Radiolabelled peptides for oncological diagnosis

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Abstract

Radiolabelled receptor-binding peptides targeting receptors (over)expressed on tumour cells are widely under investigation for tumour diagnosis and therapy. The concept of using radiolabelled receptor-binding peptides to target receptor-expressing tissues in vivo has stimulated a large body of research in nuclear medicine. The ¹¹¹In-labelled somatostatin analogue octreotide (OctreoScan™) is the most successful radiopeptide for tumour imaging, and was the first to be approved for diagnostic use. Based on the success of these studies, other receptor-targeting peptides such as cholecystokinin/gastrin analogues, glucagon-like peptide-1, bombesin (BN), chemokine receptor CXCR4 targeting peptides, and RGD peptides are currently under development or undergoing clinical trials. In this review, we discuss some of these peptides and their analogues, with regard to their potential for radionuclide imaging of tumours.

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HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor.

Y. Feng, C. Broder, P. Kennedy … (1996)

A cofactor for HIV-1 (human immunodeficiency virus-type 1) fusion and entry was identified with the use of a novel functional complementary DNA (cDNA) cloning strategy. This protein, designated "fusin," is a putative G protein-coupled receptor with seven transmembrane segments. Recombinant fusin enabled CD4-expressing nonhuman cell types to support HIV-1 Env-mediated cell fusion and HIV-1 infection. Antibodies to fusin blocked cell fusion and infection with normal CD4-positive human target cells. Fusin messenger RNA levels correlated with HIV-1 permissiveness in diverse human cell types. Fusin acted preferentially for T cell line-tropic isolates, in comparison to its activity with macrophagetropic HIV-1 isolates.

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GLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting.

Martin Stöckli, Meike Körner, Jean Claude Reubi … (2007)

Peptide hormone receptors overexpressed in human tumors, such as somatostatin receptors, can be used for in vivo targeting for diagnostic and therapeutic purposes. A novel promising candidate in this field is the GLP-1 receptor, which was recently shown to be massively overexpressed in gut and lung neuroendocrine tumors--in particular, in insulinomas. Anticipating a major development of GLP-1 receptor targeting in nuclear medicine, our aim was to evaluate in vitro the GLP-1 receptor expression in a large variety of other tumors and to compare it with that in nonneoplastic tissues. The GLP-1 receptor protein expression was qualitatively and quantitatively investigated in a broad spectrum of human tumors (n=419) and nonneoplastic human tissues (n=209) with receptor autoradiography using (125)I-GLP-1(7-36)amide. Pharmacologic competition experiments were performed to provide proof of specificity of the procedure. GLP-1 receptors were expressed in various endocrine tumors, with particularly high amounts in pheochromocytomas, as well as in brain tumors and embryonic tumors but not in carcinomas or lymphomas. In nonneoplastic tissues, GLP-1 receptors were present in generally low amounts in specific tissue compartments of several organs--namely, pancreas, intestine, lung, kidney, breast, and brain; no receptors were identified in lymph nodes, spleen, liver, or the adrenal gland. The rank order of potencies for receptor binding--namely, GLP-1(7-36)amide = exendin-4 > GLP-2 = glucagon(1-29)--provided proof of specific GLP-1 receptor identification. The GLP-1 receptors may represent a novel molecular target for in vivo scintigraphy and targeted radiotherapy for a variety of GLP-1 receptor-expressing tumors. For GLP-1 receptor scintigraphy, a low-background signal can be expected, on the basis of the low receptor expression in the normal tissues surrounding tumors.

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Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting.

Jean Claude Reubi, Beatrice Waser (2003)

Peptide receptors have been found to represent excellent targets for in vivo cancer diagnosis and therapy. Recent in vitro studies have shown that many cancers can overexpress not only one but several peptide receptors concomitantly. One of the challenges for nuclear medicine in this field in the coming decade will be to take advantage of the co-expression of peptide receptors for multireceptor tumour targeting. In vitro receptor studies can reveal which peptide receptor is overexpressed in which tumour and which receptors are co-expressed in an individual tumour; such knowledge is a prerequisite for successful in vivo development. One group of tumours of particular interest in this respect is the neuroendocrine tumours, which have previously been shown often to express peptide receptors. This review summarises our investigations of the concomitant expression of 13 different peptide receptors, in more than 100 neuroendocrine tumours of the human intestine, pancreas and lung, using in vitro receptor autoradiography with subtype-selective ligands. The incidence and density of the somatostatin receptors sst(1)-sst(5), the VIP receptors VPAC(1) and VPAC(2), the CCK(1) and CCK(2) receptors, the three bombesin receptor subtypes BB(1) (NMB receptor), BB(2) (GRP receptor) and BB(3), and GLP-1 receptors were evaluated. While the presence of VPAC(1) and sst(2) was detected in the majority of these neuroendocrine tumours, the other receptors, more differentially expressed, revealed a characteristic receptor pattern in several tumour types. Ileal carcinoids expressed sst(2) and VPAC(1) receptors in virtually all cases and had CCK(1), CCK(2), sst(1) or sst(5) in approximately half of the cases; they were the only tumours of this series to express NMB receptors. Insulinomas were characterised by a very high incidence of GLP-1, CCK(2) and VPAC(1) receptors, with the GLP-1 receptors expressed in a particularly high density; they expressed sst(2) in two-thirds and sst(1) in approximately half of the cases and lacked CCK(1) and NMB receptors. All gastrinomas had sst(2) and GLP-1 receptors; they expressed GRP receptors in three-quarters of the cases and CCK(1) or VPAC(1) in approximately half of the cases. Most bronchial carcinoids had VPAC(1), while sst(1), sst(2) and CCK(2) were found in two-thirds of the cases and BB(3) in one-third of the cases. These data provide evidence for the vast biological diversity of these neuroendocrine tumours. Moreover, the results represent a basis for starting and/or optimising the in vivo targeting of these tumours by selecting the suitable radiopeptides for tumour diagnosis and/or therapy. Finally, the data strongly encourage concomitant application of several radiopeptides to permit more efficient targeting of these tumours.

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Author and article information

Contributors

: P.Laverman@nucmed.umcn.nl

Journal

Journal ID (nlm-ta): Eur J Nucl Med Mol Imaging

Title: European Journal of Nuclear Medicine and Molecular Imaging

Publisher: Springer-Verlag (Berlin/Heidelberg )

ISSN (Print): 1619-7070

ISSN (Electronic): 1619-7089

Publication date (Electronic): 3 March 2012

Publication date PMC-release: 3 March 2012

Publication date (Print): February 2012

Volume: 39

Issue: Suppl 1

Pages: 78-92

Affiliations

[1 ]Department of Nuclear Medicine, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands

[2 ]Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London, EC1M 6BQ UK

Article

Publisher ID: 2014

DOI: 10.1007/s00259-011-2014-7

PMC ID: 3304069

PubMed ID: 22388627

SO-VID: 2e593a51-3496-48b3-b7fa-865f1757ba86

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ScienceOpen disciplines: Radiology & Imaging

Keywords: cxcr4,gastrin,bombesin,glp-1,radiolabelled receptor-binding peptides

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ScienceOpen disciplines: Radiology & Imaging

Keywords: cxcr4, gastrin, bombesin, glp-1, radiolabelled receptor-binding peptides

Radiolabelled peptides for oncological diagnosis

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Abstract

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Probing cerebral hemodynamics with BOLD fMRI

Most cited references 121

HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor.

GLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting.

Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting.

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