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Verapamil a calcium channel blocker used clinically as
2019-10-28
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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The knockout mice models of the DNMTs gene shed
2019-10-28
The knockout mice models of the DNMTs gene shed light on understanding the molecular background of male infertility development. Dnmt1−/− causes demethylation of the genome (Lei et al, 1996, Li et al, 1992) (). The Dnmt3a conditional knockout mouse models exhibit spermatogenic arrest at the spermato
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br Acknowledgements This work was supported by a
2019-10-28
Acknowledgements This work was supported by a Grant for the Program for the Strategic Research Foundation at Private Universities S1101017 organized by the Ministry of Education, Culture, Sports, Science, and Technology (MEXT), Japan and JSPS KAKENHI Grant Numbers JP22560209 and JP5K05842. The
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To understand more clearly how these
2019-10-28
To understand more clearly how these activities are combined in the heterotrimeric enzyme and to understand more clearly how DNA alkylation might effect DNA helicase activity, we summarize the relevant features of the structure of RecBCD determined in the presence of DNA. The RecB and RecC subunits
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The causes of POD are complex
2019-10-25
The causes of POD are complex, and not entirely clear. Androsova et al, believed that the main molecular mechanism of POD is a central cholinergic deficiency caused by deregulation of cholinergic anti-inflammatory pathways leading to increased inflammation. The cholinergic anti-inflammatory pathway,
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For these reasons molecules of the ET
2019-10-25
For these reasons, molecules of the ET family and in particular ET-1 are considered useful factors in the evaluation of malignancy and in consequence, in the prognosis for several forms of neoplasia, such as ovarian (Bagnato et al., 2005), prostate (Nelson et al, 1995, Nelson et al, 1996), colorecta
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Her eldest daughter individual had a normal birth and health
2019-10-25
Her eldest daughter (individual 4) had a normal birth and health history in early childhood. She developed contractures of her fourth fingers at 4–5 years of age; these contractures were associated with painless, non-erythematous swelling of the involved joints. Her PIP contractures were ∼90 degrees
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Compound was synthesized by the directed metallation procedu
2019-10-25
Compound () was synthesized by the directed -metallation procedure (DOM) at the stage of the amide using butyl lithium and dry ice as CO source for the introduction of the carboxylic group. Thiophene amides were prepared from commercial 3-thiophenecarboxylic SGC 0946 by conversion into the acid c
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That DGAT mediated hepatic steatosis did not
2019-10-25
That DGAT-mediated hepatic steatosis did not lead to insulin resistance was clearly demonstrated in Liv-DGAT2-low mice by their normal blood glucose and plasma insulin levels, normal glucose and insulin tolerance, normal insulin sensitivity by hyperinsulinemic-euglycemic clamp studies, and normal he
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Given the excellent in vitro pharmacology profiles of methyl
2019-10-25
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic AT13148 functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1 inhibi
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An AmDH is engineered by mutating two conserved
2019-10-25
An AmDH is engineered by mutating two conserved amino BV6 residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively, resulted in t
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Tenatoprazole br Conclusion The results of the present study
2019-10-25
Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by CysL
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Among the Ub interactions observed in the HOIP
2019-10-24
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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Taken together these assays demonstrate that SUMOD positioni
2019-10-24
Taken together, these assays demonstrate that SUMOD positioning is essential for all E3 ligases but dispensable for E2 and S*E2 sumoylation reactions. Thus, we propose SUMOD positioning as a key criterion to describe the enzymatic function of SUMO E3 ligases that distinguishes them from other enhanc
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DGK is not the only
2019-10-24
DGKε is not the only DGK isoform that has been associated with p53. It has been shown that DGKζ binds to p53 and modulates its activity in both the cytoplasm and the nucleus [39]. In the cytosol DGKζ promotes the degradation of p53 through the ubiquitin-proteosome system [39], also a likely mechanis
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