Evaluation of radiolabelled bombesin analogues for receptor-targeted scintigraphy and radiotherapy

Breeman, W. A. P.; Hofland, Leo J.; Jong, Marion de; Bernard, Bert F.; Sinivasan, Ananth; Kwekkeboom, Dik J.; Visser, Theo J.; Krenning, Eric P.

doi:10.1002/(sici)1097-0215(19990517)81:4<658::aid-ijc24>3.0.co;2-p

Cited by 81 publications

(80 citation statements)

References 20 publications

(30 reference statements)

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“…For example, 99m Tcand 111 In-coupled BN analogues have been developed for diagnostic SPECT imaging and 64 Cu-and 68 Ga-labelled analogues for PET imaging of GRP receptor-expressing tumours [26][27][28][29][30][31][32][33][34][35][36][37][38][39]. In addition, 90 Y-and 177 Lu-labelled analogues have been described as promising tools for targeted radiotherapy of these tumours [26,40].…”

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confidence: 99%

“…We previously developed and evaluated the radiolabelled peptide [ 111 In-DTPA-Pro 1 ,Tyr 4 ]BN, a BN analogue which internalised rapidly into GRP receptor-positive tumour cells in vitro and in vivo [37][38][39]. In addition, GRP receptorexpressing CA20948 and AR42J tumours could be visualised using gamma camera imaging in rats after injection with this radiolabelled BN analogue [37,38].…”

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confidence: 99%

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Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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Purpose It has been shown that some primary human tumours and their metastases, including prostate and breast tumours, overexpress gastrin-releasing peptide (GRP) (5-14)), was tested in vivo in biodistribution studies using rats bearing GRP receptor-expressing CA20948 tumours, and nude mice bearing human PC3 xenografts. Injection of 111In-labelled Cmp 3 in these animals showed high, receptor-mediated uptake in receptor-positive organs and tumours which could be visualised using planar gamma camera and microSPECT/CT imaging. Conclusion With their enhanced receptor affinity and their rapid receptor-mediated internalisation in vitro and in vivo, the new BN analogues, and especially Cmp 3, are promising candidates for use in diagnostic molecular imaging and targeted radionuclide therapy of GRP receptor-expressing cancers.

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confidence: 99%

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Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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“…Coinjection of samples with aliquots of labeling reaction solutions in HPLC revealed the position of parent radiopeptides (indicated by green arrow); HPLC conditions and gradient systems applied are given in text. (6)(7)(8)(9)(10)(11)(12)(13)(14) sequences (3,14,15,18). Internalization efficacy of 99m Tc radioligands followed the same trend, with 99m Tc-SARNC5 (bAla 24 replacement) displaying clearly superior internalization capacity at all time points, whereas 99m Tc-SARNC4 (bAla 24 /Leu 27 combination) internalized poorly in PC-3 cells at 37°C (Fig.…”

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confidence: 78%

“…The success of radiolabeled BBN analogs to target GRPRexpressing cancer lesions in animal models and in humans has been partly attributed to their ability to internalize rapidly and massively into cancer cells after receptor binding. Internalization enhances trapping of the radiolabel into malignant cells, a process translating into higher diagnostic sensitivity or superior therapeutic efficacy depending on the radionuclide used for labeling (10,11).…”

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confidence: 99%

“…Analogous substitution of Gly by bAla in GRP (at position 24) or in BBN (at position 11) sequences have led to a broader BBR-affinity profile (3,14). The universal radiotracer 125 I-[dTyr 6 ,bAla 11 ,Phe 13 ,Nle 14 ] BBN (6)(7)(8)(9)(10)(11)(12)(13)(14) is likewise substituted in the corresponding position 11 of the BBN-tetradecapeptide motif by bAla (22). An alternative explanation for this difference may be assigned to interspecies homology and tissue expression differences reported between the mouse and the human GRPR (14,15,23,24).…”

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^99mTc Radiotracers Based on Human GRP(18-27): Synthesis and Comparative Evaluation

Marsouvanidis

Maina

Sallegger³

et al. 2013

J Nucl Med

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Gastrin-releasing peptide receptors (GRPRs) expressed on human tumors can serve as molecular targets for radiolabeled peptide analogs based on the frog tetradecapeptide bombesin (BBN). We have recently expanded this approach toward human GRP(18-27) sequences and introduced 99m Tc-demomedin C, our first radiotracer based on , showing favorable biologic characteristics during preclinical evaluation in rodents. We now present a series of 99m Tc-demomedin C analogs, generated by single-Gly 24 or double-Gly 24 /Met 27 substitutions in the peptide chain, and compare their performance in GRPR-positive in vitro and in vivo models. at 4 h after injection). 99m Tc-SARNC6 displayed the highest tumor-to-nontumor ratios followed by 99m Tc-SARNC2. Conclusion: This structure-activity relationship study has shown the impact of single-Gly 24 or double-Gly 24 /Met 27 substitutions in the 99m Tc-SARNC1 motif on key biologic parameters, including GRPR affinity, internalization efficiency, and in vivo stability, which eventually determine the pharmacokinetic profile of resulting radiopeptides. By revealing improved analogs, this study has strengthened the applicability perspectives of radioligands based on human GRP sequences in the detection and therapy of GRPRexpressing tumors in humans.

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Pre-clinical evaluation of [111In-DTPA-Pro1, Tyr4]bombesin, a new radioligand for bombesin-receptor scintigraphy

et al. 1999

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Evaluation of radiolabelled bombesin analogues for receptor-targeted scintigraphy and radiotherapy

Cited by 81 publications

References 20 publications

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

^99mTc Radiotracers Based on Human GRP(18-27): Synthesis and Comparative Evaluation

Pre-clinical evaluation of [111In-DTPA-Pro1, Tyr4]bombesin, a new radioligand for bombesin-receptor scintigraphy

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