Abstract
Frequent overexpression of the folate receptor (FR) on a variety of tumor types and on activated macrophages makes this re-ceptor an interesting target for both imaging and therapy of cancer and inflammation. The FR is a glycosylphophatidylinositol-anchored protein that binds the vitamin folic acid with high affinity and internalizes it via endocytosis. In normal tissues and organs, FR-expression is restricted to only a few sites where it is confined to the luminal surface of polarized epithelia and hence does not have access to intra-venously administered folic acid conjugates. Thus, using folic acid as a molecular “Trojan horse” to deliver attached probes to the dis-eased tissue has emerged as a powerful strategy. A variety of folic acid radioconjugates for potential application in nuclear medicine have been developed and (pre)clinically evaluated during the last two decades. Herein we report on folate receptor targeted tracer design and in vitro/in vivo investigations using folic acid -targeted radioconjugates suitable for SPECT and PET imaging as well as for potential therapeutic purposes.
Keywords: Folic acid, folate receptor, imaging, PET, SPECT, targeted radionuclide therapy, cancer, inflammation, macrophages, endocytosis
Current Pharmaceutical Design
Title: Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation
Volume: 18 Issue: 8
Author(s): Cristina Muller
Affiliation:
Keywords: Folic acid, folate receptor, imaging, PET, SPECT, targeted radionuclide therapy, cancer, inflammation, macrophages, endocytosis
Abstract: Frequent overexpression of the folate receptor (FR) on a variety of tumor types and on activated macrophages makes this re-ceptor an interesting target for both imaging and therapy of cancer and inflammation. The FR is a glycosylphophatidylinositol-anchored protein that binds the vitamin folic acid with high affinity and internalizes it via endocytosis. In normal tissues and organs, FR-expression is restricted to only a few sites where it is confined to the luminal surface of polarized epithelia and hence does not have access to intra-venously administered folic acid conjugates. Thus, using folic acid as a molecular “Trojan horse” to deliver attached probes to the dis-eased tissue has emerged as a powerful strategy. A variety of folic acid radioconjugates for potential application in nuclear medicine have been developed and (pre)clinically evaluated during the last two decades. Herein we report on folate receptor targeted tracer design and in vitro/in vivo investigations using folic acid -targeted radioconjugates suitable for SPECT and PET imaging as well as for potential therapeutic purposes.
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Cite this article as:
Muller Cristina, Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation, Current Pharmaceutical Design 2012; 18 (8) . https://dx.doi.org/10.2174/138161212799315777
DOI https://dx.doi.org/10.2174/138161212799315777 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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