Publication

Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer

Yu, Z., Carlucci, G., Ananias, H. J. K., Dierckx, R. A. J. O., Liu, S., Helfrich, W., Wang, F., de Jong, I. J. & Elsinga, P. H., Feb-2013, In : Amino Acids. 44, 2, p. 543-553 11 p.

Research output: Contribution to journalArticleAcademicpeer-review

APA

Yu, Z., Carlucci, G., Ananias, H. J. K., Dierckx, R. A. J. O., Liu, S., Helfrich, W., Wang, F., de Jong, I. J., & Elsinga, P. H. (2013). Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer. Amino Acids, 44(2), 543-553. https://doi.org/10.1007/s00726-012-1369-9

Author

Yu, Zilin ; Carlucci, Giuseppe ; Ananias, Hildo J. K. ; Dierckx, Rudi A. J. O. ; Liu, Shuang ; Helfrich, Wijnand ; Wang, Fan ; de Jong, Igle J. ; Elsinga, Philip H. / Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer. In: Amino Acids. 2013 ; Vol. 44, No. 2. pp. 543-553.

Harvard

Yu, Z, Carlucci, G, Ananias, HJK, Dierckx, RAJO, Liu, S, Helfrich, W, Wang, F, de Jong, IJ & Elsinga, PH 2013, 'Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer', Amino Acids, vol. 44, no. 2, pp. 543-553. https://doi.org/10.1007/s00726-012-1369-9

Standard

Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer. / Yu, Zilin; Carlucci, Giuseppe; Ananias, Hildo J. K.; Dierckx, Rudi A. J. O.; Liu, Shuang; Helfrich, Wijnand; Wang, Fan; de Jong, Igle J.; Elsinga, Philip H.

In: Amino Acids, Vol. 44, No. 2, 02.2013, p. 543-553.

Research output: Contribution to journalArticleAcademicpeer-review

Vancouver

Yu Z, Carlucci G, Ananias HJK, Dierckx RAJO, Liu S, Helfrich W et al. Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer. Amino Acids. 2013 Feb;44(2):543-553. https://doi.org/10.1007/s00726-012-1369-9


BibTeX

@article{5c9b3e1a024c4a1393b3ead88c7cfb32,
title = "Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer",
abstract = "Multimerization of peptides can improve the binding characteristics of the tracer by increasing local ligand concentration and decreasing dissociation kinetics. In this study, a new bombesin homodimer was developed based on an epsilon-aminocaproic acid-bombesin(7-14) (Aca-bombesin(7-14)) fragment, which has been studied for targeting the gastrin-releasing peptide receptor (GRPR) in prostate cancer. The bombesin homodimer was conjugated to 6-hydrazinopyridine-3-carboxylic acid (HYNIC) and labeled with Tc-99m for SPECT imaging. The in vitro binding affinity to GRPR, cell uptake, internalization and efflux kinetics of the radiolabeled bombesin dimer were investigated in the GRPR-expressing human prostate cancer cell line PC-3. Biodistribution and the GRPR-targeting potential were evaluated in PC-3 tumor-bearing athymic nude mice. When compared with the bombesin monomer, the binding affinity of the bombesin dimer is about ten times lower. However, the Tc-99m labeled bombesin dimer showed a three times higher cellular uptake at 4 h after incubation, but similar internalization and efflux characters in vitro. Tumor uptake and in vivo pharmacokinetics in PC-3 tumor-bearing mice were comparable. The tumor was visible on the dynamic images in the first hour and could be clearly distinguished from non-targeted tissues on the static images after 4 h. The GRPR-targeting ability of the Tc-99m labeled bombesin dimer was proven in vitro and in vivo. This bombesin homodimer provides a good starting point for further studies on enhancing the tumor targeting activity of bombesin multimers.",
keywords = "GRPR, Bombesin homodimer, Radiolabeled, Imaging, Prostate cancer, PC-3, Tc-99m, HYNIC, SPECT, GASTRIN-RELEASING-PEPTIDE, ALPHA(V)BETA(3) INTEGRIN, RGD PEPTIDES, HETERODIMER, TUMORS, PET, IMMUNOREACTIVITY, EXPRESSION, ANALOGS, DIMERS",
author = "Zilin Yu and Giuseppe Carlucci and Ananias, {Hildo J. K.} and Dierckx, {Rudi A. J. O.} and Shuang Liu and Wijnand Helfrich and Fan Wang and {de Jong}, {Igle J.} and Elsinga, {Philip H.}",
year = "2013",
month = feb,
doi = "10.1007/s00726-012-1369-9",
language = "English",
volume = "44",
pages = "543--553",
journal = "Amino Acids",
issn = "0939-4451",
publisher = "SPRINGER WIEN",
number = "2",

}

RIS

TY - JOUR

T1 - Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer

AU - Yu, Zilin

AU - Carlucci, Giuseppe

AU - Ananias, Hildo J. K.

