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International Journal of Oncology
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Print ISSN: 1019-6439 Online ISSN: 1791-2423
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June 2012 Volume 40 Issue 6

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Journals

International Journal of Molecular Medicine

International Journal of Molecular Medicine

International Journal of Molecular Medicine is an international journal devoted to molecular mechanisms of human disease.

International Journal of Oncology

International Journal of Oncology

International Journal of Oncology is an international journal devoted to oncology research and cancer treatment.

Molecular Medicine Reports

Molecular Medicine Reports

Covers molecular medicine topics such as pharmacology, pathology, genetics, neuroscience, infectious diseases, molecular cardiology, and molecular surgery.

Oncology Reports

Oncology Reports

Oncology Reports is an international journal devoted to fundamental and applied research in Oncology.

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine is an international journal devoted to laboratory and clinical medicine.

Oncology Letters

Oncology Letters

Oncology Letters is an international journal devoted to Experimental and Clinical Oncology.

Biomedical Reports

Biomedical Reports

Explores a wide range of biological and medical fields, including pharmacology, genetics, microbiology, neuroscience, and molecular cardiology.

Molecular and Clinical Oncology

Molecular and Clinical Oncology

International journal addressing all aspects of oncology research, from tumorigenesis and oncogenes to chemotherapy and metastasis.

World Academy of Sciences Journal

World Academy of Sciences Journal

Multidisciplinary open-access journal spanning biochemistry, genetics, neuroscience, environmental health, and synthetic biology.

International Journal of Functional Nutrition

International Journal of Functional Nutrition

Open-access journal combining biochemistry, pharmacology, immunology, and genetics to advance health through functional nutrition.

International Journal of Epigenetics

International Journal of Epigenetics

Publishes open-access research on using epigenetics to advance understanding and treatment of human disease.

Medicine International

Medicine International

An International Open Access Journal Devoted to General Medicine.

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June 2012 Volume 40 Issue 6

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Article

Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy

  • Authors:
    • Weiwei Nie
    • Lin Tang
    • Haiyang Zhang
    • Jiaqing Shao
    • Yucai Wang
    • Longbang Chen
    • Donghai Li
    • Xiaoxiang Guan

  • View Affiliations / Copyright

    Affiliations: Department of Medical Oncology, Jinling Hospital, Medical School of Nanjing University, Nanjing 210002, P.R. China, Jiangsu Engineering Research Center for MicroRNA Biology and Biotechnology, State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, P.R. China, Department of Endocrinology, Jinling Hospital, Medical School of Nanjing University, Nanjing 210002, P.R. China
  • Pages: 1763-1769
    |
    Published online on: February 3, 2012
       https://doi.org/10.3892/ijo.2012.1356
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Abstract

The development and clinical application of TK domain inhibitors (TKIs) provide important insights into the broader field of cancer-targeted therapies. To discuss the recent advances in the atomic level understanding of EGFR TK domain mutations, we aim at highlighting the current and future importance of these studies on malignancies where the TK domain is improperly activated. The analysis is conducted on published TK domain crystal structures deposited in the Protein Data Bank, or homology structures generated by homology modeling and AutoDock 4.2 software using the program O. Mutations in exon 19 are the most common pathogenic mutations, so the crystal structures with these mutations are analyzed and compared in detail. In addition, we demonstrate how these crystal structures of EGFR conformation with TK domain mutations and those binding with small molecule inhibitors unveil the active or inactive mechanisms. As to the increasing resistance to the TKI, we summarize the progress on overcoming this challenge. Simultaneously, we predict the structure of BIKW-2992 binding to EGFR and compare it with the validated structure of HKI-272. It is hoped that a more accurate resistance mechanism would be found. In brief, we believe that this research will provide insights into EGFR targeted therapies.

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Copy and paste a formatted citation
Spandidos Publications style
Nie W, Tang L, Zhang H, Shao J, Wang Y, Chen L, Li D and Guan X: Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy. Int J Oncol 40: 1763-1769, 2012.
APA
Nie, W., Tang, L., Zhang, H., Shao, J., Wang, Y., Chen, L. ... Guan, X. (2012). Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy. International Journal of Oncology, 40, 1763-1769. https://doi.org/10.3892/ijo.2012.1356
MLA
Nie, W., Tang, L., Zhang, H., Shao, J., Wang, Y., Chen, L., Li, D., Guan, X."Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy". International Journal of Oncology 40.6 (2012): 1763-1769.
Chicago
Nie, W., Tang, L., Zhang, H., Shao, J., Wang, Y., Chen, L., Li, D., Guan, X."Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy". International Journal of Oncology 40, no. 6 (2012): 1763-1769. https://doi.org/10.3892/ijo.2012.1356
Copy and paste a formatted citation
x
Spandidos Publications style
Nie W, Tang L, Zhang H, Shao J, Wang Y, Chen L, Li D and Guan X: Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy. Int J Oncol 40: 1763-1769, 2012.
APA
Nie, W., Tang, L., Zhang, H., Shao, J., Wang, Y., Chen, L. ... Guan, X. (2012). Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy. International Journal of Oncology, 40, 1763-1769. https://doi.org/10.3892/ijo.2012.1356
MLA
Nie, W., Tang, L., Zhang, H., Shao, J., Wang, Y., Chen, L., Li, D., Guan, X."Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy". International Journal of Oncology 40.6 (2012): 1763-1769.
Chicago
Nie, W., Tang, L., Zhang, H., Shao, J., Wang, Y., Chen, L., Li, D., Guan, X."Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy". International Journal of Oncology 40, no. 6 (2012): 1763-1769. https://doi.org/10.3892/ijo.2012.1356
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