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Although the overall structures of mGlu and mGlu
2022-03-12
Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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To confirm the in vitro findings atorvastatin
2022-03-12
To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g
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While TUNEL staining is traditionally thought to be an
2022-03-12
While TUNEL staining is traditionally thought to be an apoptosis marker, studies have shown that TUNEL can stain necrotic Agarose GPG/ME australia [19], [20], [21]. Furthermore, DNA degradation has also been observed in necrotic cells [22]. TUNEL staining alone is therefore insufficient to distingui
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The experiments indicate that a major component of the vasod
2022-03-12
The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in ae3 preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but not in vessels preconst
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br Central control of GI ghrelin secretion The CNS
2022-03-12
Central control of GI ghrelin secretion The CNS communicates with the GI tract through the vagus nerve originating in the DMV and sympathetic spinal afferents emanating from the thoracic spinal chord (Bray, 2000). The cells that secrete peripheral ghrelin are under direct control of these two pat
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In early a collaborative effort between the
2022-03-12
In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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Prion diseases are transmissible and result in fatal neurode
2022-03-12
Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in Calcium Colorimetric Assay Kit australia lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion
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While histone modifications can alter
2022-03-11
While histone modifications can alter inter-nucleosomal interactions that govern the compaction state of a chromatin fiber (Francis et al., 2004, Kalashnikova et al., 2013, Lu et al., 2008), the potential impact of histone modifications on higher-order chromosome organization beyond chromatin-fiber
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br Materials and methods br
2022-03-11
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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In an effort to further
2022-03-11
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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It is difficult however to assure that
2022-03-11
It is difficult, however, to assure that observed alterations of pro-oxidant/antioxidant levels within the studied organisms are related directly to heavy metal pollution, rather than to other accompanying environmental stressors. Environmental factors like oxygen partial pressure, temperature, sali
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Interestingly studies from Sahai and colleagues in cancer
2022-03-11
Interestingly, studies from Sahai and colleagues in cancer-associated fibroblasts have revealed that YAP is required for the acquirement of a stiff ECM in the tumor microenvironment (Calvo et al., 2013). Subsequently, this stiffening of the matrix can activate YAP, thus creating a feed-forward loop.
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Mice lacking S nitrosoglutathione reductase GSNOR
2022-03-11
Mice lacking S-nitrosoglutathione reductase (GSNOR), a denitrosylase that regulates S-nitrosylation, have increased levels of S-nitrosoglutathione (GSNO) and exhibit nitrosative stress. GSNO is in equilibrium with protein S-nitrosylation in cells, and GSNOR controls the cellular concentration of pro
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br Conclusion In this report we describe
2022-03-11
Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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The atherosclerosis development requires additional pro infl
2022-03-11
The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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