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Beside the previously reported Topo I inhibition
2020-04-09
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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br Materials and methods br Results
2020-04-09
Materials and methods Results and discussion Conclusions Acknowledgements This work was supported financially by the LIAONING S&T Project (No. 20180550107) and Basic Scientific Research Funds of DLNU (0918110143). Introduction Since 1970s, numerous artificial mimetic enzymes have bee
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A limitation of this study
2020-04-09
A limitation of this study is the between-study heterogeneity of the datasets analyzed. To address this heterogeneity, we used a random-effects model in our analysis. Also, only 2 of the databases provided information on sex, and as a result, the sex-specific analyses were performed with a smaller c
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D609 All these results indicate that cleaving embryos posses
2020-04-09
All these results indicate that cleaving embryos possess a regulative mechanism, sensing the number of inner D609 and controlling the proportion of conservative and differentiative divisions of blastomeres. The current observations agree with the results from other laboratories and our previous stud
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CD 2665 PRRSV is a single stranded positive
2020-04-09
PRRSV is a single-stranded, positive-sense enveloped RNA virus in the family Arteriviridae of the order Nidovirales (Meng et al., 1994, 1996). The PRRSV CD 2665 is approximately 15 kb in length and contains eleven known open reading frames (ORFs) (Snijder et al., 2013). The 3′ end of the genome enco
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JNJ26481585 br Introduction The protein Epidermal Growth Fac
2020-04-09
Introduction The protein Epidermal Growth Factor Receptor Tyrosine Kinase (EGFR-TK) play important role in non small-cell lung carcinoma (NSCLC) and vital therapeutic progress withinin the treatment of this ailment has revamped the past ten years through the exploitation of this insight (Mok et a
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Main Text Post translational modifications by ubiquitin Ub
2020-04-09
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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Preparation of the regioisomeric pyridooxazepinones and was
2020-04-09
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and 2-deoxy-d-glucose chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a
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WP1130 As we all known hypoxia is a hallmark
2020-04-09
As we all known, hypoxia is a hallmark of tumour microenvironment, which is a key regulator of tumour growth and metastasis [4]. Hypoxia meditates a series of cellular responses including angiogenesis by activating transcriptional factor hypoxia inducible factor (HIF), which is consist of an obligat
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Drug drug interactions are frequently attributed to function
2020-04-08
Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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In the preclinical evaluation of CRF receptor antagonists ef
2020-04-08
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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In humans several different small ubiquitin
2020-04-08
In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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In the SUMOylation pathway SCE
2020-04-08
In the SUMOylation pathway, SCE1 as an E2 enzyme has an important role in mediating the conjugation of SUMO to target proteins. The accumulated SUMO conjugates in plants are associated with abiotic stress responses (Castro et al, 2012). We performed a drought stress analysis on WT plants, induced by
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Oxysterols modulate the immune responses and as such could
2020-04-07
Oxysterols modulate the immune responses and as such could be effectors of the tumor environment: 25-OHC impairs IgA production in B-lymphocytes [26] and induces the secretion of the proinflammatory and angiogenic cytokine IL-8 [27], [28]. Of note, oxysterols (in particular 7α,25-OHC) are potent che
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C PHNO has been described as a full agonist
2020-04-07
[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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