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Molecular imaging of integrins in oncology

Authors Höltke C, Faust A

Received 22 July 2016

Accepted for publication 3 November 2016

Published 31 January 2017 Volume 2017:10 Pages 17—30


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 5

Editor who approved publication: Professor Tarik Massoud

Carsten Höltke,1 Andreas Faust2

1Department of Clinical Radiology, University Hospital Münster, and 2European Institute for Molecular Imaging, University of Münster, Münster, Germany

Abstract: Integrins are a class of heterodimeric cell surface receptors with a variety of essential contributions to cell–cell and cell–extracellular matrix interactions. In particular, integrin αvβ3 plays an important role in the regulation of normal and tumor cell migration and survival, as well as in tumor angiogenesis and metastasis. Its overexpression has been proved for a number of malignancies, and the level of αvβ3 expression has been recognized as a potential surrogate marker of angiogenic activity. Therefore, αvβ3 represents an important target structure in noninvasive cancer diagnosis and the evaluation of antiangiogenic therapies. One common feature of many integrins is high-affinity binding to proteins containing an Arg-Gly-Asp (RGD) peptide motif, which can be found in their endogenous ligands, for example, fibronectin, vitronectin, and fibrinogen. Consequently, not only small synthetic peptides containing the RGD motif but also peptidomimetic structures based on RGD have been designed, and appropriate labeling strategies utilized them for molecular imaging approaches. This review focuses on recent advances of integrin molecular imaging in cancer diagnosis. First, clinical applications are highlighted, and then experimental approaches in preclinical research and multimodal setups are discussed.

integrins, angiogenesis, RGD, cancer diagnostics

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