PEGylation of Tc-99m-labeled bombesin analogues improves their pharmacokinetic properties

S. Daepp; Elisa Garcia-Garayoa; Veronique Maes; Luc Brans; Dirk Tourwe; Muller Christina; R. Schibli

PEGylation of Tc-99m-labeled bombesin analogues improves their pharmacokinetic properties

S. Daepp, Elisa Garcia-Garayoa, Veronique Maes, Luc Brans, Dirk Tourwe, Muller Christina, R. Schibli

Research output: Contribution to journal › Article › peer-review

33 Citations (Scopus)

Abstract

Abstract: Introduction: Radiolabeled bombesin (BN) conjugates are promising radiotracers for imaging and therapy of breast and prostate tumors in which BN2-gastrin-releasing peptide (GRP) receptors are overexpressed. However, the low in vivo stability of BN conjugates may limit their clinical application. In an attempt to improve their pharmacokinetics and counteract their rapid enzymatic degradation, we prepared a series of polyethylene glycol (PEG)-ylated BN(7-14) analogues for radiolabeling with Tc-99m(CO)(3) and evaluated them in vitro and in vivo.

Original language	English
Pages (from-to)	997-1009
Number of pages	13
Journal	Nuclear Medicine and Biology
Volume	38
Issue number	7
Publication status	Published - Oct 2011

Keywords

Gastrin-releasing peptide receptor
bombesin
Technetium-99m
SPECT/CT imaging
PEGylation
Prostate cancer

Biological Research Center (External organisation)
Dirk Tourwe (Member)
8 Mar 2001 → …
Activity: Membership › Membership of external research organisation

Cite this

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title = "PEGylation of Tc-99m-labeled bombesin analogues improves their pharmacokinetic properties",

abstract = "Abstract: Introduction: Radiolabeled bombesin (BN) conjugates are promising radiotracers for imaging and therapy of breast and prostate tumors in which BN2-gastrin-releasing peptide (GRP) receptors are overexpressed. However, the low in vivo stability of BN conjugates may limit their clinical application. In an attempt to improve their pharmacokinetics and counteract their rapid enzymatic degradation, we prepared a series of polyethylene glycol (PEG)-ylated BN(7-14) analogues for radiolabeling with Tc-99m(CO)(3) and evaluated them in vitro and in vivo.",

keywords = "Gastrin-releasing peptide receptor, bombesin, Technetium-99m, SPECT/CT imaging, PEGylation, Prostate cancer",

author = "S. Daepp and Elisa Garcia-Garayoa and Veronique Maes and Luc Brans and Dirk Tourwe and Muller Christina and R. Schibli",

year = "2011",

month = oct,

language = "English",

volume = "38",

pages = "997--1009",

journal = "Nuclear Medicine and Biology",

issn = "0969-8051",

publisher = "Elsevier Inc.",

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}

TY - JOUR

T1 - PEGylation of Tc-99m-labeled bombesin analogues improves their pharmacokinetic properties

AU - Daepp, S.

AU - Garcia-Garayoa, Elisa

AU - Maes, Veronique

AU - Brans, Luc

AU - Tourwe, Dirk

AU - Christina, Muller

AU - Schibli, R.

PY - 2011/10

Y1 - 2011/10

N2 - Abstract: Introduction: Radiolabeled bombesin (BN) conjugates are promising radiotracers for imaging and therapy of breast and prostate tumors in which BN2-gastrin-releasing peptide (GRP) receptors are overexpressed. However, the low in vivo stability of BN conjugates may limit their clinical application. In an attempt to improve their pharmacokinetics and counteract their rapid enzymatic degradation, we prepared a series of polyethylene glycol (PEG)-ylated BN(7-14) analogues for radiolabeling with Tc-99m(CO)(3) and evaluated them in vitro and in vivo.

AB - Abstract: Introduction: Radiolabeled bombesin (BN) conjugates are promising radiotracers for imaging and therapy of breast and prostate tumors in which BN2-gastrin-releasing peptide (GRP) receptors are overexpressed. However, the low in vivo stability of BN conjugates may limit their clinical application. In an attempt to improve their pharmacokinetics and counteract their rapid enzymatic degradation, we prepared a series of polyethylene glycol (PEG)-ylated BN(7-14) analogues for radiolabeling with Tc-99m(CO)(3) and evaluated them in vitro and in vivo.

KW - Gastrin-releasing peptide receptor

KW - bombesin

KW - Technetium-99m

KW - SPECT/CT imaging

KW - PEGylation

KW - Prostate cancer

M3 - Article

VL - 38

SP - 997

EP - 1009

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

SN - 0969-8051

IS - 7

ER -

PEGylation of Tc-99m-labeled bombesin analogues improves their pharmacokinetic properties

Abstract

Keywords

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Biological Research Center (External organisation)

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