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This version was published on February 1, 2008
Journal of Biomolecular Screening, Vol. 13, No. 2, 112-119 (2008)
DOI: 10.1177/1087057107312124

Development of Binding Assays for the SH2 Domain of Grb7 and Grb2 Using Fluorescence Polarization

Jean-Philippe Luzy

INSERM U648, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, UFR Biomédicale, Université Paris Descartes, Paris, France

Huixiong Chen

INSERM U648, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, UFR Biomédicale, Université Paris Descartes, Paris, France, huixiong.chen{at}univ-paris5.fr

Brunilde Gril

INSERM U648, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, UFR Biomédicale, Université Paris Descartes, Paris, France

Wang-Qing Liu

INSERM U648, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, UFR Biomédicale, Université Paris Descartes, Paris, France

Michel Vidal

INSERM U648, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, UFR Biomédicale, Université Paris Descartes, Paris, France

Dominique Perdereau

Université Paris Descartes, INSERM U567, CNRS UMR 8104, Institut Cochin, Département d'Endocrinologie, Métabolisme et Cancer, Paris, France

Anne-Françoise Burnol

Université Paris Descartes, INSERM U567, CNRS UMR 8104, Institut Cochin, Département d'Endocrinologie, Métabolisme et Cancer, Paris, France

Christiane Garbay

INSERM U648, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, UFR Biomédicale, Université Paris Descartes, Paris, France

Adaptor proteins Grb7 and Grb2 have been implicated as being 2 potential therapeutic targets in several human cancers, especially those that overexpress ErbB2. These 2 proteins contain both a SH2 domain (Src homology 2) that binds to phosphorylated tyrosine residues contained within ErbB2 and other specific protein targets. Two assays based on enzyme-linked immunosorbent assay and fluorescence polarization methods have been developed and validated to find and rank inhibitors for both proteins binding to the pY1139. Fluorescence polarization assays allowed the authors to determine quickly and reproducibly affinities of peptides from low nanomolar to high micromolar range and to compare them directly for Grb7 and Grb2. As a result, the assays have identified a known peptidomimetic Grb2 SH2 inhibitor (mAZ-pTyr-({alpha}Me)pTyr-Asn-NH2) that exhibits the most potent affinity for the Grb7 SH2 domain described to date. (Journal of Biomolecular Screening 2008:112-119)

Key Words: fluorescence polarization • assay development • Grb2 • Grb7 • SH2 domain • inhibitors


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