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br Conclusions When the authors joined the field of
2021-01-22
Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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LY2409881 Across the scaffold the platform
2021-01-22
Across the scaffold, the platform anchors the N terminus of the elongated cullin structure of APC2 [21]. This connects to the flexible cullin–RING catalytic core consisting of the C-terminal region of APC2 and the associated APC11 11, 12, 21. The flexibility and positions of the catalytic core are c
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Approximately of the etamicastat dose was recovered
2021-01-22
Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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Introduction Double strand break DSB is the most deleterious
2021-01-22
Introduction Double strand break (DSB) is the most deleterious damage that threats DNA integrity. This frequent damage arises from environmental stress like UV, chemical agents or ionizing radiations (IRs). Although environmental stress does not lead directly to DSB, it produces Altiratinib synthes
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Examination of Wnt signaling via for example complexes of fr
2021-01-21
Examination of Wnt signaling via, for example, complexes of frizzled (Fz) and lipoprotein-receptor-related protein (LRP) receptors has been hindered by difficulties in producing Wnt ligands due to their inherent hydrophobicity [20]. This bottleneck was recently bypassed by constructing highly solubl
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Each nsP plays a distinct defined and indispensable role
2021-01-21
Each nsP plays a distinct, defined and indispensable role in the replication of viral genome. nsP1 is a membrane associated protein which possesses S-adenosyl-L-methionine (SAM)-dependent methyltransferase (MTase) and guanylyltransferase (GTase) activities to catalyze the viral RNA capping reaction
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Cell lines which possess microglial or
2021-01-21
Cell lines which possess microglial or neuronal properties are uncomplicated and convenient in vitro models for studying pikfyve inhibitor injury at the cellular and molecular levels. Microglial BV-2 cells are derived from the immortalized mouse microglia and exhibit many of the morphological, phen
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To the best of our knowledge this
2021-01-21
To the best of our knowledge, this study was the first to demonstrate in vitro and in vivo that the lipolytic effect of kinsenoside results from coordination between PKA and AMPK pathways. We validated the lipolytic effect of kinsenoside in vivo and the effect of PKA activation on the modulating AMP
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The Czech Republic is a country
2021-01-21
The Czech Republic is a country with increasing CDI incidence (1.1 cases per 10,000 patient bed-days in 2008–4.4 cases in 2011–2012 and 6.2 cases per 10,000 patient bed-days in 2012–2013) (Bauer et al., 2011, Davies et al., 2014) and relatively high rates of antibiotic resistant C. difficile strains
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Sensory gating describes a filter mechanism protecting the c
2021-01-21
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits BS-181 HCl synthesis to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003)
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Temozolomide mg Another milestone in the field is the de
2021-01-21
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of Temozolomide mg , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways
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Repulsive interactions towards undesirable substrates are
2021-01-21
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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Covalent inhibitors are well suited for
2021-01-21
Covalent inhibitors are well suited for targeting the E1 PF 04418948 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in cir
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Given the structural similarity of BMAA to other amino
2021-01-20
Given the structural similarity of BMAA to other amino acids, our hypothesis was that N-nitrosation of BMAA might result in a toxic alkylating agent, providing a previously unrecognised mechanism for BMAA action. Materials and methods Results and discussion We first examined whether chemical
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Intriguingly our laboratory has shown
2021-01-20
Intriguingly, our laboratory has shown that the I638F kinase domain mutant, unlike the L63V and G505 mutants, is incapable of receptor autophosphorylation and activation of its downstream effector SHP-2 when exposed to collagen stimulation. These data indicate that I638F is a loss of function mutati
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