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Issue 7, 2012
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Src homology 2 domain proteomimetics: developing phosphopeptide selective receptors

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Abstract

SH2 domains are the paradigm of phosphotyrosine protein recognition modules and are involved in mediating numerous cancer-promoting proteinprotein complexes. In an effort to develop protein-selective receptors for inhibition of protein complexation events, we herein report the de novo rational and computationally aided design of SH2 domain proteomimetics. Lead mimetics exhibit target phosphopeptide selectivity (Ka ≈ 107 M−1) and potently disrupt SH2 domain:phosphopeptide interactions.

Graphical abstract: Src homology 2 domain proteomimetics: developing phosphopeptide selective receptors

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Article information


Submitted
22 Feb 2012
Accepted
29 Feb 2012
First published
04 Apr 2012

Med. Chem. Commun., 2012,3, 763-770
Article type
Concise Article

Src homology 2 domain proteomimetics: developing phosphopeptide selective receptors

J. A. Drewry, S. Burger, A. Mazouchi, E. Duodu, P. Ayers, C. C. Gradinaru and P. T. Gunning, Med. Chem. Commun., 2012, 3, 763
DOI: 10.1039/C2MD20052J

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