606) and E2 (aa 394–606) share a common region of ORF2, referred to as E2s (aa 459–606), which harbors the major antigenic determinants of the HEV vacci
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The first example of a broadly acting antiviral
2021-08-13

The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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