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Among the enzymes involved in adenosine metabolism
2025-01-10

Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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Introduction The first use of the term autophagy by
2025-01-09

Introduction The first use of the term “autophagy” by a French physiologist, M. Anselmier, in a short article describing the effects of fasting in mice published in 1859, took place almost a century before Christian De Duve described it from a mechanistic point of view in a symposium on lysosomes i
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Demonstration of in vivo efficacy of
2025-01-09

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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ATP citrate lyase ACLY is a cytosolic enzyme that
2025-01-09

ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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Molecular simulation has proven useful
2025-01-09

Molecular simulation has proven useful in describing the dynamics and energetics of NMDA receptor LBD cleft closure and the potentiating role of glycans (Yao et al., 2013, Dai and Zhou, 2013, Dai and Zhou, 2015, Dai and Zhou, 2016, Dutta et al., 2015, Omotuyi and Ueda, 2015, Sinitskiy and Pande, 201
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Receptor Subtypes and Their Function Critical Appraisal Larg
2025-01-09

Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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br Dysregulated aromatase expression the link between
2025-01-09

Dysregulated aromatase expression: the link between obesity and breast cancer Obesity has been associated with abnormally high expression of the enzyme aromatase in the breast, influencing the local production and bioavailability of estrogens (Morris et al, 2011, Subbaramaiah et al, 2012). Bowers
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Currently NSAIDs which achieve antineoplastic actions mainly
2025-01-09

Currently, NSAIDs which achieve antineoplastic actions mainly through apoptosis are emerging choice in chemotherapy. Their antineoplastic effects were demonstrated before in tumor-bearing models [5], [6], [7]. Through in vitro cell models, we identified an indomethacin-activation of ceramide/PP2A/Ak
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Several strategies have been employed to design
2025-01-09

Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, SCR 7 induces changes in the spectral properties of the fluorophore(s) incorporated into the
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br Technical Note Fungal spoilage of dairy
2025-01-09

Technical Note Fungal spoilage of dairy products remains a major concern for dairy manufacturers despite the use of preventive and control approaches, including the use of chemical preservatives. Among methods that are increasingly used by industries for microbial contaminant control, biopreserva
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br Small molecule homoisoflavonoid in combination with anti
2025-01-09

Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m
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Earlier studies showed that exposure of
2025-01-08

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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Thus phosphorylation of p was used to measure
2025-01-08

Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc VRT752271 synthesis expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [3
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A combination of factors might
2025-01-07

A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to iden
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Taken together BRP represents a novel chemotype of LT biosyn
2025-01-07

Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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