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In order to increase the oral bioavailability abiraterone is
2024-06-07

In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral ahr inhibitor of abiraterone acetate (156), it is recommended that this drug should be taken on
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Docking studies were performed on the selected compounds to
2024-06-07

Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-838
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Over the past decade extensive
2024-06-07

Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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The link between HPV infection and neoplasia has
2024-06-07

The link between HPV infection and neoplasia has been well established. HPV encodes two oncogenes (E6 and E7) that drive BAN ORL 24 progression by controlling the functions of tumor suppressor proteins p53 and Rb [7]. HPV is associated with more than 99% of cervical CESC cases [8]. CESC remains a m
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Recent findings imply that proper Na K
2024-06-07

Recent findings imply, that proper Na+/K+-ATPase function is crucial for unimpaired development of the vertebrate heart. Targeted knockout of Na+/K+-ATPase α1 in mice led to early embryonic lethality whereas heterozygous knockout mice displayed severe hypocontractile hearts [52]. Pharmacological inh
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br Disclaimer Statement br Acknowledgments br Introduction
2024-06-07

Disclaimer Statement Acknowledgments Introduction Metabolic changes are a common feature of cancerous tissues. Mutations in oncogenes and tumor suppressor genes cause alterations to multiple intracellular signaling pathways that rewire tumor cell metabolism and re-engineer it to allow enhan
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br Perspective AA LA and other PUFAs and
2024-06-07

Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path
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br Acknowledgements We would like to thank Dr Thomas
2024-06-07

Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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Applications for protein switches are numerous
2024-06-06

Applications for protein switches are numerous. In diagnostics, protein switches can detect analytes as components of inexpensive homogeneous assays that do not require specialized equipment or time-consuming incubation and washing steps characteristic of immunoassays [8]. Protein switches have also
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About three weeks later the patient visited our outpatient
2024-06-06

About three weeks later, the patient visited our outpatient clinic complaining of gingival bleeding and pus discharge. In clinical examination bone exposure was observed in both mandibular posterior regions and bone necrosis had developed surrounding the #35=37 and 46, 47 implants installed 6 years
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Regardless of the initial treatment most patients with advan
2024-06-06

Regardless of the initial treatment, most patients with advanced NSCLC experience relapse and disease progression [15]. A subpopulation of immediate concern and clinical need is patients who have advanced NSCLC that is especially aggressive, which is usually defined as disease that rapidly progresse
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Due to its unique histological
2024-06-06

Due to its unique histological architecture and blood supply, the lung is one of the most susceptible organs under uncontrolled systemic inflammatory circumstance [16]. Several studies have reported the anti-inflammatory benefits of metformin in acute lung injury induced by lipopolysaccharide (LPS),
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What is the mechanism by which Wnt a Fz
2024-06-06

What is the mechanism by which Wnt7a-Fz7 signaling enhances AMPAR localization and synaptic strength? Following induction of LTP, the number of AMPARs rapidly increases at extrasynaptic sites (Makino and Malinow, 2009, Yang et al., 2008a) through PKA-dependent phosphorylation of GluA1 at S845 (He et
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and LO are members of the lipoxygenase family that
2024-06-06

5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic trk inhibitor into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has shown that activation of t
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In conclusion this study detected the expression of adiponec
2024-06-06

In conclusion, this study detected the expression of adiponectin and its receptors, AdipoR1 and AdipoR2, in goat ovarian follicles. In addition, adiponectin was shown to enhance the progression of goat oocyte nuclear maturation in vitro. The present findings provide evidence for paracrine/autocrine
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