Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Rebekka Hueting; Martin Christlieb; Jonathan R Dilworth; Elisa Garcia-Garayoa; Veronique Gouverneur; Michael W. Jones; Veronique Maes; R. Schibli; X. Sun; Dirk Tourwe

Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Rebekka Hueting, Martin Christlieb, Jonathan R Dilworth, Elisa Garcia-Garayoa, Veronique Gouverneur, Michael W. Jones, Veronique Maes, R. Schibli, X. Sun, Dirk Tourwe

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44 Citations (Scopus)

Abstract

Abstract: A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both Cu-64 and Tc-99m. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic methodologies and the Cu-64-labeled conjugate was shown to have good tumour uptake in mice with xenografted PC-3 tumours.

Original language	English
Pages (from-to)	3620-3632
Journal	Dalton Transactions
Volume	39
Issue number	15
Publication status	Published - 1 Jan 2010

Keywords

COPPER RADIOPHARMACEUTICALS
BOMBESIN ANALOGS
IN-VITRO
COMPLEXES
HYPOXIA
BIODISTRIBUTION
CHEMISTRY
TUMORS
AGENT
TOOLS

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title = "Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides",

abstract = "Abstract: A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both Cu-64 and Tc-99m. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic methodologies and the Cu-64-labeled conjugate was shown to have good tumour uptake in mice with xenografted PC-3 tumours.",

keywords = "COPPER RADIOPHARMACEUTICALS, BOMBESIN ANALOGS, IN-VITRO, COMPLEXES, HYPOXIA, BIODISTRIBUTION, CHEMISTRY, TUMORS, AGENT, TOOLS",

author = "Rebekka Hueting and Martin Christlieb and Dilworth, {Jonathan R} and Elisa Garcia-Garayoa and Veronique Gouverneur and Jones, {Michael W.} and Veronique Maes and R. Schibli and X. Sun and Dirk Tourwe",

year = "2010",

month = jan,

day = "1",

language = "English",

volume = "39",

pages = "3620--3632",

journal = "Dalton Transactions",

issn = "1477-9226",

publisher = "Royal Society of Chemistry",

number = "15",

}

TY - JOUR

T1 - Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

AU - Hueting, Rebekka

AU - Christlieb, Martin

AU - Dilworth, Jonathan R

AU - Garcia-Garayoa, Elisa

AU - Gouverneur, Veronique

AU - Jones, Michael W.

AU - Maes, Veronique

AU - Schibli, R.

AU - Sun, X.

AU - Tourwe, Dirk

PY - 2010/1/1

Y1 - 2010/1/1

N2 - Abstract: A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both Cu-64 and Tc-99m. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic methodologies and the Cu-64-labeled conjugate was shown to have good tumour uptake in mice with xenografted PC-3 tumours.

AB - Abstract: A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both Cu-64 and Tc-99m. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic methodologies and the Cu-64-labeled conjugate was shown to have good tumour uptake in mice with xenografted PC-3 tumours.

KW - COPPER RADIOPHARMACEUTICALS

KW - BOMBESIN ANALOGS

KW - IN-VITRO

KW - COMPLEXES

KW - HYPOXIA

KW - BIODISTRIBUTION

KW - CHEMISTRY

KW - TUMORS

KW - AGENT

KW - TOOLS

M3 - Article

SN - 1477-9226

VL - 39

SP - 3620

EP - 3632

JO - Dalton Transactions

JF - Dalton Transactions

IS - 15

ER -

Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Abstract

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