Vasoactive Intestinal Peptide-Receptor Imaging for the Localization of Intestinal Adenocarcinomas and Endocrine Tumors

Virgolini, Irene; Raderer, Markus; Kurtaran, Amir; Angelberger, P.; Banyai, S; Yang, Qing; Li, Shuren; Banyai, Martin; Pidlich, Johann; Niederle, Bruno; Scheithauer, Werner; Valent, Peter

doi:10.1056/nejm199410273311703

Cited by 229 publications

(48 citation statements)

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“…Cleavage of the peptides from the resin and identification of the CF-labeled peptides was performed as already described above. [5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24] ]NPY, and [Lys(CF) 4 , Ahx [5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24] ]NPY. The analytical data of these peptides are summarized in Table I.…”

Section: Labeling With 5(6)-carboxyfluorescein (Cf)mentioning

confidence: 99%

“…4 Another clinical application has been the therapeutic targeting of receptor-expressing tumors by using high doses of these radiolabeled peptides. [5][6][7] The successful application of radiolabeled somatostatin and vasoactive intestinal peptide analogs for the imaging of some receptor-expressing tumors 4,8 has promoted the development of other regulatory peptides such as bombesin, sub-…”

Section: Introductionmentioning

confidence: 99%

“…21 Several proteolytic enzymes like neutral endopeptidase or metalloendopeptidase have been reported to affect the metabolic stability of peptides in plasma. 22 In the present study, we have studied the metabolic stability of NPY, the Y 2 -receptor selective analog [Ahx [5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24] For modification we chose labelling of the peptides with 5(6)-carboxyfluorescein (CF), in order to discriminate the peptide signal from plasma proteins by HPLC at its excitation/emission wavelengths as 450/517 nm, respectively. In addition to NPY itself the two selective compounds were modified at the N-terminus as well as at the side chain of Lys 4 in order to investigate the best position for modification with respect to metabolic stability.…”

Section: Introductionmentioning

confidence: 99%

“…Accordingly, we decided not to use any smaller reported analogs, e. g. NPY (25)(26)(27)(28)(29)(30)(31)(32)(33)(34)(35)(36), although this analog has been shown to exhibit some agonistic properties at Y 2 -receptors as well. 36,37 In case of CF-[Ahx [5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24] ]NPY, which is a centrally truncated Y 2 receptor selective analog, [17][18][19] an enzymatic degradation product CF-[Ahx [5][6][7][8][9][10][11][12][13][14][15][16][17]…”

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confidence: 99%

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Identification of neuropeptide Y cleavage products in human blood to improve metabolic stability

2007

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Regulatory, receptor‐binding peptides are considered as the agents of choice for diagnostic imaging and therapy of cancers, because their receptors are overexpressed in various human cancer cells. It has been recently indicated that there is a putative role of NPY in breast tumors. The expression of the two best‐investigated NPY receptor subtypes, Y1 and Y2, in breast tissue shows predominant occurrence of the Y1 receptor subtype in tumors, whereas Y2 receptors are found in nonproliferative tissue. To investigate the usefulness of NPY analogs for tumor diagnosis and therapy, we investigated the metabolic stability of receptor‐selective NPY analogs in human blood plasma. NPY analogs were synthesized by Fmoc/t‐Bu solid‐phase strategy. Prior to the cleavage of peptides from the resin, they were labeled with 5(6)‐carboxyfluorescein (CF) either at the N‐terminus or at the side chain of Lys4. For the metabolic stability study, the digestion of peptides was monitored by HPLC and the cleavage products were identified by MALDI‐ToF mass spectrometry. The data showed that full‐length [Phe7, Pro34]NPY analogs, which show high binding affinity to Y1 receptors are enzymatically more stable than centrally truncated analogs, which show high binding affinity to Y2 receptors. Furthermore, the N‐terminally CF‐labeled Y1 and Y2 receptor‐selective peptides were found to be enzymatically more resistant than their counterparts containing the CF label at Lys4 side chain. © 2007 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 88: 182–189, 2007. This article was originally published online as an accepted preprint. The ‘Published Online’ date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com

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Section: Labeling With 5(6)-carboxyfluorescein (Cf)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

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Identification of neuropeptide Y cleavage products in human blood to improve metabolic stability

2007

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“…123 I-labelled vasoactive intestinal peptide (VIP) receptor scintigraphy generally has lower sensitivity than SRS for GEP-NET localisation and is, therefore, generally not recommended for the diagnostic work-up of GEPNETs (74,75,76).…”

Section: Vasoactive Intestinal Peptide Receptor Scintigraphymentioning

confidence: 99%

GEP-NETs update: Functional localisation and scintigraphy in neuroendocrine tumours of the gastrointestinal tract and pancreas (GEP-NETs)

Herder¹

2014

European Journal of Endocrinology

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For patients with neuroendocrine tumours (NETs) of the gastrointestinal tract and pancreas (GEP) (GEP-NETs), excellent care should ideally be provided by a multidisciplinary team of skilled health care professionals. In these patients, a combination of nuclear medicine imaging and conventional radiological imaging techniques is usually mandatory for primary tumour visualisation, tumour staging and evaluation of treatment. In specific cases, as in patients with occult insulinomas, sampling procedures can provide a clue as to where to localise the insulin-hypersecreting pancreatic NETs. Recent developments in these fields have led to an increase in the detection rate of primary GEP-NETs and their metastatic deposits. Radiopharmaceuticals targeted at specific tumour cell properties and processes can be used to provide sensitive and specific whole-body imaging. Functional imaging also allows for patient selection for receptor-based therapies and prediction of the efficacy of such therapies. Positron emission tomography/computed tomography (CT) and single-photon emission CT/CT are used to map functional images with anatomical localisations. As a result, tumour imaging and tumour follow-up strategies can be optimised for every individual GEP-NET patient. In some cases, functional imaging might give indications with regard to future tumour behaviour and prognosis.

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Type 1 vasoactive intestinal peptide receptor expression in PC3/AR cells is evidence of prostate epithelial differentiation

2000

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Vasoactive Intestinal Peptide-Receptor Imaging for the Localization of Intestinal Adenocarcinomas and Endocrine Tumors

Abstract: Scanning with radiolabeled VIP can visualize intestinal tumors and metastases that express receptors for VIP.

Cited by 229 publications

References 15 publications

Identification of neuropeptide Y cleavage products in human blood to improve metabolic stability

Identification of neuropeptide Y cleavage products in human blood to improve metabolic stability

GEP-NETs update: Functional localisation and scintigraphy in neuroendocrine tumours of the gastrointestinal tract and pancreas (GEP-NETs)

Type 1 vasoactive intestinal peptide receptor expression in PC3/AR cells is evidence of prostate epithelial differentiation

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