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Issue 9, 2016
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Fluorescent IGF-II analogues for FRET-based investigations into the binding of IGF-II to the IGF-1R

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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.

Graphical abstract: Fluorescent IGF-II analogues for FRET-based investigations into the binding of IGF-II to the IGF-1R

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Publication details

The article was received on 12 Oct 2015, accepted on 26 Jan 2016 and first published on 26 Jan 2016


Article type: Paper
DOI: 10.1039/C5OB02110C
Citation: Org. Biomol. Chem., 2016,14, 2698-2705
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    Fluorescent IGF-II analogues for FRET-based investigations into the binding of IGF-II to the IGF-1R

    J. M. Cottam Jones, P. W. R. Harris, D. B. Scanlon, B. E. Forbes, M. A. Brimble and A. D. Abell, Org. Biomol. Chem., 2016, 14, 2698
    DOI: 10.1039/C5OB02110C

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