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Participants Andexanet alfa works as a decoy for the FXa inh
2021-11-18
Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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br Acknowledgment br Introduction Non
2021-11-18
Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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The synthetic pathway of the target compounds and
2021-11-18
The synthetic pathway of the target compounds , , , and is presented in . The intermediate was synthesized according to a reported method. The intermediate was prepared by mixing UA with an equimolar concentration of KCO, a catalytic amount of KI, and more than two equivalents of 1,2-dibromoethan
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The observed tendency for higher plasma
2021-11-18
The observed tendency for higher plasma lactate levels in the aerated thermal exposure suggests increased reliance on o6 methylguanine methyltransferase metabolism to maintain function. This finding is supported by a recent study that observed an increased ṀO2 in European perch (Perca fluviatilis) e
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Under increased drug pressure more
2021-11-18
Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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br Introduction The replacement of a regular intake of healt
2021-11-18
Introduction The replacement of a regular intake of healthy oils and fibres for a diet based substantially on high fat- and high sugar-content foods has had profound consequences for public health. These changes in the way that the populations of high income, particularly Western countries, manag
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br Mutagenesis and Receptor Modeling
2021-11-18
Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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br FXR Agonists Azepinol b indole hEC nM efficacy eff
2021-11-17
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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While the S site has been implicated
2021-11-17
While the S2 site has been implicated in binding, it BAY 61-3606 receptor is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. However, th
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D-Pantothenic acid BCCA occlusion followed by reperfusion in
2021-11-17
BCCA occlusion, followed by reperfusion injury, significantly increased the brain AT1 and AT2 receptor expression in mice. Reports have demonstrated elevation of AT1 receptor expression in the cerebral D-Pantothenic acid during ischemia [34,35]. The gene expression of brain AT2 receptor is increased
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br Methods br Results br Discussion Significant alterations
2021-11-17
Methods Results Discussion Significant alterations in the expression of genes related to the glutamatergic system have been shown in several experimental models of epilepsy; however, in most studies focused on acute changes or modifications in expression, these were investigated during the
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Underlying this study is the hypothesized importance
2021-11-17
Underlying this study is the hypothesized importance of insulin and glucose metabolism on bone. In our investigation of GIP and GIPR gene polymorphisms in relation to bone phenotypes in young and old women our findings depict a complex relationship between glucose metabolism genes and bone. In the c
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Kif15-IN-1 Data were collected using a Powerlab and Chart so
2021-11-17
Data were collected using a Powerlab and Chart 5 software (ADInstruments, Bella Vista, NSW, Australia) and were analysed using GraphPad Prism 5 (GraphPad Software, San Diego, CA). Responses to ghrelin receptor agonists in phenylephrine, methoxamine, endothelin-1, U46619 and 60mM [K+] contracted vess
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br Introduction Hepatocyte injury initiates
2021-11-17
Introduction Hepatocyte injury initiates and facilitates inflammation in the course of liver disease progression. Thus, understanding the regulatory basis for sensing and responding to damage-associated inflammatory processes in the liver’s parenchymal cells is a primary issue in liver pathophysi
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br Acknowledgements This work was in
2021-11-17
Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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