AU - Dierckx, Rudi A. J. O.

AU - Liu, Shuang

AU - Helfrich, Wijnand

AU - Wang, Fan

AU - de Jong, Igle J.

AU - Elsinga, Philip H.

PY - 2013/2

Y1 - 2013/2

N2 - Multimerization of peptides can improve the binding characteristics of the tracer by increasing local ligand concentration and decreasing dissociation kinetics. In this study, a new bombesin homodimer was developed based on an epsilon-aminocaproic acid-bombesin(7-14) (Aca-bombesin(7-14)) fragment, which has been studied for targeting the gastrin-releasing peptide receptor (GRPR) in prostate cancer. The bombesin homodimer was conjugated to 6-hydrazinopyridine-3-carboxylic acid (HYNIC) and labeled with Tc-99m for SPECT imaging. The in vitro binding affinity to GRPR, cell uptake, internalization and efflux kinetics of the radiolabeled bombesin dimer were investigated in the GRPR-expressing human prostate cancer cell line PC-3. Biodistribution and the GRPR-targeting potential were evaluated in PC-3 tumor-bearing athymic nude mice. When compared with the bombesin monomer, the binding affinity of the bombesin dimer is about ten times lower. However, the Tc-99m labeled bombesin dimer showed a three times higher cellular uptake at 4 h after incubation, but similar internalization and efflux characters in vitro. Tumor uptake and in vivo pharmacokinetics in PC-3 tumor-bearing mice were comparable. The tumor was visible on the dynamic images in the first hour and could be clearly distinguished from non-targeted tissues on the static images after 4 h. The GRPR-targeting ability of the Tc-99m labeled bombesin dimer was proven in vitro and in vivo. This bombesin homodimer provides a good starting point for further studies on enhancing the tumor targeting activity of bombesin multimers.

AB - Multimerization of peptides can improve the binding characteristics of the tracer by increasing local ligand concentration and decreasing dissociation kinetics. In this study, a new bombesin homodimer was developed based on an epsilon-aminocaproic acid-bombesin(7-14) (Aca-bombesin(7-14)) fragment, which has been studied for targeting the gastrin-releasing peptide receptor (GRPR) in prostate cancer. The bombesin homodimer was conjugated to 6-hydrazinopyridine-3-carboxylic acid (HYNIC) and labeled with Tc-99m for SPECT imaging. The in vitro binding affinity to GRPR, cell uptake, internalization and efflux kinetics of the radiolabeled bombesin dimer were investigated in the GRPR-expressing human prostate cancer cell line PC-3. Biodistribution and the GRPR-targeting potential were evaluated in PC-3 tumor-bearing athymic nude mice. When compared with the bombesin monomer, the binding affinity of the bombesin dimer is about ten times lower. However, the Tc-99m labeled bombesin dimer showed a three times higher cellular uptake at 4 h after incubation, but similar internalization and efflux characters in vitro. Tumor uptake and in vivo pharmacokinetics in PC-3 tumor-bearing mice were comparable. The tumor was visible on the dynamic images in the first hour and could be clearly distinguished from non-targeted tissues on the static images after 4 h. The GRPR-targeting ability of the Tc-99m labeled bombesin dimer was proven in vitro and in vivo. This bombesin homodimer provides a good starting point for further studies on enhancing the tumor targeting activity of bombesin multimers.

KW - GRPR

KW - Bombesin homodimer

KW - Radiolabeled

KW - Imaging

KW - Prostate cancer

KW - PC-3

KW - Tc-99m

KW - HYNIC

KW - SPECT

KW - GASTRIN-RELEASING-PEPTIDE

KW - ALPHA(V)BETA(3) INTEGRIN

KW - RGD PEPTIDES

KW - HETERODIMER

KW - TUMORS

KW - PET

KW - IMMUNOREACTIVITY

KW - EXPRESSION

KW - ANALOGS

KW - DIMERS

U2 - 10.1007/s00726-012-1369-9

DO - 10.1007/s00726-012-1369-9

M3 - Article

VL - 44

SP - 543

EP - 553

JO - Amino Acids

JF - Amino Acids

SN - 0939-4451

IS - 2

ER -

ID: 5769506