Cellular Targets of Gefitinib-Reference-Cited by-同舟云学术

Cellular Targets of Gefitinib

Published:2005-01-15 Issue:2 Volume:65 Page:379-382
ISSN:0008-5472
Container-title:Cancer Research
language:en
Short-container-title:

Author:

Brehmer Dirk¹,Greff Zoltán²,Godl Klaus¹,Blencke Stephanie¹,Kurtenbach Alexander¹,Weber Martina¹,Müller Stefan¹,Klebl Bert¹,Cotten Matt¹,Kéri György²³,Wissing Josef¹,Daub Henrik¹

Affiliation:

1. 1Axxima Pharmaceuticals AG, Munich, Germany and

2. 2Vichem Chemie Ltd. and

3. 3Department of Medicinal Chemistry, Peptide Biochemistry Research Group, Semmelweis University, Budapest, Hungary

Abstract

Abstract Targeted inhibition of protein kinases with small molecule drugs has evolved into a viable approach for anticancer therapy. However, the true selectivity of these therapeutic agents has remained unclear. Here, we used a proteomic method to profile the cellular targets of the clinical epidermal growth factor receptor kinase inhibitor gefitinib. Our data suggest alternative cellular modes of action for gefitinib and provide rationales for the development of related drugs.

Publisher

American Association for Cancer Research (AACR)

Subject

Cancer Research,Oncology

Link

https://aacrjournals.org/cancerres/article-pdf/65/2/379/2535561/379-382.pdf

Reference20 articles.

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3. Lynch TJ, Bell DW, Sordella R, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004; 350: 2129–39.

4. Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004: 304; 1497–500.

5. Godl K, Wissing J, Kurtenbach A, et al. An efficient proteomics method to identify the cellular targets of protein kinase inhibitors. Proc Natl Acad Sci U S A 2003; 100: 15434–9.

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