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

doi:10.1074/jbc.M113.492280

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

Research output: Contribution to journal › Article › peer-review

29 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 language	English (US)
Pages (from-to)	26879-26886
Number of pages	8
Journal	Journal of Biological Chemistry
Volume	288
Issue number	37
DOIs	https://doi.org/10.1074/jbc.M113.492280
State	Published - Sep 13 2013
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Cell Biology

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Ahsan, A., Ray, D., Ramanand, S. G., Hegde, A., Whitehead, C., Rehemtulla, A., Morishima, Y., Pratt, W. B., Osawa, Y., Lawrence, T. S., & Nyati, M. K. (2013). Destabilization of the epidermal growth factor receptor (EGFR) by a peptide that inhibits egfr binding to heat shock protein 90 and receptor dimerization. Journal of Biological Chemistry, 288(37), 26879-26886. https://doi.org/10.1074/jbc.M113.492280

Ahsan, A, Ray, D, Ramanand, SG, Hegde, A, Whitehead, C, Rehemtulla, A, Morishima, Y, Pratt, WB, Osawa, Y, Lawrence, TS & Nyati, MK 2013, 'Destabilization of the epidermal growth factor receptor (EGFR) by a peptide that inhibits egfr binding to heat shock protein 90 and receptor dimerization', Journal of Biological Chemistry, vol. 288, no. 37, pp. 26879-26886. https://doi.org/10.1074/jbc.M113.492280

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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.",

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AU - Ray, Dipankar

AU - Ramanand, Susmita G.

AU - Hegde, Ashok

AU - Whitehead, Christopher

AU - Rehemtulla, Alnawaz

AU - Morishima, Yoshihiro

AU - Pratt, William B.

AU - Osawa, Yoichi

AU - Lawrence, Theodore S.

AU - Nyati, Mukesh K.

PY - 2013/9/13

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AB - 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.

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

Abstract

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