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According to the literature HER mutations
2022-06-08
According to the literature, HER2 mutations are present in 2–4% of lung adenocarcinoma (ADC) patients. Most HER2 mutations are in-frame insertional mutations occurring at exon 20 in the protein kinase domain [[2], [3], [4], [5]]. Although several small molecules and HER2 L-Carnitine inner salt austr
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br Material and methods br Results
2022-06-08
Material and methods Results Discussion In vitro testing is necessary to study DAA activity and putative RASs. Compared to enzymatic assays and replicons, HCV infectious culture systems reflect the full viral life cycle and previous results in these systems reflected clinical data.[13], [14
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All the compounds and were
2022-06-08
All the compounds –, , , –, , – and – were assayed for their potential cytotoxicity at a single dose of 10 µM on Huh7 cells. Interestingly, all compounds proved to be non toxic, with the exception of and which exhibited high cellular toxicity and therefore were excluded from further experiments (a
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br Financial support This study was supported
2022-06-08
Financial support This study was supported by Grant PH-102-PP-11, PH-103-PP-11 from the National Health Research Institutes, Taiwan. Conflict of interest Please refer to the accompanying ICMJE disclosure forms for further details. Authors’ contributions Acknowledgements Introduction
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br For some time it was known that membrane bound
2022-06-08
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor ONO-8711 synthesis in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on t
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Thus our data demonstrate that polymorphisms
2022-06-08
Thus, our data demonstrate that polymorphisms of GSTP1-1 differentially mediate activation of Prdx6 peroxidase activity, providing a platform to imply that contingent upon their GSTP genotype, individuals will have significant differences in mounting an antioxidant response, particularly affecting p
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Ellagic acid br Mutagenesis and Receptor Modeling Studies
2022-06-08
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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Apart from the different assays used biased agonism
2022-06-08
Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 MK-0822 stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+ was b
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Gene expression of both GPR A and GPR in
2022-06-08
Gene expression of both GPR109A and GPR81 in adipocytes has been linked to PPARγ activation [22]. Treatment with the thiazolidinedione (TZD) PPARγ agonist, rosiglitazone, increases GPR109A and GPR81 expression, and knockdown of PPARγ suppresses receptor expression in fully differentiated human multi
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As GLO is the major detoxification system of reactive
2022-06-08
As GLO1 is the major detoxification system of reactive dicarbonyls, it is plausible that differences in production and activity of the enzyme influences AGE production and the development and/or modulation of diabetic neuropathy. Glo1 exists as a copy number variant (CNV) in many inbred strains mice
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Our overall goal is to develop selective compounds for low
2022-06-08
Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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Hippo signaling is an emerging tumor suppressor pathway that
2022-06-08
Hippo signaling is an emerging tumor suppressor pathway that plays key roles in normal physiology and tumorigenesis through the regulation of cellular proliferation and survival [4]. In humans, YAP is over-expressed as a result of genomic amplification of the 11q22 locus in a wide spectrum of human
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Several studies have found decreased astroglial
2022-06-08
Several studies have found decreased astroglial and neuronal cell numbers and Natural Product Library damage after OP exposure. Neuronal loss and brain lesions increase proportionally to the severity and duration of OP-induced seizures (Albuquerque et al., 2006, Carpentier et al., 2000, Gullapalli
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There is increasing evidence that
2022-06-08
There is increasing evidence that Cxs in astrocytes may play a role in several models of brain pathologies. Interestingly their roles are at the moment more considered through their hemichannel function (Bennett et al., 2012; Bosch and Kielian, 2014; Davidson et al., 2013; Orellana et al., 2016; Kim
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In summary the SAR of a series of
2022-06-07
In summary, the SAR of a series of phenylpropanoic acid-free fatty Methylmalonate receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust
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