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A comparison of our results with literature data on the
2021-10-01
A comparison of our results with literature data on the action of pregnane and androstane steroids on the functional activity of NMDAR, GABAAR and GlyR enables us to draw the following conclusions. First, androstane steroids (with no substituents at C-17) at a concentration up to 50 μM do not affect
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Natural products are a diverse and interesting source for th
2021-10-01
Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind
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We note that zinc speciation at and mol equiv of
2021-10-01
We note that zinc speciation at 0 and 2 mol. equiv. of myristate is already markedly different; this means that FFAZn2+ crosstalk is in operation under normal physiological conditions. At present, there are few data to allow tracking of the effects of such physiological crosstalk, although there are
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AD is a major neurological disorder usually effecting the
2021-10-01
AD is a major neurological disorder, usually effecting the elderly population, which is difficult to diagnose until symptoms begin to accumulate. As of 2013, approximately five million Americans were living with AD. The number with this disease is projected to be 16 million by 2050 (Hebert et al., 2
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The cytotoxicity of these compounds against Hep B
2021-10-01
The cytotoxicity of these compounds against Hep3B cells was assessed using the MTT assay. As shown in , compounds in series and (except ), which retained the carboxyl at C-17, showed no appreciable cytotoxic activity (IC > 100 μM), whereas compounds in series (except ,) were modestly cytotoxic, i
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We report herein an electrochemical analysis of the interact
2021-10-01
We report herein an electrochemical analysis of the interaction between L1 and sGC, where conventional solution phase voltammetry is combined with a novel technique, the voltammetry of microparticles (VMP), in order to obtain mechanistic information on the deactivation of sGC by L1. The VMP is a sol
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As a measure of ROS formation we measured
2021-10-01
As a measure of ROS formation we measured the extent by which Cu(I) affected the production of hydrogen peroxide and, at the same time, to ensure that there would not be shortage of NADH substrate. Our results show that H2O2 production is increased over time by LPS stimulation but it is not when mic
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Although resembling a differential symbiotic relationship in
2021-10-01
Although resembling a differential symbiotic relationship, interplay between prostate tumour CAFs promotes PKM2/HIF-1-driven transcriptional regulation in prostate cancer cells that exploit lactate produced by CAFs and undergo epithelial-to-mesenchymal transition (EMT) [21]. Although recent observat
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br Methods br Results br Discussion Our
2021-10-01
Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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A general synthesis of the
2021-10-01
A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic Senexin B followed by reduction of the
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Apple juice is the most consumed apple
2021-10-01
Apple juice is the most consumed apple derivative since more than 20% of freshly harvested apples are consumed as juice (Schulze et al., 2014). Apple juice production implies several technological interventions, among which are skin and pomace removal, enzymatic depectinization, and pasteurization.
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The present study also demonstrated that edoxaban
2021-09-30
The present study also demonstrated that edoxaban inhibited both free and clot-bound FXa activity. The IC50 values for free and clot-bound FXa in this study are well consistent with Ki values for free FXa and FXa incorporated in prothrombinase complex (0.561 and 2.98nM, respectively) in our previous
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br Experimental br Acknowledgments br Human
2021-09-30
Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic diseases
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AKT inhibitor VIII sale Sometime ago we have described diam
2021-09-30
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by AKT inhibitor VIII sale and zymosan. In this work we des
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The fibulins are a newly abundantly
2021-09-30
The fibulins are a newly abundantly in the basement membrane of blood vessels. Among them, fibulin-1 is essential for elastin polymerization. Tropoelastin cannot be assembled into mature elastin fibrils without the functional fibulin-1. In adult blood vessels, pronounced fibulin 1 deposition can be
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