Selective imaging of the angiogenic relevant integrins α5β1 and αvβ3

Angew Chem Int Ed Engl. 2013 Oct 25;52(44):11656-9. doi: 10.1002/anie.201306376. Epub 2013 Sep 20.

Abstract

Pattern seekers: For the two angiogenic relevant integrins α5β1 and αvβ3, functionalized derivatives of the selective antagonists 1 and 2 could target and discriminate between tumor cells in vivo based on their different integrin patterns and also delay tumor growth in vivo. In addition, the first α5β1-selective integrin antagonist that enables specific molecular imaging by positron emission tomography was developed.

Keywords: RGD sequence; angiogenesis; integrins; peptidomimetics; positron emission tomography.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Modulating Agents
  • Animals
  • Humans
  • Integrin alpha5beta1 / antagonists & inhibitors*
  • Integrin alphaVbeta3 / antagonists & inhibitors*
  • Mice
  • Peptidomimetics
  • Positron-Emission Tomography / methods*
  • Rats

Substances

  • Angiogenesis Modulating Agents
  • Integrin alpha5beta1
  • Integrin alphaVbeta3
  • Peptidomimetics