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Coordination complex SH2 domain proteomimetics: an alternative approach to disrupting oncogenic protein-protein interactions.

ABSTRACT: We report the first application of coordination complexes as functional proteomimetics of the Src homology 2 (SH2) phosphopeptide-binding domain. As a proof-of-concept, functionalized bis-dipicolylamine (BDPA) copper(ii) complexes are shown to disrupt oncogenic Stat3-Stat3 protein complexes and elicit promising anti-tumour activity.

SUBMITTER: Drewry JA 

PROVIDER: S-EPMC2910512 | biostudies-literature | 2010 Feb

REPOSITORIES: biostudies-literature

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Coordination complex SH2 domain proteomimetics: an alternative approach to disrupting oncogenic protein-protein interactions.

Drewry Joel A JA   Fletcher Steven S   Yue Peibin P   Marushchak Denys D   Zhao Wei W   Sharmeen Sumaiya S   Zhang Xiaolei X   Schimmer Aaron D AD   Gradinaru Claudiu C   Turkson James J   Gunning Patrick T PT  

Chemical communications (Cambridge, England) 20091201 6

We report the first application of coordination complexes as functional proteomimetics of the Src homology 2 (SH2) phosphopeptide-binding domain. As a proof-of-concept, functionalized bis-dipicolylamine (BDPA) copper(ii) complexes are shown to disrupt oncogenic Stat3-Stat3 protein complexes and elicit promising anti-tumour activity. ...[more]

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