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At this stage it is still difficult
2021-08-02
At this stage it is still difficult to assign specific domains to some of the regions observed in these structures, although some attempts have already been made (Brewerton et al., 2004). Clearly, higher resolution data is needed. In the future, even if an atomic structure of DNA-PKcs is determined,
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A range of therapies exists for the treatment
2021-08-02
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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Introduction Cyclin dependent kinases CDKs are a family of
2021-08-02
Introduction Cyclin dependent kinases (CDKs) are a family of proline-directed serine/threonine kinases with roles in regulation of crucial cellular processes such as smo inhibitor and transcription [1]. One of the unifying features of this family is its dependence on association with cyclins/cycli
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We analyzed whether HaCaT cells treated with PLD
2021-08-02
We analyzed whether HaCaT Voreloxin treated with PLD can alter the expression of genes involved in DNA damage response. Key DNA damage cues activate the sensory DNA-PK/ATM/ATR kinases, which relay two parallel cascades that ultimately serve to inactivate the Cyclin B-cdc2 complex. The protein kinas
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In summary A is a
2021-08-02
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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Before addressing point by point the
2021-08-02
Before addressing point-by-point the aforementioned topics in separate sub-sections it should be remarked that the strength of recommendations provided by guidelines is graded in three classes: I (evidence and/or general agreement that a given treatment or procedure is beneficial, useful,effective),
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Among RAS mutant tumors analyzed we
2021-08-02
Among RAS mutant tumors analyzed, we found that the efficacy of either the SHP2 inhibitor SHP099, or combined MEK and SHP2 inhibition was best in those expressing RAS mutations at G12 (Figure 7B). Recent studies revealed that cellular RAS(G12C) activity depends on RTK-mediated nucleotide exchange,
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The effect of transformation of the linker
2021-08-02
The effect of transformation of the linker Y between the carboxylic vorapaxar residue and the phenyl moiety of 2b was also investigated, and is illustrated in Table 5. Analogs 2b, 16, and 17, possessing conformationally restricted carboxylic acid residues, tended to show stronger antagonist activit
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Enzyme activity loss during the hydrolysis process
2021-08-02
Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important
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br Substrate characterization of candidate peptide
2021-08-02
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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br Acknowledgements br Introduction Endothelial
2021-07-31
Acknowledgements Introduction Endothelial Bisindolylmaleimide VIII acetate constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) play
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While we previously demonstrated that TraG is
2021-07-31
While we previously demonstrated that TraG is inhibited by specific transglycosylase inhibitors and that enzymatic activity is strongly reduced upon mutation of the potential catalytic core (Arends et al., 2013), the enzymatic mechanism of both domains was not assigned. Here, by mass spectrometry an
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The imbalance that renders greater lipid
2021-07-31
The imbalance that renders greater lipid uptake toxic is unclear, but the comparison of our in vitro studies with those in mice illustrates the importance of TAG storage versus accumulation of less non-polar molecules. Protective effects of ACSL1 and PPARγ have been reported in other cell types. Par
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One of the isolated interactors
2021-07-31
One of the isolated interactors against Mulan259–352–Ube2E3 fusion bait was found to be the GABARAP protein, a known member of the Atg8 family that includes LC3 [20]. The Atg8 family-of-proteins are major players in autophagy/mitophagy since they are part of the autophagosome [20], [21], [22]. Our s
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Compounds that interact with MDR
2021-07-31
Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant IFN-gamma, murine recombinant and there was
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