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Molecular docking study of compound
2020-05-27
Molecular docking study of Lithocholic Acid sale was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and
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Plasminogen is composed of five N terminal kringle domains a
2020-05-26
Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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HOIP s ability to build linear Ub chains
2020-05-26
HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4
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Taken together these assays demonstrate that SUMOD positioni
2020-05-26
Taken together, these assays demonstrate that SUMOD positioning is essential for all E3 ligases but dispensable for E2 and S*E2 sumoylation reactions. Thus, we propose SUMOD positioning as a key criterion to describe the enzymatic function of SUMO E3 ligases that distinguishes them from other enhanc
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br E mediated E discharge E ligases simultaneously interact
2020-05-26
E3-mediated E2 discharge E3 ligases simultaneously interact with the substrate and the SUMOD charged E2 enzyme to catalyze the discharge of the thioester-bound SUMOD from the E2 to the substrate. E3 interaction with SUMOD via a SIM results in a closed conformation which is highly reactive and lea
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In the present study we
2020-05-26
In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma
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smad pathway Sp family protein has been regarded as
2020-05-26
Sp family protein has been regarded as the housekeeping gene and is ubiquitously expressed. Although Sp family expression is regulated with some stimuli [17], [20], the total Sp family protein levels are not changed in most cases, as observed in our present study (Fig. 4). Constitutive binding of th
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DGK is classified into the type II DGK subfamily
2020-05-26
DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a
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Inhibition of DHODH is reflected by an antiproliferative eff
2020-05-26
Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear Harringtonine mg (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few selected c
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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2020-05-26
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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br Anti inflammatory effects of MTX In addition to
2020-05-26
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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br Anti inflammatory effects of MTX In addition to
2020-05-26
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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Aspergillus nigerA niger is another filamentous fungus in wh
2020-05-26
Aspergillus nigerA. niger is another filamentous fungus, in which alternative dehydrogenases have been described. Filamentous fungi are a very important group of microorganisms that are used in industry (O’Donnell et al. 2011). Biotechnological production processes using these organisms are often hi
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One of the most frequent gene alterations in MM is
2020-05-26
One of the most frequent gene alterations in MM is methylation of the p15 and p16 genes in the 5′ upstream region. P15 and p16 proteins are calcifediol regulators involved in the inhibition of transition from G1 to S phase. Frequencies of p15 or p16 gene methylation up to 32% and 53%, respectively
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It has been reported that CysLT receptors negatively regulat
2020-05-26
It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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