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Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

Author

Listed:
  • Wenjun Zhou

    (Department of Cancer Biology,
    Department of Biological Chemistry and Molecular Pharmacology,)

  • Dalia Ercan

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA)

  • Liang Chen

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA)

  • Cai-Hong Yun

    (Department of Cancer Biology,
    Department of Biological Chemistry and Molecular Pharmacology,)

  • Danan Li

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA)

  • Marzia Capelletti

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA)

  • Alexis B. Cortot

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA)

  • Lucian Chirieac

    (Brigham and Women’s Hospital, Boston, Massachusetts 02115, USA)

  • Roxana E. Iacob

    (The Barnett Institute of Chemical & Biological Analysis,
    Northeastern University, Boston, Massachusetts 02115, USA)

  • Robert Padera

    (Brigham and Women’s Hospital, Boston, Massachusetts 02115, USA)

  • John R. Engen

    (The Barnett Institute of Chemical & Biological Analysis,
    Northeastern University, Boston, Massachusetts 02115, USA)

  • Kwok-Kin Wong

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA
    Brigham and Women's Hospital and Harvard Medical School, Boston, Massachusetts 02115, USA
    Ludwig Center at Dana-Farber/Harvard Cancer Center, Boston, Massachusetts 02115, USA)

  • Michael J. Eck

    (Department of Cancer Biology,
    Department of Biological Chemistry and Molecular Pharmacology,)

  • Nathanael S. Gray

    (Department of Cancer Biology,
    Department of Biological Chemistry and Molecular Pharmacology,)

  • Pasi A. Jänne

    (Lowe Center for Thoracic Oncology,
    Dana-Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA
    Brigham and Women's Hospital and Harvard Medical School, Boston, Massachusetts 02115, USA)

Abstract

Antitumour drugs: novel EGFR inhibitors Non-small-cell lung tumours with activating mutations in the epidermal growth factor receptor (EGFR) often show a clinical response to receptor inhibitors, but tend to develop resistance due to the additional EGFR T790M mutations. Pasi Jänne and colleagues now have developed a new class of EGFR inhibitor that selectively inhibits the mutant receptor, rather that the wild type, and also inhibits the T790M mutant. These compounds reduce tumour growth in a mouse model and may prove more clinically effective and better tolerated than current EGFR kinase inhibitors in clinical use.

Suggested Citation

  • Wenjun Zhou & Dalia Ercan & Liang Chen & Cai-Hong Yun & Danan Li & Marzia Capelletti & Alexis B. Cortot & Lucian Chirieac & Roxana E. Iacob & Robert Padera & John R. Engen & Kwok-Kin Wong & Michael J., 2009. "Novel mutant-selective EGFR kinase inhibitors against EGFR T790M," Nature, Nature, vol. 462(7276), pages 1070-1074, December.
    • Handle: RePEc:nat:nature:v:462:y:2009:i:7276:d:10.1038_nature08622
    DOI: 10.1038/nature08622
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    Citations

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    Cited by:

    1. Tyler S. Beyett & Ciric To & David E. Heppner & Jaimin K. Rana & Anna M. Schmoker & Jaebong Jang & Dries J. H. Clercq & Gabriel Gomez & David A. Scott & Nathanael S. Gray & Pasi A. Jänne & Michael J. , 2022. "Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors," Nature Communications, Nature, vol. 13(1), pages 1-11, December.

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