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The pharmacokinetics properties of compound were evaluated i
2019-10-02
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability (
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Nimodipine clinical br Discussion Cytomegalovirus CMV is a h
2019-10-02
Discussion Cytomegalovirus (CMV) is a herpes virus that causes primary infection in normal hosts and re-activation infection in compromised hosts with impaired CMI, e.g., organ transplants. Following primary infection, which may be severe, CMV becomes latent in lymphocytes. Reactivation may occur
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ET expression occurs in many carcinomas including those
2019-10-02
ET-1 expression occurs in many carcinomas, including those arising in the kidney [38], prostate [7], ovary [5] endometrium [39], melanocyte [40], and central nervous system [41], [42], among others [43]. The endothelin axis expression in RCC appears to be dependent upon the tumor subtype [38]. In se
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br Experimental Procedures br Author Contributions
2019-10-02
Experimental Procedures Author Contributions M.M. and M.T. designed and supervised the study. S.I. conducted the analysis on NOG-rd mice. H.-Y.T., M.F., and T.M. conducted and analyzed MEA. S.I., H.-Y.T., and M.M. performed 3D image analysis. N.K., T.K., M.G., and R.T. planned and established
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Given that dimethylamine substitution was tolerated as in
2019-10-02
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated Y-27632 amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The slig
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br Introduction Hematopoietic stem cells and
2019-10-02
Introduction Hematopoietic stem d ap5 and leukemic stem cells (HSCs and LSCs, respectively) both have a capacity of self-renewal. Whereas HSCs give rise to all blood lineages during lifetime hematopoiesis, LSCs are responsible for the initiation and propagation of leukemia, as well as drug resis
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It is interesting to note that Eibinger and
2019-10-01
It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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Direct coupling between DNA methyltransferase
2019-10-01
Direct coupling between DNA methyltransferase enzymes and posttranslational modifications on histone proteins has been observed in mammals. For example, DNMT3A recognizes unmodified H3 through an ATRX-DNMT3-DNMT3L (ADD) domain, and its activity is inhibited by methylation of H3 at K4 (Li et al., 201
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Atg cleaves Atg at the peptide bond on
2019-10-01
Atg4 cleaves Atg8 at the peptide bond on the glycine residue at the C-terminus, thus allowing the conjugation of Atg8 to phosphatidylethanolamine (PE) with the participation of other autophagy molecules. Atg4 can also serve as a deconjugating enzyme, which cleaves the amide bond of the conjugated At
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Introduction The first reference to a possible involvement
2019-10-01
Introduction The first reference to a possible involvement of orexins in the effects of drugs of abuse appeared in 2003 and showed that orexigenic peptide neurons respond to the chronic administration of morphine followed by abrupt withdrawal symptoms caused by opioid receptor antagonists (Georgesc
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It should be noted that the long lifetime binding
2019-10-01
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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Rat pheochromocytoma PC cells have been widely used
2019-10-01
Rat pheochromocytoma PC12 cells have been widely used as a cell system to study intracellular signaling leading to neurite outgrowth. The advantages of using PC12 cells in the CHK studies are the fact that they naturally express the rat form of CHK and the observation that down-regulation of CHK fun
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br In patients with type I
2019-10-01
In patients with type I diabetes mellitus poor management causes/INS; a drastic rise in glucose levels resulting in diabetic ketoacidosis (DKA). About 1% of DKA episodes can be complicated by cerebral edema. ET and its receptors are involved in the regulation of /INS;cerebral blood flow. We studie
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For this reason downstream components of the inflammatory
2019-10-01
For this reason, downstream components of the inflammatory pathway have been investigated in the search for alternative targets. Targeting such downstream elements might result in safer and more tolerable analgesics. PGE mediates its effects through binding to four G-protein-coupled receptors (EP1-
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br Early developments Historically the advent
2019-10-01
Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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