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Tankyrase Inhibitors 22 Several in vivo and in vitro studies
2025-02-14
Several in vivo and in vitro studies have demonstrated changes in bioactive lipid profiles under hyperglycemic conditions and have linked these changes with increased leukocyte adhesion and vascular dysfunction during diabetes. This input has originated partly from lipidomic studies that showed elev
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Several studies have demonstrated that depletion of
2025-02-14
Several studies have demonstrated that depletion of functional ATR increases the sensitivity of cancer cells to oncogene-induced replication stress thereby hindering tumour growth and inducing extensive cell death (Gilad et al., 2010, Murga et al., 2011, Schoppy et al., 2012). Importantly, Schoppy e
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br Apelin Discovered in apelin was initially identified
2025-02-14
Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence
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Weak and transient interactions of HMGB proteins
2025-02-14
Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o
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br Selective Androgen Receptor Modulators SARMs
2025-02-14
Selective Androgen Receptor Modulators (SARMs) The AR and its endogenous ligands, androgens, are important for development and maintenance of muscle and bone, secondary sexual organs, and development of other tissues (Mooradian et al., 1987). Although androgens are important for normal developmen
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Immunohistochemistry Hearts from young and
2025-02-14
Immunohistochemistry: Hearts from young and aged mice were collected at the indicated times, fixed overnight in 10% formalin, and embedded in paraffin. Serial 5-μm heart sections from each group were analyzed. Samples were stained with H&E for routine histologic examination. Immunohistochemical stai
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Recently Kamoshita et al evaluated a mouse model of
2025-02-14
Recently, Kamoshita et al. (2016) evaluated a mouse model of retinal neuronal disturbance with the intraperitoneal injection of LPS and found that treatment with AICAR suppressed the reduction of conical function and decreased mRNA levels of TNF-α as well as improved mRNA levels of the mitochondrial
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Some of the earliest LOX inhibitors were
2025-02-13
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic Cy5 RNA (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+) st
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The mechanisms that control Ahr
2025-02-13
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic Diabetes medication receptor (RAR)-related orphan receptor γt] based on
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br Acknowledgments This work was supported by Grant in
2025-02-13
Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cul
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Another significant group of reductase inhibitors
2025-02-13
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic Verapamil HCl derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and an anioni
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br Introduction The process of mitosis is highly complex and
2025-02-13
Introduction The process of mitosis is highly complex and tightly regulated. This phase of the metaformin resulted in two identical daughter cells. The aurora kinases (aurora A, B, and C) are a family of three highly homologous serine-threonine protein kinases that play a key role in regulating
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NOS is classified into three isoforms endothelial eNOS neuro
2025-02-12
NOS is classified into three isoforms: endothelial (eNOS), neuronal (nNOS), and inducible (iNOS), iNOS is expressed in macrophages (Eisenstein, Huang, Meissler Jr, & al-Ramadi, 1994) and osteoblast-like cells (Riancho et al., 1995) and is involved in the regulation of inflammatory reactions (Eisenst
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Patients with cardiovascular disorders typically have lower
2025-02-12
Patients with cardiovascular disorders typically have lower plasma apelin levels than matched healthy controls. For example, plasma apelin levels are reduced in patients with coronary artery disease (CAD), and among CAD patients with unstable angina or acute myocardial infraction there is a further
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br Materials and methods br Results br Discussion Diabetic k
2025-02-12
Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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