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semagacestat In response to DSB the
2024-02-19
In response to DSB, the lesion recognition factor Mre11-Rad50-Nbs1 (MRN) complex helps the recruitment of ATM to the damage site and its activation by phosphorylation [29]. However, whether UV-damage recognition factors directly influence ATR and ATM recruitment and their phosphorylation is not clea
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VEGFR inhibition using sunitinib does not
2024-02-19
VEGFR2 inhibition using sunitinib does not result in tumor growth reduction or in a further decrease in vessel density in NDRG1 overexpressing glioma rendering these tumors intrinsically resistant to antiangiogenic treatment. Intrinsic resistance to antiangiogenic therapy is defined as a non-respons
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Ultracentrifugation of AD brain was
2024-02-18
Ultracentrifugation of AD Valinomycin was reported to remove >99.95% of Aβ, while only reducing seeding capacity by 70% (Langer et al., 2011). This suggests that the most potent seeding Aβ species are relatively small soluble oligomers rather than larger insoluble fibrils. It was also noted that th
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Synaptic scaling up is induced within primary visual
2024-02-18
Synaptic scaling up is induced within primary visual tetraethylammonium (V1) by brief sensory deprivation (Desai et al., 2002; Lambo and Turrigiano, 2013). Several studies have examined the transcriptional changes within extracts of V1 following visual deprivation protocols (Lachance and Chaudhuri,
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br Perspectives br Acknowledgments This
2024-02-18
Perspectives Acknowledgments This investigation was supported by a Research Grant 2010/01385-5 from FAPESP (Sao Paulo Research Foundation, Brazil). P.F.S. was recipient of a CNPq (National Council for Scientific and Technological Development, Brazil) productivity grant. R.F.A. was recipient of
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Alectinib is a second generation ALK antagonist that is
2024-02-18
Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a prostaglandi
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For the first series we
2024-02-18
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivative
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Synthesis of the pterin carboxamides was achieved as
2024-02-18
Synthesis of the pterin-7-carboxamides was achieved, as shown in , based on a previously reported method that utilizes DBU as a key additive to dissolve pterin in organic solvents and accelerate the reaction., With this method, the pterin-amino Mifepristone conjugates (–) were readily obtained by s
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Heart failure is a chronic syndrome in
2024-02-18
Heart failure is a chronic syndrome in which the heart is unable of pumping an adequate supply of blood to meet the metabolic requirements of the body or generating the required elevated ventricular filling pressures to maintain output [34]. Despite considerable advances in the treatment of heart fa
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The present work has implications for our thinking about
2024-02-18
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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br Materials and methods br Results
2024-02-18
Materials and methods Results Discussion More experiments were performed in order to explain the mechanism that is involved in monohydrochloride death both PC3 and Hep G2 cells using compound 5. Results showed that this compound inhibits cell viability inducing apoptosis in a concentration
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br Aberrantly enhanced adenosine signaling in retina of oxyg
2024-02-18
Aberrantly enhanced adenosine signaling in retina of oxygen-induced retinopathy Current therapeutic development of ROP focuses on directly targeting VEGF and HIF-1α signaling pathway (Cavallaro et al., 2014, Penn et al., 2008, Mintz-Hittner et al., 2011, Hartnett and Penn, 2012). However, cellula
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An alternative approach to the
2024-02-18
An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T
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Finasteride has been shown to be a mechanism
2024-02-18
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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In an effort to determine if one ARI
2024-02-18
In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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