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In HepG cells compound showed inhibition of total lipid synt
2024-01-24
In HepG2 cells, auda mg showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, compound sh
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br Author contributions br Conflicts of interest
2024-01-24
Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur
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Receptor Subtypes and Their Function Critical Appraisal Larg
2024-01-24
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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A different mechanism has been suggested
2024-01-24
A different mechanism has been suggested for the role of TRX1 in ASK1 regulation based on disulfide bond-mediated ASK1 multimerization and its reduction through the thiol-reductase activity of TRX1 (Nadeau et al., 2007, Nadeau et al., 2009). In this model, oxidative stress induces intermolecular dis
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Electron paramagnetic resonance studies of mixtures of A and
2024-01-24
Electron paramagnetic resonance studies of mixtures of Aβ1–40 and Aβ1–42 suggest that interlaced fibrils might also form [40] where Aβ1–40 and Aβ1–42 is found within the same fibril. Considering the Aβ fold rather than the sequence, these observations imply two mechanisms that might lower the total
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br Polymorphic variation ERAP is polymorphic and
2024-01-24
Polymorphic variation ERAP1 is polymorphic and several single nucleotide polymorphisms (SNPs) in its gene that encode amino neostigmine bromide changes have been associated with predisposition to a variety of diseases, ranging from viral infections to cancer and autoimmunity (Alvarez-Navarro and
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Sodium ascorbate We found that several anticancer drugs inhi
2024-01-24
We found that several anticancer drugs inhibit 5-HT3 Sodium ascorbate current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used f
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As an alternative to chronic receptor blockade we have been
2024-01-23
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify 873 adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facilitates the cle
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The physiological effect of adenosine is
2024-01-23
The physiological effect of adenosine is now considered a new direction in halting the progression of organ damage in cardiovascular disease [24], [25], [26]. Adenosine has diverse functions, depending on its interaction with different receptor subtypes: A1, A2A, A2B, and A3[24], [25], [26]. Stimula
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Ten strains of lactobacilli TMW isogenic with strain
2024-01-23
Ten strains of lactobacilli: TMW 1.1434 (isogenic with strain F19 ), TMW 1.1733 (isolated from fermented food), TMW 1.1628 (isolated from baby feces), TMW 1.1609 (isolated from baby feces), TMW 1.1734 (isolated from fermented food), TMW 1.313 (isolated from non-pasteurized Heineken beer), TMW
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Although effects of low concentrations of agonist were not
2024-01-23
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major Senexin B α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiti
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br Experimental procedure br Introduction Migraine is a debi
2024-01-23
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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The most potent compounds within the current series of
2024-01-23
The most potent compounds within the current series of compounds were therefore , , , , and , with Cyclophosphamide mg possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17
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The introduction of a pyrazole moiety into any position
2024-01-23
The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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At present drugs that specifically inhibit YAP
2024-01-23
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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