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br ATX LPA pathway in animal models of rheumatoid arthritis
2024-01-13
ATX–LPA pathway in animal models of rheumatoid arthritis Several animal models have been used to characterize the mechanisms involved in the pathogenesis of arthritis and to test new therapeutic strategies. The collagen-induced arthritis (CIA) model (Courtenay et al., 1980, Luross and Williams, 2
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Despite the growing knowledge surrounding the
2024-01-13
Despite the growing knowledge surrounding the link between ATX and cholestatic pruritus in PBC, it remains unclear if the role of the ATX-LPA signaling axis includes lymphocytes homing in the liver of PBC, and if the resulting inflammation is associated with PBC pruritus (Fig. 3). PBC is characteriz
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The tumor suppressor function of LOX in
2024-01-13
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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In previous years evidence emerged that inferred secondary
2024-01-13
In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic gnf (7) and piceatannol (8) (Fig. 3b) on mammalian arginase with IC50s of 10.6 a
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Consistent with the above prediction there
2024-01-12
Consistent with the above prediction, there are additional reports in which HMGA proteins have been demonstrated to facilitate recruitment of chromatin remodeling complexes to gene regulatory regions containing positioned nucleosomes during the transcriptional activation process. One particularly il
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STA-4783 Since artemisinin shows low solubility and poor ora
2024-01-12
Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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The functional significance of the
2024-01-12
The functional significance of the cap residues with regard to the established role of PfA-M1 in hemoglobin catabolism in the food vacuole is a key question that is difficult to address with in vitro studies. We note that three of the dipeptide substrates used in our study are found in the sequences
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In order to postulate its binding mode in
2024-01-12
In order to postulate its binding mode in APN, carboxypeptidase a 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupie
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br Discussion AhR is a receptor that binds
2024-01-12
Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds
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br Conclusions Several lines of evidence have been establish
2024-01-12
Conclusions Several lines of evidence have been established, which support the adenosine kinase hypothesis of epileptogenesis, which is based on a sequence of events leading from acute 3CAI injury to initial downregulation of ADK, rise in extracellular adenosine, changes in astrocytic adenosine
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br Introduction Adenosine deaminase ADA
2024-01-12
Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA
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Introduction Myasthenia gravis MG is an autoimmune disorder
2024-01-12
Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic Aloperine receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesis of MG. Exp
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In this paper we describe the formation of a
2024-01-12
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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AS-252424 br Acknowledgements This work was supported by the
2024-01-11
Acknowledgements This work was supported by the Victorian Government Operational Infrastructure Support Program. KAB is supported by the Mavis Robertson Fellowship from the National Breast Cancer Foundation (NBCF; ECF-16-004), by an NBCF Novel Concept Award (NC-14-011), and by NHMRC project grant
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In addition to calpain I activity cathepsin
2024-01-11
In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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