• The potential use of derivatives belonging to this

  2024-04-07

  

  The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore

• AdK as an important upstream regulator of adenosine based ho

  2024-04-07

  

  AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi

• br Acknowledgments We thank the anonymous reviewers for thei

  2024-04-03

  

  Acknowledgments We thank the anonymous reviewers for their constructive comments on the manuscript, and also thank Dr. Hans-U. Dahms for his comments on the manuscript. This work was supported by a grant from the National Research Foundation (2009-0071218) funded to Young-Mi Lee. This work was al

• Axl which belongs to the Tyro Axl Mer TAM

  2024-04-03

  

  Axl, which belongs to the Tyro-Axl-Mer (TAM) family of RTKs, has been reported to regulate a variety of physiological processes including cell survival, proliferation, migration and adhesion, through the activation of the phosphoinositide 3-kinase (PI3K)/V-akt murine thymoma viral oncogene homolog (

• SKF 96365 hydrochloride synthesis Physiological total plasma

  2024-04-03

  

  Physiological total plasma LPA levels are normally less than 1μM in healthy subjects. LPA levels have been reported to be increased in malignant effusions or plasma in cancer patients [20]. In addition, increasing ATX activity detected in healthy pregnant women in the third trimester of pregnancy ex

• Thiorphan br Aurora A Aurora B and

  2024-04-03

  

  Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig

• Ryoichi et al modified potent clinical

  2024-04-03

  

  Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos

• In considering the roles of these enzymes in normal

  2024-04-03

  

  In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty Calphostin C synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes results in a surpr

• In the pituitary of R quelen mRNA levels of

  2024-04-03

  

  In the pituitary of R. quelen mRNA levels of cyp19a1b were found to be higher in males than females, suggesting a sex-specific function, and perhaps a local action to regulate gonadotropins or other pituitary hormone secretion (Olivereau and Callard, 1985; Zhang et al., 2014). Interestingly, the hig

• CORT induced hippocampal damage has been implicated in

  2024-04-03

  

  CORT-induced hippocampal damage has been implicated in depression, aging and long-term glucocorticoid therapy. Therefore, finding a drug that can protect hippocampal neurons from the adverse effects of CORT could have significant clinical benefits. In this regard, we tested the potential protective

• Another hypothesis is angiogenesis inhibition

  2024-04-03

  

  Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial cathepsin g to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in tumor met

• Since ARBs strongly reduce inflammation it was

  2024-04-03

  

  Since ARBs strongly reduce inflammation, it was hypothesized that the protective effects on cognition were the result of reduction of inflammation and amelioration of neurogenic decrease. However, ARB treatment did not normalize increased inflammation and neurogenic loss. For this reason, the protec

• Recently the FDA approved the first

  2024-04-03

  

  Recently, the FDA approved the first blood-based test for the detection of EGFR mutations in non-small cell lung cancer patients (http://www.fda.gov) (Voelker, 2016). This allows detection of specific, recurrent mutations, which can help the selection of the patients that could benefit from Erlotini

• AMP activated protein kinase AMPK is composed of and subunit

  2024-04-03

  

  AMP-activated protein kinase (AMPK) is composed of α-, β-, and γ-subunits [17,18]. Phosphorylation of α-subunit at Thr-172 residue is essential for AMPK activation [17,18]. The serine/threonine kinase coordinates metabolic pathways in response to energy supply and demand [17,18]. Studies have shown

• Furthermore to address the concern that the observed positiv

  2024-04-03

  

  Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo

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