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Regarding A Rs and A
2024-05-16
Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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Acknowledgements The work was supported
2024-05-15
Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic
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Our sample is representative of mRCC treated with sunitinib
2024-05-15
Our sample is representative of mRCC treated with sunitinib. However, the results from CCC setting have limited inference due to small exploratory sample (n = 51). Additionally, the significance of survival differences in CCC according to AXL staining is tangential. Unfortunately, we were unable to
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Previous studies have demonstrated that the expression of th
2024-05-15
Previous studies have demonstrated that the expression of the Aurora B gene is maximally increased at G2/M phage during mitosis (Honda et al., 2003, Fu et al., 2007, Goldenson and Crispino, 2015), and exhibits an extraordinary upregulation in a number of human cancers (Fu et al., 2007, Kollareddy et
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bace inhibitors Aurora A and B are required
2024-05-15
Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for t
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It is increasingly evident that many metabolic genes
2024-05-15
It is increasingly evident that many metabolic genes are associated with cancer progression of various tumor cells, including NSCLC. In particular, GLUT1 overexpression has been reported in NSCLC, and correlations between GLUT1 expression and a number of clinical parameters such as gender, smoking s
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A high throughput screening campaign led to the
2024-05-15
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Gefitinib hydrochloride br Polymorphic variation ERAP is
2024-05-15
Polymorphic variation ERAP1 is polymorphic and several single nucleotide polymorphisms (SNPs) in its gene that encode amino Gefitinib hydrochloride changes have been associated with predisposition to a variety of diseases, ranging from viral infections to cancer and autoimmunity (Alvarez-Navarro
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The preferential expression of ALOX B
2024-05-15
The preferential expression of ALOX15B in human macrophages may explain why human genetic studies investigating the association of ALOX15 with cardiovascular disease did not show consistent results. Two rare functional polymorphisms have been characterized in the ALOX15 gene, which leads to increase
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br Conflict of interest br Acknowledgement This
2024-05-14
Conflict of interest Acknowledgement This study was supported by a grant from University Grants Commission - Basic Scientific Research (UGC-BSR), New Delhi, India (UGC-BSR No:F-7-115/2007). Introduction The G protein-coupled receptors activated by extracellular adenosine (Ado), called Aden
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br Conclusions and clinical relevance Astrogliosis and an in
2024-05-14
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic E-64-d is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK inhibit
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There has been growing interest
2024-05-14
There has been growing interest over computational methods to predict the biological activity by chemical structure, so as to decide whether it kinase inhibitors has objective qualities or not. In this contribution, the well-known method, which is called quantitative structure–activity relationship
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CT-99021 br Materials and methods Bacterial strains and grow
2024-05-14
Materials and methods Bacterial strains and growth conditions. Escherichia coli TOP10 and E. coli BL21Star (DE3) (ThermoFisher, Waltham, MA) were grown at 37 °C in Luria broth (LB) or LB-agar containing kanamycin (50 μg/ml). Bioinformatic analyses. The amino CT-99021 sequence of Rv2477c was obt
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Aurora A or B selective and pan
2024-05-14
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Consistent with a damaging role for increased LOX activity
2024-05-14
Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he