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Potential break through technology poised to overcome these
2020-10-06
Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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In the present study we investigated the deeper
2020-10-06
In the present study, we investigated the deeper role of eNOS in the pathogenesis of nasal polyps and analyzed the influence of 1,8-cineol on nasal polyp gene and protein expression of eNOS in vitro. Different studies dealt with the localization and expression of eNOS in nasal polyps and nasal mucos
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br Material and methods br Results
2020-10-06
Material and methods Results Discussion Cysticerci located in host tissues are exposed to several effector mechanisms of the immune system (Flisser et al., 1986; Sciutto et al., 2000; Amit et al., 2011; Singh et al., 2013). In addition, the extensive uptake of host proteins by cysticerci ha
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There is literature precedence for the
2020-10-05
There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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br Acknowledgments br Introduction Hypertensive
2020-09-30
Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat
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br Methods An ongoing prospective study
2020-09-30
Methods An ongoing prospective study at the Princess Margaret Cancer Centre is enrolling consenting patients with stage IV EGFRm NSCLC for longitudinal blood collection. Patients may enrol at any point in their treatment. In this study, we performed a cross-sectional analysis of 72 patient liquid
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From a mechanistic standpoint the BCL RD domain
2020-09-30
From a mechanistic standpoint, the BCL6 RD2 domain represses the GPR183 and S1PR1 loci by recruiting HDAC2, but not MTA3-NuRD, to suppress the enhancer activation mark H3K27ac at their distal regulatory elements. However, these data do not exclude the possibility that other as yet unknown corepresso
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E ubiquitin ligases are key players in
2020-09-30
E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligase
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br APC C Uses a
2020-09-30
APC/C Uses a Dynamic Cullin–RING Mechanism to Elongate Polyubiquitin Chains Human APC/C generates Lys11-linked poly-Ub chains through an entirely different mechanism, via the distinctive E2 enzyme, UBE2S 30, 31, 32. Although APC2 and APC11 are necessary and sufficient to activate UBE2S, the mecha
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br Cysteine proteases as molecular
2020-09-29
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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Converging evidence suggests that reduced glutamate transmis
2020-09-29
Converging evidence suggests that reduced glutamate transmission in the LS is linked to increased anxiety-like behaviors (Radulovic et al., 1999, Henry et al., 2006, Bakshi et al., 2002, Liu et al., 2004). Therefore, attenuated CRF1 receptor-mediated excitatory transmission in the LS following ASV-t
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Based on the finding described above the
2020-09-29
Based on the finding described above, the present study was designed to investigate the effects of specific CRF receptors, CRF1 and CRF2, in the BLA and CeA on the duration of TI in guinea pigs (Cavia porcellus). To this end, we evaluated whether administration of the CRF1 colorimetric antagonist CP
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To determine the time course of
2020-09-29
To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour Kinase Inhibitor Library were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, sugg
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In the present study we did not
2020-09-29
In the present study, we did not examine whether the CpG site-specific COMT methylation are associated with any genetic variants in response to E2, GEN or SFN. Some studies suggest that oxidative DNA damage causes genetic variation which may induce epigenetic changes that lead to gene silencing (Kho
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Compounds were synthesized as illustrated in tetrazole yl be
2020-09-28
Compounds – were synthesized as illustrated in , , , , . 3-(1-tetrazole-5-yl)benzaldehyde was obtained in 95% yield via [2+3] cycloaddition of sodium azide to commercially available 3-cyanobenzaldehyde in presence of triethylamine as reported in the literature. Nitration of 3-hydroxyacetophenone wit
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