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br Results br Discussion Our UbV
2021-07-26
Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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The molecular docking data supported the potential interacti
2021-07-26
The molecular docking data supported the potential interaction of lapachol and the synthetic naphthoquinonolyl compounds with the PfDHODH enzyme as the putative mechanism of action and the inhibition of parasite growth in vitro. In general, compounds fit well into the binding pocket of PfDHODH, the
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br Conclusions This report describes the discovery
2021-07-26
Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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Keratin K has been identified
2021-07-26
Keratin 8 (K8) has been identified as the first intermediate filament expressed during development in amphibians and mammals. In zebrafish, a type II cytokeratin 8 (zf-K8) cDNA has been cloned. zf-K8 gene was maternally inherited and expressed in all surface cells throughout the embryonic stages old
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Functionally all members of the IL family
2021-07-26
Functionally, all members of the IL-12 family have been annotated along major inflammatory signaling axes but their roles have often weighed on opposing sides of the immunological balance. For instance, IL-12 and IL-23 are classified as pro-inflammatory cytokines [10] as opposed to the rather protec
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Cystatins are potent inhibitors of cysteine proteases from
2021-07-26
Cystatins are potent inhibitors of cysteine proteases from the C1A family. These inhibitors primarily reduce the activities of cathepsin L-like proteases, although high concentration of barley cystatin hampers the degradation of storage proteins caused by cathepsin F-like protein (HvPap-1) (Cambra e
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The protein levels of the three enzymes in
2021-07-26
The protein levels of the three enzymes in the organs in the three earthworm species ranked body wall > intestine > seminal receptacle ≈ seminal vesicle (Fig. 3B).The presence of significant detoxification capability in the body wall would be logically expected in a soil dwelling organism, to facil
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Currently no evidence supports pathogenic variants in exons
2021-07-26
Currently, no evidence supports pathogenic variants in exons 20, 21, and 22, which are part of transcript isoform hCDKL5_5, or within exon 17, which is part of transcript isoform hCDKL5_2. The pathogenicity of variants in the 5′ untranslated region remain uncertain except for deletions extending to
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Common to all models for nuclear transport is
2021-07-26
Common to all models for nuclear transport is the binding of importins/exportins to FG repeats found in about a third of the ∼30 nucleoporins, the so-called FG-Nups (Iovine et al., 1995, Rexach and Blobel, 1995); for review, see Grossman et al. (2012), Stewart (2007), and Terry and Wente (2009). FG-
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In order to validate the ATP
2021-07-23
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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More recently it was discovered that BChE
2021-07-23
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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Other studies have investigated the role of HDAC inhibitors
2021-07-23
Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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Only a few studies have examined the effect of
2021-07-23
Only a few studies have examined the effect of prostanoids on cardiac fibroblasts. Therefore, this study examines the effect of PGE2 on cardiac fibroblast proliferation and tests the hypothesis that PGE2 causes cardiac fibroblast proliferation via alterations of cox inhibitor regulatory molecules a
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The dihydroxynaphthalene derived substrates a
2021-07-23
The 2,3-dihydroxynaphthalene-derived substrates 18a, 20a and 22a (Table 2) allowed only moderate growth of all members of the panel of microorganisms suggesting that these substrates were inhibitory to some extent. Strong growth of the Gram-negative microorganisms and moderate growth of the Gram-pos
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br Funding This work was
2021-07-23
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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