Protein kinase CK2--a key suppressor of apoptosis.

Cellular and Molecular Biochemistry Research Laboratory (151), V.A. Medical Center, Department of Laboratory Medicine and Pathology, University of Minnesota, Minneapolis, MN 55417, USA.
Advances in enzyme regulation 05/2008; 48:179-87. DOI: 10.1016/j.advenzreg.2008.04.002
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    ABSTRACT: In this work, the quantitative structure-activity relationship models were developed for predicting activity of a series of compounds as CK2 inhibitors using multiple linear regressions and support vector machine methods. The data set consisted of 48 compounds was divided into two subsets of training and test set, randomly. The most relevant molecular descriptors were selected using the genetic algorithm as a feature selection tool. The predictive ability of the models was evaluated using Y- randomization test, cross-validation and external test set. The genetic algorithm- multiple linear regression model with six selected molecular descriptors was obtained and showed high statistical parameters (R2train=0.893, R2test=0.921, Q2LOO= 0.844, F=43.17, RMSE=0.287). Comparison of the results between GA-MLR and GA-SVM demonstrates that GA-SVM provided better results for the training set compounds, however the predictive quality for both models are acceptable. The results suggest that atomic mass and polarizabilities and also number of heteroatom in molecules are the main independent factors contributing to the CK2 inhibition activity. The predicted results of this study can be used to design of new and potent CK2 inhibitors.
    Arabian Journal of Chemistry 01/2015; 9. · 2.68 Impact Factor
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    ABSTRACT: Cancer is a leading cause of death worldwide. Cancer cells proliferate uncontrollably and, many cases, spread to other parts of the body. A protein historically involved in cancer is protein kinase CK2. CK2 is a serine-threonine kinase that has been involved in cell growth, cell proliferation and cell apoptosis. CK2 functions as an oncogene when overexpressed in mouse tissues, and can synergize with known oncogenes, such as ras, to induce cell transformation in cells in culture. CK2, typically the CK2α protein, is found elevated in a number of human tumors. However, we have little information on CK2α' and CK2β proteins, and scarce information on CK2 gene transcript expression. Here, we explore the expression of CK2 transcripts in primary tumor tissues using the database Oncomine in the six cancers with the highest mortality in the U.S.A. In addition, we studied the correlation between CK2 expression and overall survival using the Kaplan-Meier Plotter database in breast, ovarian, and lung cancers. We found widespread upregulation in the expression of CK2 genes in primary tumor tissues. However, we found underexpression of CK2α' transcripts in some tumors, increased CK2β transcripts in some invasive tumors, and deregulation of CK2 transcripts in some tumor precursors. There was also correlation between CK2 expression levels and patient survival. These data provides additional evidence for CK2 as a biomarker for cancer studies and as a target for cancer therapy.
    PLoS ONE 12/2014; 9(12):e115609. · 3.53 Impact Factor
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    ABSTRACT: Head-and-neck cancer is a major form of the disease worldwide. Treatment consists of surgery, radiation therapy and chemotherapy, but these have not resulted in improved survival rates over the past few decades. Versatile nanoparticles, with selective tumor targeting, are considered to have the potential to improve these poor outcomes. Application of nanoparticle-based targeted therapeutics has extended into many areas, including gene silencing, chemotherapeutic drug delivery, radiosensitization, photothermal therapy, and has shown much promise. In this review, we discuss recent advances in the field of nanoparticle-mediated targeted therapeutics for head-and-neck cancer, with an emphasis on the description of targeting points, including future perspectives.
    International journal of medical sciences. 12(2):187-200.

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