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Intriguingly one E residue may serve as a molecular
2019-11-19

Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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In addition to G coupling it is important to
2019-11-19

In addition to Gα coupling, it is important to consider that the transition from goal-directed to habitual drug taking also relies on striatal D2R-A2AR heterodimers. Following cocaine self-administration, D2R-A2AR density is increased in the NAc, leading to greater antagonism of the inhibitory (anti
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br Material and methods br
2019-11-19

Material and methods Results Discussion In the present study, twenty strains of Y. enterocolitica were analyzed for their inhibitory potential on cysteine proteases. Five of these strains belonged to bioserotype 4/O:3, which is distinguished for its pathogenicity towards humans. The rest of
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br Materials and methods br Results
2019-11-19

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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br Materials and methods br Results and discussion br
2019-11-19

Materials and methods Results and discussion Conclusions Acknowledgments This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korean government (MEST) (No. 2011-0030635) and the MarineBio Research Program (NRF-C1ABA001-2011-0018561). The Fonta
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br Clinical studies br Practical implications for young
2019-11-19

Clinical studies Practical implications for young women Conclusion Research on the oncogenic mechanism of hormones has advanced dramatically in the latter years. The finding that progestogens are more powerful determinants of risk than estrogens in breast cancer has been added to advances i
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Our previous high throughput screening
2019-11-19

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based dextromethorphan hydrobromide receptor assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimi
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Enzyme selectivity of many enzymes like galactosidases acyla
2019-11-19

Enzyme selectivity of many hippo pathway like β-galactosidases, acylases, epoxyhydrolases, lipases, etc. has also been modulated by using different immobilization techniques. It can result in the selection of optimal biocatalyst for different processes. This has many advantages over strategies like
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The applications of fungal enzymes in paper
2019-11-19

The applications of fungal enzymes in paper industry involve biobleaching of pulp, pulp de-inking, degradation of dissolved and suspended organic compounds in concentrated effluents of mills and enhanced fibrillation. Enzymes usage is encouraged in paper industry in order to reduce the use of chemic
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br Assessing DUB activity The Ub field has benefited greatly
2019-11-19

Assessing DUB activity The Ub field has benefited greatly from the past efforts of biochemists and chemical biologists who have reconstituted Ub signals in vitro and generated tools for capturing or measuring DUB activities, many of which can be readily produced or are commercially available (Ekk
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The lack of effective strategies aiming to
2019-11-19

The lack of effective strategies, aiming to directly increase the neuronal survival, is reflected by the fact that the only available therapeutic interventions are indirect. They consist of acute therapeutic interventions involving chemical and/or surgical removal of the thrombotic clot (Taqi et al.
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Verapamil a calcium channel blocker used clinically as a
2019-11-19

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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Currently phosphodiesterase type PDE inhibitors
2019-11-18

Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is
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Approximately of the etamicastat dose was recovered in urine
2019-11-18

Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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Henderson et al reported that allergen induced
2019-11-18

Henderson et al. [20] reported that allergen-induced airway remodeling was blocked by the CysLT1 receptor antagonist montelukast. The development of epithelial thickening and mucus accumulation at relatively small Sulconazole Nitrate was also suppressed by montelukast. The CysLT2 receptor antagonis
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