title: 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.
authors.affiliation: Department of Chemistry, University of Toronto, Toronto, Canada.
authors.forename: Joel A
authors.initials: JA
authors.lastname: Drewry
authors.forename: Steven
authors.initials: S
authors.lastname: Fletcher
authors.forename: Peibin
authors.initials: P
authors.lastname: Yue
authors.forename: Denys
authors.initials: D
authors.lastname: Marushchak
authors.forename: Wei
authors.initials: W
authors.lastname: Zhao
authors.forename: Sumaiya
authors.initials: S
authors.lastname: Sharmeen
authors.forename: Xiaolei
authors.initials: X
authors.lastname: Zhang
authors.forename: Aaron D
authors.initials: AD
authors.lastname: Schimmer
authors.forename: Claudiu
authors.initials: C
authors.lastname: Gradinaru
authors.forename: James
authors.initials: J
authors.lastname: Turkson
authors.forename: Patrick T
authors.initials: PT
authors.lastname: Gunning
mesh_terms: D000588:Amines / Q000737:chemistry; D000595:Amino Acid Sequence; D000818:Animals; D056831:Coordination Complexes / Q000737:chemistry*; D003300:Copper / Q000737:chemistry; D066246:ErbB Receptors / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D051379:Mice; D041681:NIH 3T3 Cells; D010848:Picolinic Acids / Q000737:chemistry; D054730:Protein Interaction Domains and Motifs; D017434:Protein Structure, Tertiary; D050796:STAT3 Transcription Factor / Q000737:chemistry / Q000378:metabolism; D018909:src Homology Domains
chemical_list: C501847:2,2'-dipicolylamine; D000588:Amines; D056831:Coordination Complexes; D010848:Picolinic Acids; D050796:STAT3 Transcription Factor; D003300:Copper; D066246:ErbB Receptors