• Apelin induced G i activation has been demonstrated as

  2024-06-21

  

  Apelin induced Gαi activation has been demonstrated as a benefiting effect on cardiac contractility [12], [38], [39], and a vasodilator activity that protects against angiotensin-II-induced cardiovascular fibrosis and atheroma [40], [41]. In contrast, stretch causes hypertrophy through diminishing G

• AP was originally described as a

  2024-06-21

  

  AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi

• br Acknowledgments br Introduction Alzheimer s disease AD is

  2024-06-21

  

  Acknowledgments Introduction Alzheimer's disease (AD) is a severe neurodegenerative disorder primarily affecting the elderly population. Senile plaques in the brain, one of the pathological hallmarks of AD, are formed by the accumulation of aggregated β-amyloid (Aβ) with an extensive β-sheet s

• Application of the broad acting HTR antagonist

  2024-06-20

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• The biology of the A BR is complex

  2024-06-20

  

  The biology of the A2BR is complex and needs to be considered contextually as the expression and effect of receptor engagement varies according to time post hypoxic injury, cell type and downstream signaling pathway. For example, A2BR expression is dynamic - low under basal and increasing under isch

• The hippocampus is the primary brain structure

  2024-06-20

  

  The hippocampus is the primary brain structure involved in learning and memory. The role of hippocampal synaptic plasticity in neurological processes in cognition and depression has been extensively demonstrated. Synaptophysin is a critical substance in synaptogenesis, which is necessary for learnin

• The most potent compounds within the current

  2024-06-20

  

  The most potent compounds within the current series of compounds were therefore , , , , and , with 8-Methoxypsoralen synthesis possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM aga

• The synthesis and secretion of adrenal androgens

  2024-06-20

  

  The synthesis and secretion of adrenal androgens is apparently unique to humans and nonhuman primates, and requires the expression of key mediators such as CYP17 [26]. Endocrine control of CYP17 expression in rhesus monkeys is comparable to that in humans [27]. An analysis of baboon cDNA for CYP17 s

• Our previous studies found that some steroid mimetic

  2024-06-20

  

  Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du

• br Acknowledgements We thank Dr Stefan Schulte Merker and

  2024-06-20

  

  Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific

• Inactivation of the proton pump comes with luminal alkaliniz

  2024-06-20

  

  Inactivation of the proton pump comes with luminal alkalinization of the targeted vesicles such as lysosomes (Fig. 2b). Lysosome pH can also be raised stoichiometrically by addition of a membrane-permeable weak Cyclo(RGDyK) such as methylamine or chloroquine which accumulates in its protonated, non

• A large number of studies have shown

  2024-06-20

  

  A large number of studies have shown that oxidative stress is involved in the pathophysiological process of ventricular remodeling and is associated with left ventricular dysfunction (Hori and Nishida, 2009, Lord et al., 2010). The generation of reactive oxygen species (ROS) that exceeds anti-oxidat

• The mitogen activated protein kinase

  2024-06-20

  

  The mitogen-activated protein kinase (MAPK) plays an important role in a variety of cell processes by controlling transcriptional or translational regulation [14]. There are three major MAPK family members that have been well characterized: extracellular signal-regulated kinase (ERK), c-Jun N-termin

• br Material and methods br Results

  2024-06-20

  

  Material and methods Results Discussion Asparagine, arginine, leucine, methionine, and glutamine are the essential N1-Methyl-ATP for cancer cells and intensively investigated for the development of selective targeted therapeutics. Among them, asparagine depleting bacterial enzyme asparagina

• The results of our in vivo experiments provide promising

  2024-06-19

  

  The results of our in vivo experiments provide promising evidence that the apelin/APLNR axis is implicated in CCA growth and that targeting this axis with a receptor specific antagonist may help develop effective, tumor directed therapies. Not only do we show decreased proliferation and angiogenesis

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