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Moreover our results indicate that ADP is by far a
2024-02-19
Moreover, our results indicate that ADP is by far a better phosphate donor than AMP (Table 2). Yet, the bindings of AMP and ATP are mutually exclusive, whereas the bindings of ADP and ATP are additive (Fig. 7). The multiplicity of the phosphate donors in the TgAK reaction (Tables 1 & 2), suggests th
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Encouraged by this observation a
2024-02-19
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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PD0325901 The knowledge on the structure
2024-02-19
The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig
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br Viral manipulation of host factors to oppose anti viral
2024-02-19
Viral manipulation of host factors to oppose anti-viral autophagy To escape or manipulate autophagy, some viruses developed strategies that are based on the recruitment of host-cell endogenous factors. The non-enveloped double-stranded DNA virus adenovirus is rapidly endocytosed after attachment.
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Having taken a step back from
2024-02-19
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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Finally the comparison between data obtained by antioxidant
2024-02-19
Finally, the comparison between data obtained by antioxidant assays in in vitro cultured cells [11], [12] and in liposomes has disclosed the possibility to choose more confidently “the better phenolipid” of a series of fatty acids esters antioxidant derivatives. Looking at the physical parameters th
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br Introduction The development and plasticity
2024-02-18
Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo
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The mechanisms that control Ahr transcription are
2024-02-18
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic rvx receptor (RAR)-related orphan receptor γt] based on ChIP-Seq analyses
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In contrast to the beneficial treatment of skin inflammation
2024-02-18
In contrast to the beneficial treatment of skin-inflammation with PAH containing coal tar, epidemiology showed that environmental pollution, containing AHR-activating PAH, lead to more eczema [80]. Of note, other epidemiological data suggested that Th17 cell polarization may be enhanced air pollutio
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However there are a lot of external
2024-02-18
However, there are a lot of external magnetic field disturbances in urban environments, for example when the AHRS is close to a ferrous or magnetic object, which will disturb the output of magnetometer, then the observational errors cannot satisfy the assumption of Kalman filtering, and so, the atti
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To examine whether the interaction between mGlu and adrenerg
2024-02-18
To examine whether the interaction between mGlu7 and α1-adrenergic receptors could be confirmed at a behavioural level, we performed the FST in mice. This test has value in predicting the antidepressant-like effect of drugs or environmental manipulations (Krishnan and Nestler, 2008, Krishnan and Nes
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Considering the physicochemical stability results
2024-02-18
Considering the physicochemical stability results on Fig. 5, it was observed that the particles are stable when they are stored at 4 °C for 30 days. After day 30, a significant increase was observed in particle size, but at the end of the 90 days the SLN particle size is still below 100 nm. Stabilit
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The combination of Aurora kinase inhibitors with standard
2024-02-18
The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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In our study caspase and DRAM were identified as being
2024-02-18
In our study, caspase3 and DRAM were identified as being involved in full-length AIFM1-induced apoptosis. Caspase3 is best known for its role in the execution phase of apoptosis in both intrinsic and extrinsic apoptotic pathways [17]. The members of the caspase family are generally in inactive pro-f
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MADS box proteins are combinatorial transcription factors in
2024-02-18
MADS box proteins are combinatorial transcription factors in that they often derive their regulatory specificity from other DNA binding or accessory factors. In many cases, the cofactor with which MADS box proteins interact specifies which genes are regulated, when they are regulated and if these ge
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