E-peptides control bioavailability of IGF-1

PLoS One. 2012;7(12):e51152. doi: 10.1371/journal.pone.0051152. Epub 2012 Dec 10.

Abstract

Insulin-like growth factor 1 (IGF-1) is a potent cytoprotective growth factor that has attracted considerable attention as a promising therapeutic agent. Transgenic over-expression of IGF-1 propeptides facilitates protection and repair in a broad range of tissues, although transgenic mice over-expressing IGF-1 propeptides display little or no increase in IGF-1 serum levels, even with high levels of transgene expression. IGF-1 propeptides are encoded by multiple alternatively spliced transcripts including C-terminal extension (E) peptides, which are highly positively charged. In the present study, we use decellularized mouse tissue to show that the E-peptides facilitate in vitro binding of murine IGF-1 to the extracellular matrix (ECM) with varying affinities. This property is independent of IGF-1, since proteins consisting of the E-peptides fused to relaxin, a related member of the insulin superfamily, bound equally avidly to decellularized ECM. Thus, the E-peptides control IGF-1 bioavailability by preventing systemic circulation, offering a potentially powerful way to tether IGF-1 and other therapeutic proteins to the site of synthesis and/or administration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alternative Splicing
  • Animals
  • Base Sequence
  • Biological Availability
  • Blotting, Northern
  • DNA Primers
  • Extracellular Matrix / metabolism
  • HEK293 Cells
  • Humans
  • Immunohistochemistry
  • Insulin-Like Growth Factor I / metabolism*
  • Mice
  • Mice, Transgenic
  • Peptides / genetics
  • Peptides / physiology*
  • Protein Binding

Substances

  • DNA Primers
  • Peptides
  • Insulin-Like Growth Factor I

Grants and funding

This work was supported by funds from European Molecular Biology Laboratory and the FP7 ENDOSTEM grant from European Commission HEALTH-2009-1.4-3 Grant agreement No. 241440, and by a sponsored research agreement with Novartis. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.