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In conclusion we have found
2021-04-12

In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response AKT inhibitor VIII at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promo
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bms-690514 Several DA receptors heteromers with a therapeuti
2021-04-12

Several DA receptors heteromers with a therapeutic potential have been described, including D1R/D3R (Fiorentini et al., 2010), but their roles remain to be established. Moreover, most studies on receptor heteromers in addiction focused on the striatum because of its key role in the pathology and its
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Two parameters were extracted from these experiments
2021-04-12

Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin
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In conclusion we demonstrated phenoconversion of
2021-04-12

In conclusion, we demonstrated phenoconversion of CYP3A in stable kidney transplant recipients, and that higher plasma indoxyl sulfate concentrations in these subjects may be involved in the phenomenon. The present findings suggest that dose adjustment of drugs metabolized by CYP3A may be needed in
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br Conclusion The preclinical data reported in this
2021-04-12

Conclusion The preclinical data reported in this study shows that LAS191859 is a potent and safe CRTh2 antagonist, with a long receptor residence time that provides a sustained in vivo efficacy. This property is reflected in the prolonged duration of action of LAS191859 in in vitro and in vivo fu
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It was recently reported that a functional single
2021-04-12

It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid chloroquine phosphate 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an autosomal
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br Results br Discussion This study assesses impacts of
2021-04-12

Results Discussion This study assesses impacts of HLA-DPB1 and CMV reactivation on GVHD, relapse, and OS after allo-HSCT. Here we demonstrate that HLA-DPB1 and CMV reactivation both increase aGVHD risk independently. Consistent with reported data, we show that HLA-DPB1 mismatching is associate
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Replacement of the saturated propoxy group in
2021-04-12

Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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In recent years there has been much interest
2021-04-12

In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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br Conflicts of interest br Author contributions br Acknowle
2021-04-10

Conflicts of interest Author contributions Acknowledgements This work was supported by the University of Brescia (ex 60%) and Siderurgica Leonessa research funds to AF. RR was supported by Associazione Italiana per la Ricerca sul Cancro - AIRC (MFAG 18459 grant). We are grateful to Umberto
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Our study revealed elevated basal Akt phosphorylation in die
2021-04-10

Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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Currently two approaches can be used individually or
2021-04-10

Currently, two approaches can be used individually or combinedly to overcome weak immunogenicity of subunit Nalidixic acid (Bookstaver et al., 2018; Moyle, 2017; Vartak and Sucheck, 2016). The first is to design particulate antigens. Virus-like particles (VLPs), for example—mainly derived from the c
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The roles of ginsenoside in E and S proteasome
2021-04-10

The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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It is of interest to consider an explanation
2021-04-10

It is of interest to consider an explanation for the apparent phosphorylation of hSSB1 in undamaged cells. One such may be that in order to execute a rapid response to replication inhibition, basal S134 phosphorylation could function to keep hSSB1 in a ‘primed’ state prior to stress. Such an arrange
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In glioblastoma methylation of pMGMT is predictive
2021-04-10

In glioblastoma, methylation of pMGMT is predictive of the efficacy of temozolomide with an increased survival [22], [23], [24], [25]. As in glioblastoma [24], [26], [27], [28], pMGMT methylation assessed by pyrosequencing (with immunochemistry, IHC) is the most effective and reproducible technique
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