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Methods Very briefly PLA polymeric nanoparticles as well as
2021-12-14
Methods Very briefly: PLA polymeric nanoparticles as well as liposomes were synthesized and loaded with three different FGFR inhibitors. The encapsulation efficiency, average size, PDI, zeta potential, stability and release kinetics were investigated. The most promising formulations were biological
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Moreover long term treatment of leukemia cells with imatinib
2021-12-13
Moreover, long term treatment of leukemia cells with imatinib activates AKT, ERK and STAT5 signaling pathway and induce upregulation of EZH2 protein in patients with CML, Ph + ALL and human eosinophilic leukemia cell line (EOL-1 cells) [142]. So, resistance to tyrosine kinase inhibitor (TKI) imatini
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Although it has been observed
2021-12-13
Although it has been observed in numerous studies and by many investigators that intraplatelet cGMP elevation results in platelet inhibition, there are a few papers which proposed a platelet stimulatory role for cGMP when elevated in response to NO donors or PDE5 inhibitors in mouse and human platel
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br Conclusion and prospect Small GTPases are very important
2021-12-13
5. Conclusion and prospect Small GTPases are very important regulatory proteins of eukaryotes. They play crucial regulatory function in various movement processes of organism [75], [76], [77]. Different nanoparticles used to investigate the interaction with small GTPases inside BH3I-1 mg have be
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GlxI is a member of the superfamily
2021-12-13
GlxI is a member of the βαβββ superfamily of proteins, consisting of fosfomycin resistance protein (FosA), methylmalonyl-CoA epimerase (MMCE), extradiol dioxygenase (DIOX), mitomycin C resistance protein (MRP) and bleomycin resistance protein (BRP) [29], [30], [31]. These proteins are believed to ha
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jak kinase Epidemiological studies revealed that vitamin D d
2021-12-13
Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio
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Limitations of our study are the
2021-12-13
Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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The mechanism underlying the anorectic effect of OXM is well
2021-12-13
The mechanism underlying the anorectic effect of OXM is well established. It is centrally mediated via GLP-1 receptor activation, confirmed by both pharmacological blockade of the GLP-1 receptor, and using GLP-1 receptor knock-out mice [2], [11], [12]. However, the mechanism by which it increases en
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In order to address the Cyp inhibition issue
2021-12-13
In order to address the Cyp inhibition issue, we tested the possibility of further changes in the heterocycle combined with reducing the electron density in the ring system by swapping the central aniline nitrogen atom for a ketone. details the synthesis of these analogs, which started with 7-bromo
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These reports have gradually established G
2021-12-13
These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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In a recent study Neelaveni et al
2021-12-13
In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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Magtanong et al observed that caspase dependent apoptotic li
2021-12-13
Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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br Acknowledgments R Dalmann has obtained a
2021-12-13
Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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It is possible that maternal separation induced USV
2021-12-10
It is possible that maternal separation-induced USV in neonatal rodents is not a good model of adult anxiety for examining GlyT1 inhibitors, if the expression levels of GlyT1, GlyA, and GlyB markedly differ between pups and adults. However, several reports provide evidence that this is not the case.
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The general synthetic routes leading to aspartate
2021-12-10
The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic MDL 12330A hydrochloride analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is wor
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