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Signaling pathways that control the redox stress response in
2021-10-25

Signaling pathways that control the redox stress response in P. brasiliensis are poorly known, but in other dimorphic fungi, the involvement of MAPK is an important factor in this process [[13], [14], [15]]. For example, when alveolar macrophages are challenged with Aspergillus or Cryptococcus conid
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Indeed GSTP mRNA appears to be already highly stable in
2021-10-25

Indeed GSTP1-1 mRNA appears to be already highly stable in K562 leukemia tgf beta receptor 1 with a half-live of more then 40h which is even further increasing to 92h after hemin treatment and erythroid differentiation. Previous reports quantified GST mRNA half-lives which depend on the cellular mo
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Glycogen synthase kinase GSK is
2021-10-25

Glycogen synthase kinase 3 (GSK3) is currently considered to be a multifunctional serine/threonine kinase involved in a wide spectrum of cellular processes such as glycogen metabolism, cell proliferation, neuronal function, oncogenesis or embryonic development (for recent reviews see: Rayasam et al.
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Materials and methods Standard curve for http www apexbt
2021-10-25

Materials and methods Standard curve for methylglyoxal. Different concentrations (10, 25, 50, and 100μM) of pure MG (Sigma) were derivatized with 1,2-diaminobenzene and the absorbance of the resulting derivative was read by Cary 50 Bio UV-Visible spectrophotometer (Varian). One milliliter of total
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The two competitive bivalent GlxI inhibitors polyBHG nM and
2021-10-25

The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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br Perspectives br Contributors BP study concept design
2021-10-25

Perspectives Contributors BP: study concept & design, literature review, data analysis & synthesis & presentation, primary draft of the manuscript; JDR: data analysis, Fig. 1 illustration, manuscript review & revision; ZP: study concept & design, manuscript review & edit; MI: manuscript review
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br Acknowledgment br Introduction Positive and negative rein
2021-10-25

Acknowledgment Introduction Positive and negative reinforcement are known as the two pivotal components in various models of drug dependence. Compulsive drug seeking behavior results from both the euphoric effects of drug use (positive reinforcement) and the unpleasant withdrawal signs followi
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Fatty acids have been repeatedly shown to increase the respo
2021-10-25

Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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The development of metabolic stable
2021-10-25

The development of metabolic stable, non-peptidergic galanin agonists could be the basis to clinical diagnosis and treatment of tumors with high levels of galanin receptor expression like gliomas and pituitary tumors. As for gliomas, penetration of the blood brain barrier by the compounds might be p
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Active compounds and were further tested and EC
2021-10-23

Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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Chemotherapeutic approaches to glioblastoma which are highly
2021-10-23

Chemotherapeutic approaches to glioblastoma, which are highly invasive, are still largely unsuccessful and have only a minimal impact on patients’ survival rate . New agents that target the specific molecular aberrations in the tumors are presently being investigated for their efficacy against this
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Based on the aforementioned findings variations of the imida
2021-10-23

Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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An interesting question is why RhoF has such
2021-10-23

An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino BI-847325 mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF, rather than
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br Materials and methods br Results and discussion br
2021-10-23

Materials and methods Results and discussion Conflict of interest Introduction In the presence of continuous and excessive levels of nutrients, adipocytes become hypertrophic and release several pro-inflammatory adipocytokines such as interleukin-6 (IL-6), monocyte chemoattractant protei
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As disclosed in our preceding paper
2021-10-23

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, cyclic amp function
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