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Here we explored the relative contribution of D
2020-11-20

Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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Here we uncover a highly
2020-11-20

Here we uncover a highly diverse superfamily of self-replicating MGEs, dubbed pipolins, which are present in three major bacterial phyla, as well as in mitochondria, and encode divergent PolB carrying TPR1 and TPR2 subdomains. Biochemical characterization of a representative enzyme encoded by a pipo
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Some family I DNA ligases can use dATP as nucleotide
2020-11-20

Some family I DNA ligases can use dATP as nucleotide cofactor. For instance, human Pleuromutilin I uses dATP with a catalytic efficiency that is only 36-fold lower in comparison to ATP [9]. EhDNAlig is unable to use dATP as a nucleotide cofactor, indicating a more constrained active site in compari
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br Acknowledgements Thanks are due to Science
2020-11-20

Acknowledgements Thanks are due to Science and Technology Development Fund – Egypt for the Research Support Technology Development Grant (RSTDG) no. 12626. Our deep thanks and gratitude is also extended to National Cancer Institute (NCI), Bethesda, Maryland, USA for performing the anticancer eval
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The authentic PPase was purified from B subtilis
2020-11-19

The authentic PPase was purified from B. subtilis as described previously [21], whereas the recombinant enzyme was purified to homogeneity from E. coli by a simplified procedure including only phenyl-Sepharose CL-4B column chromatography and DEAE-HPLC [21]. About 26 mg of pure enzyme was obtained fr
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br Chagas disease and HAT drug R
2020-11-19

Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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br Results and discussion br Conclusion Novel
2020-11-19

Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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cholecystokinin receptor In these studies the inflammatory c
2020-11-19

In these studies, the inflammatory cytokine IL-8 was demonstrated as one of the responsible molecules induced by CysLTs via activating CysLT2 receptors. IL-8 is synthesized in and released from mononuclear cells, macrophages, fibroblasts and airway epithelial cells, and it promotes inflammation as a
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The use of inhibitors clearly has its caveats and the
2020-11-19

The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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The CYP D inferred metabolizer
2020-11-19

The CYP2D6-inferred metabolizer phenotype describes only one phase of the tramadol (T) ADME (absorption, distribution, metabolism, and excretion) and response process and does not explain all genotypic contribution of an individual’s phenotypic expression [11]. Numerous polymorphisms in the downstre
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In the course of carbohydrate metabolism
2020-11-19

In the course of carbohydrate metabolism, pyruvate, the end product of glycolysis, is converted to acetyl-CoA, which fuels the citrate cycle for further generation of energy. In the case of elevated levels of acetyl-CoA, acetyl-CoA is converted into malonyl-CoA by the action of acetyl-CoA carboxylas
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What is the predominant mechanism underlying the benefits of
2020-11-19

What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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There is an opposite opinion indicating that EphB plays a
2020-11-18

There is an opposite opinion indicating that EphB plays a role as cancer suppressor. Batlle et al. showed that loss of EphB expression represented a critical step in CRC progression, and CRCs that lacked EphB2 expression have been correlated with more advanced tumour stage, poor differentiation, and
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br Conflict of interest br
2020-11-18

Conflict of interest Acknowledgments This work was supported in part by grants from the , Spain (INCITE08PXIB203092PR). VGM was supported by a FPU pre-doctoral scholarship from the , Spain. MLR was supported in part by a crowdfunding campaign (PRECIPITA), coordinated by the Spanish Foundation
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A comparative analysis of the cleavage
2020-11-18

A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25
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