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The cavity volume of the binding
2024-06-11
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino brain natriuretic peptide substitution within a binding pocket may result in a change in the cavity volume. This, i
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Introduction Diabetic nephropathy is a rapidly growing cause
2024-06-11
Introduction Diabetic nephropathy is a rapidly growing cause of end-stage renal disease [1]. Glomerular, tubular and vascular toxicity resulting from hyperglycemia (glucotoxicity) have been evaluated extensively at the molecular level as contributing factors for diabetic nephropathy [[1], [2], [3]]
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KU55933 mg The acetylcholinesterase AChE inhibitor tacrine T
2024-06-11
The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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br Methods br Results br Discussion br Acknowledgements br
2024-06-11
Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V
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Previous studies have demonstrated that the
2024-06-11
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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Phagosomes acquire some hydrolases early
2024-06-11
Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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br Materials and methods br Results br
2024-06-11
Materials and methods Results Discussion Human MutL-family complexes (MutLα: MLH1-PMS2, MutLβ:MLH1-PMS1, MutLγ:MLH1-MLH3) exhibit multiple molecular activities including DNA binding, DNA cleavage, ATP binding and hydrolysis [43]. In our recent study, we have uncovered an important function
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It has also been reported that defects in ATM or
2024-06-08
It has also been reported that defects in ATM or ATR signalling are synthetically lethal with PARP inhibition (Turner et al., 2008, Peasland et al., 2011, Yap et al., 2011, Michels et al., 2014), suggesting that combined inhibition of PARP and ATM or ATR may be an effective therapeutic strategy. In
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Based on its kinetic parameters and quaternary structure
2024-06-08
Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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br Funding br Introduction Plants absorb both inorganic
2024-06-07
Funding Introduction Plants absorb both inorganic nitrogen (ammonium and nitrate) and organic nitrogen (amino acids and peptides) from the soil [1]. The first organic nitrogenous molecule produced from inorganic nitrogen is Gln, whose terminal amino group is successively transferred to make Gl
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The beneficial treatment with several statins have been eval
2024-06-07
The beneficial treatment with several statins have been evaluated in AD patients (Kivipelto et al., 2005), with controversial results. It has been suggested that statins slow cognitive decline in mild to moderate AD (Miida et al., 2005). Treatment with atorvastatin, combined with other medications,
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Adenosine is an endogenous nucleoside that plays pivotal rol
2024-06-07
Adenosine is an endogenous nucleoside that plays pivotal roles in different physiological and pathophysiological processes by triggering specific cell-surface receptors both in the IC-87114 and in the periphery. The adenosine receptors (ARs) are four different subtypes of G protein-coupled receptors
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In the presence of detrimental
2024-06-07
In the presence of detrimental conditions, such as inflammation, hypoxia, ischemia trauma or neoplastic milieu, the extracellular levels of adenosine increase massively, reaching micromolar range [51,52]. In these pathological contexts, adenosine accumulation stems from increased extracellular depho
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mek inhibitors Our initial approach to identify hits was two
2024-06-07
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI mek inhibitors library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility w
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As mentioned above variation of the
2024-06-07
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to Metabolism Compound Library (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () hav
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