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To develop antagonists selective for the
2020-01-20

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic ampar () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde . 4-C
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Expression of both CH H
2020-01-20

Expression of both CH25H and CYP7B1 by lymphoid stromal Z-YVAD-FMK is required for the synthesis of 7α,25-OHC in lymphoid tissues and the correct positioning of B cells. Production of EBI2 ligand by hematopoietically derived cells appears limited [24] but may occur under some circumstances, given th
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Sunitinib mg Two primary members of the TRIM family TRIM and
2020-01-20

Two primary members of the TRIM family – TRIM5α and TRIM25 – function as antiviral effector and immune regulator, respectively. TRIM5α is one of the best characterized members of the TRIM family (both structurally and functionally) and reported to be an important ubiquitin-mediated regulator of a ma
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br Results and Discussion br Experimental Procedures br
2020-01-20

Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac
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br Materials and methods br
2020-01-20

Materials and methods Results Discussion ParI, the first C5-DNA-MTase from a psychrophilic bacterium to be characterized, displays DNA methylation activity in vivo and in vitro. Its biophysical characteristics are consistent with large regions of disorder including thermal unfolding transit
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Since the initial identification of DNA ligase inhibitors by
2020-01-20

Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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The first example of a broadly
2020-01-20

The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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br General Characteristics of the
2020-01-20

General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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br Conflict of interest br Acknowledgments Dr Hauger was
2020-01-20

Conflict of interest Acknowledgments Dr. Hauger was supported by a BLR&D Merit Review grant from the Department of Veterans Affairs, Veterans Health Administration, Office of Research and Development. Dr. Hauger also received support from the VA Center of Excellence for Stress and Mental Healt
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A previous pharmacokinetic study of
2020-01-20

A previous pharmacokinetic study of curcumin in mice demonstrated that curcumin could not be detected in plasma after a single oral dose of 75 mg/kg of curcumin. After 4-months administration of 75 and 300 mg/kg of curcumin, plasma levels of curcumin and THC were 0.095 and 0.465 μM and 0.025 and 0.1
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Previously to detect CDKL activity we used
2020-01-19

Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti
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In addition to carbamates organophosphates are classic inhib
2020-01-19

In addition to carbamates, organophosphates are classic inhibitors of cholinesterases. Previous studies with aquatic organisms have demonstrated their sensitivity to such chemicals. For example, individuals of the freshwater fish Colossoma macropomum exposed to the organophosphate dichlorvos, chlorp
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Our present results support a
2020-01-19

Our present results support a major role of EP1 receptors in peripheral heat sensitization and a smaller contribution to central heat sensitization but no contribution to mechanical sensitization. While the contribution of peripheral EP1 receptors to heat hyperalgesia is in good agreement with the a
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The synthesis of the required substrates is shown in see
2020-01-19

The synthesis of the required substrates is shown in (see for experimental details). Treatment of heterocycle with Almorexant under basic conditions afforded a mixture of the mono-substituted product (22%) and the di-substituted compound (38%) which were separated by column chromatography. Co
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br Conflict of interest br Acknowledgements This
2020-01-19

Conflict of interest Acknowledgements This work was supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP: 2014/00926-3). Introduction The metacestodes of Taenia solium are the causative agent of cysticercosis, which mainly resides the skeletal muscles and the central n
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