Non-oncological applications of RGD-based single-photon emission tomography and positron emission tomography agents
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REVIEW ARTICLE
Non-oncological applications of RGD-based single-photon emission tomography and positron emission tomography agents Thomas Ebenhan 1,2
&
Janke Kleynhans 1,2 & Jan Rijn Zeevaart 2,3 & Jae Min Jeong 4 & Mike Sathekge 1
Received: 14 May 2020 / Accepted: 23 July 2020 # Springer-Verlag GmbH Germany, part of Springer Nature 2020
Abstract Introduction Non-invasive imaging techniques (especially single-photon emission tomography and positron emission tomography) apply several RGD-based imaging ligands developed during a vast number of preclinical and clinical investigations. The RGD (Arg-Gly-Asp) sequence is a binding moiety for a large selection of adhesive extracellular matrix and cell surface proteins. Since the first identification of this sequence as the shortest sequence required for recognition in fibronectin during the 1980s, fundamental research regarding the molecular mechanisms of integrin action have paved the way for development of several pharmaceuticals and radiopharmaceuticals with clinical applications. Ligands recognizing RGD may be developed for use in the monitoring of these interactions (benign or pathological). Although RGD-based molecular imaging has been actively investigated for oncological purposes, their utilization towards non-oncology applications remains relatively under-exploited. Methods and Scope This review highlights the new non-oncologic applications of RGD-based tracers (with the focus on singlephoton emission tomography and positron emission tomography). The focus is on the last 10 years of scientific literature (2009– 2020). It is proposed that these imaging agents will be used for off-label indications that may provide options for disease monitoring where there are no approved tracers available, for instance Crohn’s disease or osteoporosis. Fundamental science investigations have made progress in elucidating the involvement of integrin in various diseases not pertaining to oncology. Furthermore, RGD-based radiopharmaceuticals have been evaluated extensively for safety during clinical evaluations of various natures. Conclusion Clinical translation of non-oncological applications for RGD-based radiopharmaceuticals and other imaging tracers without going through time-consuming extensive development is therefore highly plausible.
Keywords Arginyl-glycyl-aspartic acid . Integrin αVβ1 . Integrin αVβ3 . Positron emission tomography . Single-photon computed tomography . Optical imaging . RGD
Introduction Thomas Ebenhan and Janke Kleynhans contributed equally to this work. This article is part of the Topical Collection on Cardiology * Thomas Ebenhan [email protected] 1
Nuclear Medicine, University of Pretoria, Pretoria 0001, South Africa
2
Nuclear Medicine Research Infrastructure, NPC, Pretoria 0001, South Africa
3
DST/NWU Preclinical Drug Development Platform, North-West University, Potchefstroom 2520, South Africa
4
Department of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, 101 Daehangno Jongno-gu, Seoul
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