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Cancer Research
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About the Cover

Cover image

Cover image expansion

GW572016 (Lapatinib) is a dual EGFR/ErbB-2 kinase inhibitor in clinical development. Wood et al. determined the structure of EGFR bound to GW572016 and found it is significantly different from EGFR bound to a related inhibitor, Tarceva. GW572016 was found to have a significantly slower off-rate from purified EGFR than Tarceva and the slow off-rate correlates with a prolonged suppression of receptor activity in tumor cells. The GW572016/EGFR structure provides potential explanations for the compound's slow-off rate and ability to inhibit ErbB-2. The cover image shows the structure of the ATP binding pocket of EGFR bound to GW572016. The compound protrudes deep into a back pocket that was not present in structures of apo-EGFR or EGFR bound to Tarceva. (The authors wish to acknowledge Aaron Miller for production of this image of the GW572016/EGFR structure.) For details, see the article by Wood et al. on page 6652 of this issue.

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Cancer Research: 64 (18)
September 2004
Volume 64, Issue 18
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Issue Highlights

  • A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib)
  • Choline Kinase Activation Is a Critical Requirement for the Proliferation of Primary Human Mammary Epithelial Cells and Breast Tumor Progression
  • Targeted Disruption of the 3p12 Gene, Dutt1/Robo1, Predisposes Mice to Lung Adenocarcinomas and Lymphomas with Methylation of the Gene Promoter
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Copyright © 2021 by the American Association for Cancer Research.

Cancer Research Online ISSN: 1538-7445
Cancer Research Print ISSN: 0008-5472
Journal of Cancer Research ISSN: 0099-7013
American Journal of Cancer ISSN: 0099-7374

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