title: Fluorescent IGF-II analogues for FRET-based investigations into the binding of IGF-II to the IGF-1R.
abstract: The interaction of IGF-II with the insulin receptor (IR) and type 1 insulin-like growth factor receptor (IGF-1R) has recently been identified as potential therapeutic target for the treatment of cancer. Understanding the interactions of IGF-II with these receptors is required for the development of potential anticancer therapeutics. This work describes an efficient convergent synthesis of native IGF-II and two non-native IGF-II analogues with coumarin fluorescent probes incorporated at residues 19 and 28. These fluorescent analogues bind with nanomolar affinities to the IGF-1R and are suitable for use in fluorescence resonance energy transfer (FRET) studies. From these studies the F19Cou IGF-II and F28Cou IGF-II proteins were identified as good probes for investigating the binding interactions of IGF-II with the IGF-1R and its other high affinity binding partners.
authors.affiliation: Department of Chemistry, The University of Adelaide, Adelaide 5001, SA, Australia.
authors.forename: J M
authors.initials: JM
authors.lastname: Cottam Jones
authors.affiliation: School of Chemical Sciences, The University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand and Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1010, New Zealand and Institute for Innovation in Biotechnology, The University of Auckland, 3A Symonds Street, Auckland 1010, New Zealand.
authors.forename: P W R
authors.initials: PW
authors.lastname: Harris
authors.affiliation: Department of Chemistry, The University of Adelaide, Adelaide 5001, SA, Australia.
authors.forename: D B
authors.initials: DB
authors.lastname: Scanlon
authors.affiliation: School of Molecular and Biomedical Sciences, The University of Adelaide, Adelaide 5005, SA, Australia and School of Medicine, Flinders University of South Australia, Bedford Park, 5042, SA, Australia.
authors.forename: B E
authors.initials: BE
authors.lastname: Forbes
authors.affiliation: School of Chemical Sciences, The University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand and Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1010, New Zealand and Institute for Innovation in Biotechnology, The University of Auckland, 3A Symonds Street, Auckland 1010, New Zealand.
authors.forename: M A
authors.initials: MA
authors.lastname: Brimble
authors.affiliation: Department of Chemistry, The University of Adelaide, Adelaide 5001, SA, Australia and ARC Centre of Excellence for Nanoscale BioPhotonics (CNBP), The University of Adelaide, South Australia, 5005, Australia.
authors.forename: A D
authors.initials: AD
authors.lastname: Abell
mesh_terms: D001665:Binding Sites; D005453:Fluorescence; D031541:Fluorescence Resonance Energy Transfer; D007335:Insulin-Like Growth Factor II / Q000031:analogs & derivatives / Q000737:chemistry*; D015394:Molecular Structure; D017526:Receptor, IGF Type 1 / Q000737:chemistry*
chemical_list: D007335:Insulin-Like Growth Factor II; D017526:Receptor, IGF Type 1