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The in vivo IC M in
2021-03-23
The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free Nextura
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cpi 1 br Introduction Lung cancer is the
2021-03-23
Introduction Lung cancer is the leading cause of cancer-related death worldwide, accounting for more than 1.5 million deaths in 2012. Non–small-cell lung cancers represent approximately 85% of lung neoplasms; among these, squamous cell carcinomas (SCC) account for approximately 30% of cases. The
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Introduction Cysteinyl leukotrienes CysLTs LTC LTD and
2021-03-23
Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic LY3009120 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3], [4] and montelukas
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In a previous study we reported that the systemic administra
2021-03-22
In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in Schaftoside reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to inve
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The small molecule d mannuronic acid M patented DE has
2021-03-22
The small molecule β-d-mannuronic IL-18, human recombinant protein (M2000), patented (DE-102016113018.4), has been tested as an anti-inflammatory and a novel immunosuppressive agent in various experimental models such as animal models of immune complex glomerulonephritis, nephrotic syndrome, multip
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Therapeutic options targeting intrahepatic resistance are ve
2021-03-22
Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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Mammalian cells contain significant amounts of a relatively
2021-03-22
Mammalian cells contain significant amounts of a relatively lesser known enzyme that shows marked specifity for ether lipids containing AA and other 20–22 carbon fatty acids. This enzyme is called CoA-independent transacylase (CoA-IT), and transfers polyunsaturated moieties of 20–22 carbons, typical
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br Oxysterols as Key Players
2021-03-22
Oxysterols as Key Players in Metabolic Syndrome? Obesity and sedentary lifestyle are on the rise and pose serious threats to people's health and wellbeing. Obesity is often associated with other pathologies and is one of the criteria included in the definition of metabolic syndrome (MetS) (see Gl
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Introduction Protein ubiquitination is a
2021-03-22
Introduction Protein ubiquitination is a posttranslational modification that plays a major role in almost all cellular processes in eukaryotes (Hochstrasser, 2009; Komander & Rape, 2012). It involves the covalent attachment of ubiquitin (Ub) via its C-terminal glycine carboxylate to a primary amine
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serine threonine protein kinase Our data indicate that the a
2021-03-22
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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mct2 inhibitor Oral antipsychotics are substrates of CYP enz
2021-03-22
Oral antipsychotics are substrates of CYP450 enzymes, which are crucial to their metabolism and elimination (Fig. 1). The efficacy and toxicity of antipsychotic agents is affected by factors that induce or inhibit CYP450 expression and function, such as drug–drug interactions. Additionally, the mult
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Confidence with which data of
2021-03-22
Confidence with which data of animal safety/toxicity studies can be translated to human depends upon the knowledge that whether humans would be exposed to similar chemical entities (parent and its metabolites) as the animals exposed during toxicity studies. In this regard, in vitro qualitative evalu
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br Experimental section br Results br Discussion
2021-03-22
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised ha 47 did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a patient by alter
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Fmoc-Val-OH australia br Most reported binding data are obta
2021-03-22
Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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br Introduction Cell transplantation therapies
2021-03-22
Introduction Cell transplantation therapies using embryonic stem cell (ESC) and induced pluripotent stem cell (iPSC)-derived retinal tissue (ESC/iPSC retina) or Asiatic acid have emerged as therapeutic options for retinal degeneration following recent breakthroughs. A number of groups have shown
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