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Recently roflumilast has been approved as the first selectiv
2021-04-12
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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in your pocket Molecular imaging that provides a non invasiv
2021-04-12
Molecular imaging that provides a non-invasive means to visualize and measure a biological process of interest at the molecular and cellular level in living subjects has emerged as a promising approach for in vivo detection of enzyme activity in recent decades [6]. In in your pocket to anatomical im
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bag price Adding more pieces to the puzzle using a human
2021-04-12
Adding more pieces to the puzzle, using a human-to-animal crossover study, blood taken from healthy volunteers that underwent exercise was used as a dialysate to perfuse a rabbit heart in a Langendorff model of MI [62]. Unprecedentedly, dialysate of plasma from exercised humans reduced infarct size
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br Materials and methods br Results
2021-04-12
Materials and methods Results Discussion In rodent species, CYP2E1 and CYP2B have been implicated in CCl4 metabolism. In this study, we used expressed human CYP2E1 to show that this enzyme is a high-affinity catalyst responsible for low-dose CCl4 metabolism. Studies employing an inhibitory
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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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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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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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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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