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Crystal structures were obtained of sulfonamide and
2024-04-22
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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It has been proven that genetic polymorphisms
2024-04-22
It has been proven that genetic polymorphisms can play an important role in development of hypertension and CVDs. In a Turkish population-based study, it was found that the APLNR gene (rs948847-A445C) polymorphism was not associated with coronary artery disease (CAD), but it was shown to be related
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Linagliptin is a recently approved dipeptidyl peptidase
2024-04-22
Linagliptin is a recently approved dipeptidyl peptidase-4 (DPP-4) inhibitor and widely considered as first-line treatment for patients with type 2 diabetes. DPP-4 is responsible for the inactivation of incretin hormones, such as glucagon-like peptide 1 (GLP-1). GLP-1 is released by the intestine aft
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Clinical observations of individuals with a decrease in LOX
2024-04-22
Clinical observations of individuals with a decrease in 12-LOX wdr5 are consistent with 12-LOX potentiating platelet activation and thrombus formation [40]. However, the relative contribution of 12-LOX to these complex disorders cannot be fully elucidated in the absence of a biochemical assessment o
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APN accounts for of total plasma proteins in
2024-04-19
APN accounts for 0.01% of total plasma proteins in humans; this proportion increases with age to a small extent (Barb et al., 2007). Normal APN levels in the circulation range 3–30μg/mL (Aprahamian and Sam, 2011). APN levels are lower in men than women due to the presence of testosterone and even mo
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br Materials and methods br
2024-04-19
Materials and methods Results Discussion More experiments were performed in order to explain the mechanism that is involved in thymidine phosphorylase death both PC3 and Hep G2 cells using compound 5. Results showed that this compound inhibits cell viability inducing apoptosis in a concent
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Caffeic acid dihydroxycinnamic acid is a natural compound
2024-04-19
Caffeic Perhexiline maleate (3,4-dihydroxycinnamic acid) is a natural compound that inhibits 5-LO and exerts potent anti-inflammatory and antioxidant properties. Recently, Takeda et al. reported that caffeic acid provided neuroprotective and anti-depressive activities [23]. Sertraline, a selective
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A review has recently been published
2024-04-19
A review has recently been published to evaluate the potential effects of food, alcohol and epirubicin juices on the pharmacokinetics and pharmacodynamics of the drugs for BPH. The authors reviewed the PubMed database during the years 1991–2015. In addition, a digital version of Stockley on drug in
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MK-2206 Demonstration of in vivo efficacy
2024-04-19
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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In considering the roles of these enzymes in normal
2024-04-19
In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty colorimetric synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes results in a surpr
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Earlier studies showed that exposure of cells
2024-04-19
Earlier studies showed that exposure of cells to IR caused ATM-dependent phosphorylation of 53BP1, as judged by electrophoretic mobility shift [24], [25], [26]. To date, the only known in vivo 53BP1 phosphorylation site(s) are Ser25 and possibly Ser29 [27]. In the course of our studies, we noticed t
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Recent studies have demonstrated that in response
2024-04-19
Recent studies have demonstrated that in response to IR, hundreds of substrates are phosphorylated in an ATM-dependent manner, clearly demonstrating the complexity of the ATM-mediated DDR pathways (Matsuoka et al., 2007, Bennetzen et al., 2010, Bensimon et al., 2010). However, evidence suggesting th
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Human hepatocyte transplantation resulted in some animals
2024-04-19
Human hepatocyte transplantation resulted in some animals with relatively sparse repopulation while others had >90% of their liver containing human hepatocytes. The presence of circulating human albumin varied based on the amount of repopulation as the degree of humanization is reported to correlate
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br Introduction Hepatocellular carcinoma HCC
2024-04-19
Introduction Hepatocellular carcinoma (HCC) is an aggressive and malignant cancer detected in clinical practice, as it is the third key reason of tumor-related deaths worldwide, with > 800, 000 mortalities every year (Torre et al., 2015). Current treatments for HCC are surgical therapy, liver tra
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Most human diseases e g cancer diabetes
2024-04-19
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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