Destabilization of the epidermal growth factor receptor (EGFR) by a peptide that inhibits egfr binding to heat shock protein 90 and receptor dimerization

Aarif Ahsan, Dipankar Ray, Susmita G. Ramanand, Ashok Hegde, Christopher Whitehead, Alnawaz Rehemtulla, Yoshihiro Morishima, William B. Pratt, Yoichi Osawa, Theodore S. Lawrence, Mukesh K. Nyati

27 Scopus citations

Abstract

Background: An eight-amino acid segment lying within the αC-β4 loop region of many protein kinases determines sensitivity to Hsp90 inhibitors. Results:Apeptide comprised of this segment of the EGFR inhibits both Hsp90 binding and EGF-dependent EGFR dimerization. Conclusion: The peptide selectively degrades EGFR versus other Hsp90 clients. Significance: This peptide represents a unique approach to the therapy of EGFR-driven tumors.

Original languageEnglish (US)
Pages (from-to)26879-26886
Number of pages8
JournalJournal of Biological Chemistry
Volume288
Issue number37
DOIs
StatePublished - Sep 13 2013
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

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