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In the particular case of
2020-02-03

In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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MoAbs targeting the tumourigenic pathways such as
2020-02-03

MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own imm
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Several studies have shown that independently
2020-02-03

Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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Conventional aromatic radiofluorination via nucleophilic
2020-02-03

Conventional aromatic radiofluorination via nucleophilic substitution requires electron-withdrawing activating group(s) at the ortho or para position to achieve good radiolabeling yield. In the case of CJ-042794 (), the phenoxy substitution para to the fluoro group is considered an electro-donating
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ci-1033 Given its high frequency it is not surprising that
2020-02-03

Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant ci-1033 to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been proved ef
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br Acknowledgment This work was supported by the
2020-02-03

Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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br Acknowledgments br The design of polyaromatic molecules
2020-02-03

Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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The compounds were ranked based on the Glide
2020-02-03

The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR a
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It is now widely known that
2020-02-03

It is now widely known that blockade of CysLT1 receptors strongly inhibits antigen-induced bronchial contractions in specimens isolated from non-asthma subjects. However, this blockade is not complete as shown in the present study and in other literature.4, 15, 16 The results of the current study su
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br Conflicts of interest br Acknowledgements br
2020-02-03

Conflicts of interest Acknowledgements Lung cancer continues to be the leading cause of cancer deaths in the US and worldwide., Non–small-cell lung cancer (NSCLC) remains the predominant form of lung cancer (approximately 85%)., With some improvements in surgical techniques and combined ther
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Abha et al reported Natural coumarinolignoids isolated from
2020-02-03

Abha et al. reported Natural coumarinolignoids isolated from the seeds of Cleome viscosa consist of a racemic mixture of cleomiscosins A 19, B 20 and C 21 and were screened for anti-inflammatory activity through mol. docking and QSAR studies by using reported in vivo activity of Swiss albino mice. B
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Since PTKs are involved in numerous aspects of
2020-02-03

Since PTKs are involved in numerous aspects of cell function, their regulation is critical for cell survival and function. The carboxyl-terminal tyrosine of Src-family PTKs is a key site of regulation. Phosphorylation on this carboxyl-terminal tyrosine contributes to the induction of a conformationa
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Several questions remain to be addressed The hormones and
2020-02-03

Several questions remain to be addressed. The hormones and metabolites that modulate expression of EERγ in the steps leading to maturation need to be identified to learn more about physiological and pathophysiological regulation of EERγ in β cells. Considering that ERRγ repressed cell cycle genes in
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The imaging and biochemical data
2020-02-03

The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a
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At the therapeutic level the logical approach
2020-02-03

At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn
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