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#27633918   2016/09/16 Save this To Up

An inhibitor of the acetyltransferases CBP/p300 exerts antineoplastic effects on gastrointestinal stromal tumor cells.

Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal neoplasm featured by activated mutations of KIT and PDGFRA. Although overall survival rates have greatly improved by the development of receptor tyrosine kinase inhibitors, most patients ultimately acquire resistance due to secondary mutations of KIT or PDGFRA. Inhibition of the histone acetyltransferases (HATs) CREB‑binding protein (CBP) and p300 results in antineoplastic effects in various cancers. To determine whether CBP/p300 can serve as an antineoplastic target for GISTs, specific short interfering RNA sequences and the selective HAT inhibitor C646 were administered to GIST882 cells. Cell viability, apoptosis and the cell cycle were analysed using the Cell Counting Kit-8, a caspase-3/7 activity assay or Annexin V-fluorescein isothiocyanate/propidium iodide (PI) staining and PI staining. Gene and protein expression levels were measured by quantitative real-time polymerase chain reaction and western blotting, respectively. Transcriptional blockage of CBP, rather than p300, resulted in suppression of cell proliferation. Interestingly, both CBP and p300 depletion enhanced caspase-3/7 activity. A lack of CBP and p300 caused ETS translocation variant 1 (ETV1) downregulation and KIT inhibition in GIST cells. Nevertheless, the absence of CBP, not p300, leads to extracellular signal-regulated kinase 1/2 inactivation and c-Jun NH2-terminal kinase activation, suggesting a more crucial role for CBP than p300 in cell proliferation and survival. Furthermore, proliferation of GIST cells was reduced by administration of C646, a selective HAT inhibitor for CBP/p300. Apoptosis induction and cell cycle arrest were detected after exposure to C646, indicating that its antitumor activities were supported by its antiproliferative and proapoptotic effects. Additionally, C646 treatment attenuated ETV1 protein expression and inactivated KIT-dependent pathways. Taken together, the present study suggests that CBP/p300 may serve as novel antineoplastic targets and that use of the selective HAT inhibitor C646 is a promising antitumor strategy for GISTs.

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#25665416   2015/02/10 Save this To Up

[Excessive fluoride inducing calcium overload and apoptosis of ameloblasts].

To study the effect of excessive fluoride on calcium overload and apoptosis in cultured rat ameloblasts in vitro.

2305 related Products with: [Excessive fluoride inducing calcium overload and apoptosis of ameloblasts].

Calcium fluoride CAS Numb Anti-Apoptosis-Inducing F Anti Apoptosis Inducing F Apoptosis Inducing Factor Apoptosis Inducing Factor Apoptosis Inducing Factor Apoptosis Inducing Factor Calcium Stain Kit (Modif Calcium Stain Kit (Modif Androgen Receptor (Phosph Androgen Receptor (Phosph Rabbit Anti-Human Androge

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#19029664   2008/11/25 Save this To Up

Preparation of antibody against horseradish peroxidase using hybridoma technology.

Monoclonal antibody against horseradish peroxidase (HRP) has many applications which peroxidase anti-peroxidase. Peroxidase-antiperoxidase (PAP) complex formation is its most known and important usage. This complex is used in many immunohistochemical and immunocytochemical staining techniques.

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#18325031   2008/04/18 Save this To Up

Montelukast inhibits tumour necrosis factor-alpha-mediated interleukin-8 expression through inhibition of nuclear factor-kappaB p65-associated histone acetyltransferase activity.

Montelukast is a potent cysteinyl leukotriene-1 receptor antagonist possessing some anti-inflammatory effects although the molecular mechanism of these anti-inflammatory effects is unknown. In this study, we aimed to investigate the effect of montelukast on nuclear factor (NF)-kappaB-associated histone acetylation activity in phorbol myristate acetate (PMA)-differentiated U937 cells.

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#16424596   2006/01/20 Save this To Up

Production of monoclonal antibody against alkaline phosphatase.

Monoclonal antibody against alkaline phosphatase (Alp) has many applications which Alp-anti Alp complex (APAAP) formation is one of the most important ones. This complex is applicable in many immunohistochemical and immunocytochemical techniques such as diagnosis of various kinds of leukemias, lymphomas, skin diseases, kidney dysfunctions, etc.

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