• Aurora kinases are a conserved family of

  2025-02-17

  

  Aurora kinases are a conserved family of serine/threonine kinases that are important for the transition through mitosis and amplification and overexpression of Aurora kinases have been implicated in CPI-203 and transformation. Aurora B is located at the centromere and controls aspects of kinetochor

• br Author contributions br Acknowledgments TJC KW and VG

  2025-02-17

  

  Author contributions Acknowledgments TJC, KW, and VG are supported by awards made to MJN: a Consolidator Grant from the European Research Council under Grant no. 311336; a University Research Fellowship from the Royal Society, and a Career Development Award from the Human Frontiers Science Pro

• At the outset of targeting the

  2025-02-17

  

  At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am

• Apelin APJ triggers a variety of cellular

  2025-02-15

  

  Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si

• It has been proven that genetic

  2025-02-15

  

  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

• The objectives of this study were to investigate

  2025-02-15

  

  The objectives of this study were to investigate 1) the mRNA and protein expression of apelin and APJ in porcine ovarian follicles of different sizes, and their immunolocalization and concentrations in follicular fluid and ovarian follicle, and 2) the direct effect of recombinant human apelin-13 on

• In recent years the higher lipophilicity thus better

  2025-02-15

  

  In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty Sitafloxacin esters of nat

• Other reports however have indicated that all components of

  2025-02-15

  

  Other reports, however, have indicated that all components of RAS are produced within the central nervous system (CNS) (Saavedra, 2005). Thus, AGTR1 and AGTR2 in circumventricular organs and in cerebrovascular endothelial cells may respond to circulating ANG2 of peripheral origin, whereas neural rec

• br AMPK as a druggable target AMPK signaling has attracted

  2025-02-15

  

  AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in

• The beneficial treatment with several statins have been eval

  2025-02-15

  

  The beneficial treatment with several statins have been evaluated in AD patients (Kivipelto et al., 2005), with controversial results. It has been suggested that statins slow cognitive decline in mild to moderate AD (Miida et al., 2005). Treatment with atorvastatin, combined with other medications,

• Zoniporide hydrochloride br AHR mediates TCDD toxicity and

  2025-02-15

  

  AHR mediates TCDD toxicity and wasting syndrome TCDD causes numerous toxicities in laboratory animals, including teratogenesis, hepatic steatosis, thymic atrophy, immune dysfunction and a lethal wasting syndrome [17]. The dose-dependent sensitivity to TCDD-induced toxicities varies widely among l

• br Impact of global AHR

  2025-02-15

  

  Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s

• One study has demonstrated that PUFA reduced

  2025-02-15

  

  One study has demonstrated that ω-3 PUFA reduced both cholesterol and caveolin-1 (a marker of raft), thereby displacing raft-associated signaling molecules from lipid raft [36]. Additionally, DHA treatment decreased the amount of lipid raft in the cell surface and displaced several lipid raft-associ

• CGP 42112 br Perspectives and challenges Previously the main

  2025-02-15

  

  Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular

• The same applies also to intermediate formally obtained

  2025-02-15

  

  The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char

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