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Analysis of the enzyme activity expressed as rate of product
2023-11-14
Analysis of the enzyme activity, expressed as rate of product formation per unit serum volume (20μl), between the diagnostic groups revealed that ApB activity was significantly decreased in the patient group both at recruitment and after 13months when the substrate concentration used was 1.5mM (peth
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Dose Response Studies Against Puromycin Sensitive
2023-11-14
Dose–Response Studies Against Puromycin–Sensitive Aminopeptidase (PSA). PSA is a ubiquitous metallopeptidase encoded by the NPEPPS gene with subcellular distribution in the cytosol and nucleus [49]. Comprising of a 919 amino 69 2 australia sequence, it has a broad substrate specificity, and is resp
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Pregnane X receptor PXR is a nuclear receptor that
2023-11-14
Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli
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salubrinal br Materials and methods br
2023-11-13
Materials and methods Results Discussion More experiments were performed in order to explain the mechanism that is involved in salubrinal death both PC3 and Hep G2 cells using compound 5. Results showed that this compound inhibits cell viability inducing apoptosis in a concentration-depend
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-11-13
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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br Introduction Myasthenia gravis MG is an autoimmune
2023-11-13
Introduction Myasthenia gravis (MG) is an autoimmune disease characterised by failure of transmission at the neuromuscular junction (NMJ). In 80–85% of myasthenia gravis patients, the disease is mediated by antibodies to the nicotinic p2x receptors receptor (AChR; (Lindstrom et al., 1976). Many
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Compounds were profiled for their
2023-11-13
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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The inhibition of ACLY induces an anticancer effect that
2023-11-13
The inhibition of ACLY induces an anticancer effect that has been reported to be involved in mitochondrial reactive oxygen species (ROS) generation [14], [16], dual blockade of mitogen-activated protein kinase and phosphatidylinositol-3-kinase/AKT pathways [11], and the glycolytic phenotype of tumor
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Demonstration of in vivo efficacy of potential chemopreventi
2023-11-13
Demonstration of in vivo efficacy of potential chemopreventive agents in animal models is necessary for their clinical development. Our present study provides experimental evidence that CuB 0.1μmol by oral administration (for 2weeks before the cancer cell injection, 5days per week) significantly inh
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Recently competitive inhibitors of arginase have
2023-11-13
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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br Physiology of the apelin pathway br Role
2023-11-13
Physiology of the apelin pathway Role of apelin in heart disease Both apelin and apelin receptor null mice manifested moderate reduction in cardiac contractile function under basal conditions and their exercise capacity was markedly reduced (Table 1) [56]. Apelin has direct effects on the prop
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Later on Wayner Burton Ingold Barclay and Locke
2023-11-13
Later on, Wayner, Burton, Ingold, Barclay, and Locke (1987) modified the method by using lipid to examine the ability of an antioxidant NVP-BEP800 protect against lipid peroxidation generated by azo-compound. It was later improved using β-phycoerythrin (β-PE) as a fluorescent probe, and the ability
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This progressive behaviour is summarized in Fig
2023-11-13
This progressive behaviour is summarized in Fig. 4, which depicts the variation in convexity of the obtained cut-off patterns for the series of six antioxidants. The form and degree of convexity of the obtained cut-off curves should in principle correlate with the AOs hydrophobicities, and therefor
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br HIF Blockade in AA Therapy In
2023-11-13
HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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In the largest postmortem study of autopsied individuals alm
2023-11-13
In the largest postmortem study of 3618 autopsied individuals, almost 75% of the individuals without Aβ pathology already harbored cortical NFT pathology mostly confined to the medial temporal regions (Murray et al., 2015). In Braak's study of 2366 autopsied individuals (Braak and Del Tredici, 2014)
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