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Recently competitive inhibitors of arginase have been develo
2023-12-16

Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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Most human diseases e g
2023-12-16

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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The AT hook motif is highly conserved in
2023-12-16

The AT-hook motif is highly conserved in evolution from bacteria to humans and is found in one or more copies in a large number of other, non-HMGA, proteins, many of which are transcription factors or are involved in chromatin remodeling [8]. For example, AT-hook peptide motifs are essential compone
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br Acknowledgments br Protein microarrays were
2023-12-16

Acknowledgments Protein microarrays were developed to provide miniaturized high-throughput tools to study protein function, Mexiletine HCl receptor and post-translational modifications. Just a few years ago, the seminal work performed in Stuart Schreiber's laboratory at Harvard University () an
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br STAR Methods br Acknowledgments We
2023-12-15

STAR★Methods Acknowledgments We thank Simcere Pharmaceuticals, Nanjing, China, for providing a rabbit anti-VEGF neutralizing monoclonal antibody. We thank Dr. Schlisio in the Ludwig Institute for Cancer Research, Karolinska Institute, for assistance with hypoxia assay. Y.C.’s laboratory is sup
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Angiotensin I (human, mouse, rat) receptor Expression of Twi
2023-12-15

Expression of Twist1 and the AR are increased by oxidative stress, but the change in the receptor (mRNA/protein) is lost after treatment with siRNAs that target Twist 1 (Shiota et al., 2010). Twist 1 was found to bind to E-boxes, 5′-CANNTG-3′, in the proximal promoter (−442 to +51 bp) and upstream r
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br Acknowledgements This work was supported by Programme Gra
2023-12-15

Acknowledgements This work was supported by Programme Grants from the MRC and the Wellcome Trust (SGC-C and MF). CB was in receipt of a Marie Curie Intra-European Fellowship during part of this work. We thank past and present members of our group for numerous valuable discussions throughout these
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The RAS may have different functions
2023-12-15

The RAS may have different functions depending on whether we consider the circulatory component or the different local tissue systems (including brain) well described previously [29]. The cardiovascular control and hydroelectrolytic balance (among other functions), are largely the result of the infl
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br Discussion Herein we demonstrate that mice deficient in
2023-12-15

Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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Aldose reductase ALR EC the first enzyme
2023-12-15

Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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In conclusion we have shown that mGlu
2023-12-15

In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, Norfloxacin hydrochloride tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of no
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ADA catalyzes the deamination of adenosine and
2023-12-15

ADA catalyzes the deamination of adenosine and deoxyadenosine into their respective inosine nucleoside (Cristalli et al., 2001). This conversion is an initial step in a series of reactions responsible for lymphocyte proliferation and differentiation. Moreover, ADA is considered an indicator of cellu
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The zebrafish Danio rerio is a popular model
2023-12-15

The zebrafish (Danio rerio) is a popular model organism for virtually any biological function of vertebrates, and has, therefore, received a wide distribution in particular in developmental biology and toxicology (Strähle et al., 2012). With respect to AChE, the zebrafish has, e.g., been identified
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br Clinical realities br Commentary on uses
2023-12-15

Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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Fencilli et al reported derivatives of PHA
2023-12-15

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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