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Conclusion We have constructed a series
2019-09-07
Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9.
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In conclusion we designed novel E1 inhibitors
2019-09-06
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds and we identified compound as a novel E1 inhibitor.
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Among the high value compounds derived from
2019-09-05
Among the high value compounds derived from agricultural residues there are enzymes with industrial application. The extraction processes have been focused on the development of new strategies that guarantee high recovery rates with maximum activity (Nadar et al., 2017).
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In summary our data demonstrated a biological
2019-09-04
In summary, our data demonstrated a biological function of cpt1a gene from large yellow croaker. In particular, we indicated the effects of fasting on free carnitine status, CPT1 kinetics, and cpt1a mRNA expression in liver of large yellow croaker. During short-term fasting, the fish liver may have a strong capacity for ensuring the optimal catalytic efficiency through regulating carnitine-dependent Km rather than gene transcription and enzyme avtivity.
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In sum although it is reasonable to assume that the
2019-09-03
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different organismal lineages 57, 58.
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After repeated intermittent exposure
2019-09-02
After repeated, intermittent exposure to a psychostimulant an augmentation of drug response to motor activity is commonly observed, a phenomenon known as behavioral sensitization (Kalivas and Stewart, 1991, Steketee and Kalivas, 2011).
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These studies established IAP proteins as
2019-08-30
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization.
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Primases are classified into two major groups
2019-08-29
Primases are classified into two major groups: first, the DnaG primases, found in bacteria and bacteriophages, and second, the archaeoeukaryotic primases.
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Recent studies from the literature have
2019-08-28
Recent studies from the literature have identified new GSK1904529A of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-tolylurea (16d)
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A subgroup of pediatric solid neoplasms
2019-08-27
A subgroup of pediatric solid neoplasms, collectively referred to as small round cell tumors (SRCTs) of childhood, demonstrates undifferentiated small round cell morphological characteristics.
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Cardiogenesis is enhanced with timely
2019-08-26
Cardiogenesis is enhanced with timely application of Wnt pathway activators and inhibitors. A combination of Wnt/β-catenin signaling pathway activators such as CHIR99021 and inhibitors such as IWP-2 and IWR-1 have been found to be highly efficient cardiomyocyte differentiation protocols [27], [28].
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Materials and methods Between January 2006
2019-08-24
Materials and methods Between January 2006 and December 2008, 34 patients with GBM were treated with postoperative three-dimensional (3D) radiotherapy at Tartu University Hospital or North Estonian Medical Centre.
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Acknowledgements This study was funded
2019-08-23
Acknowledgements This study was funded by Kuwait University Research Administration (Project MI03/10). Introduction Epidemiological, experimental and biologic plausibility support a cardioprotective effect of estrogens in women [1].
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Research funding This work was financially
2019-08-22
Research funding This work was financially supported by Shanghai Committee of Science and Technology (No. 16431903800).
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Likewise the conserved cysteine in the E2
2019-08-21
Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003).
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