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Compound was synthesized in a racemic fashion with this
2021-10-02

Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position
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The previous study demonstrated that
2021-10-02

The previous study demonstrated that the main CYP isoforms present in the human mmp endocrinology included CYP46A1, 2J2, 2U1, 1B1, 2E1 and 2D6 (Dutheil et al., 2009b, 2010). CYP1B1 and CYP2U1 were found in the mitochondrial and microsomal fractions of astrocytes in the human frontal lobe, hippocamp
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Recent studies revealed that synthetic
2021-10-02

Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast
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uPAR promotes cell associated proteolysis
2021-10-01

uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot
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Tetrazole is one of the most commonly used bioisosteres
2021-10-01

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Conclusion In conclusion our results demonstrate
2021-10-01

Conclusion In conclusion, our results demonstrate that incubation of both LAD and SCA rat coronary arteries rapidly increases the ETB receptor-mediated contraction as well as upregulation of ETB receptor protein levels. These findings may have important experimental implications in tissue bath ex
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Histone acetylation is regulated by two groups of
2021-10-01

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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xav The fibulins are a newly abundantly in the basement
2021-10-01

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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The experiments reported herein were
2021-10-01

The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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The mechanisms of action of
2021-10-01

The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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Elevated methylglyoxal levels also contribute
2021-10-01

Elevated methylglyoxal levels also contribute to carbonyl stress, cytotoxicity, DNA damage, apoptosis and cell death. These mechanisms may be important for normal aging of the nervous system as well as for the development of neurodegenerative diseases such as Alzheimer's and Parkinson's disease wher
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substance p australia br Investigations br Genetics GLUT is
2021-10-01

Investigations Genetics GLUT1 is a membrane-bound glycoprotein that provides base-rate glucose transport across blood-tissue barriers. It is constituitively expressed in erythrocytes, substance p australia microvessels and astroglia. The gene exclusively associated with GLUT1 is SLC2A1, locat
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br Acknowledgments This research was
2021-10-01

Acknowledgments This research was supported by a grant from the Korea Health Technology R&D Project through the Korean Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI17C0616). Dr. Jun-Mo Yang was supported by the Natio
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AZD-5438 br Experimental br Acknowledgments This project was
2021-10-01

Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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In type diabetic subjects with mean
2021-10-01

In type-2 diabetic subjects with mean baseline glycated hemoglobin A (HbA) of 8.4%, q.d. administration of MK-0893 for 12weeks as a monotherapy resulted in dose-dependent decreases in HbA and FPG. Administration of MK-0893 q.d. at doses of 20, 40, 60, and 80mg led to observed reductions in HbA of 0.
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