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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Amines / chemistry
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Amino Acid Sequence
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Animals
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Coordination Complexes / chemistry*
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Copper / chemistry
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ErbB Receptors / chemistry
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ErbB Receptors / metabolism
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Humans
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Mice
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NIH 3T3 Cells
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Picolinic Acids / chemistry
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Protein Interaction Domains and Motifs
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Protein Structure, Tertiary
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STAT3 Transcription Factor / chemistry
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STAT3 Transcription Factor / metabolism
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src Homology Domains*
Substances
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2,2'-dipicolylamine
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Amines
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Coordination Complexes
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Picolinic Acids
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STAT3 Transcription Factor
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Copper
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ErbB Receptors