111In-labeled 1,4,7,10-tetraazacyclododecane- N,N′,N″,N‴-tetraacetic acid-Lys8-vasotocin

A new powerful radioligand for oxytocin receptor-expressing tumors

G. Bussolati, M. Chinol, B. Chini, A. Nacca, P. Cassoni, G. Paganelli

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

We developed a radioactive ligand for tumors expressing oxytocin receptors (OTRs) by linking the chelating agent 1,4,7,10-tetraazacyclododecane. N,N′,N″,N‴-tetraacetic acid (DOTA) to Lys8-vasotocin (LVT), an analogue of oxytocin with high affinity for OTRs. The new reagent (DOTA-LVT) retained high affinity for human OTRs, as proved by in vitro affinity binding to cells endogenously expressing OTRs, such as MCF7 breast carcinoma and MOG-U-V-W glioblastoma cells lines, as well as to transiently transfected COS7 cells. In in vivo experiments, DOTA-LVT carrying 111In showed specific binding activity to OTR-positive TS/A mouse mammary tumors. The present study opens new perspectives for imaging and, possibly, therapy of OTR-positive human tumors such as breast and endometrial carcinomas, neuroblastomas, and glioblastomas.

Original languageEnglish
Pages (from-to)4393-4397
Number of pages5
JournalCancer Research
Volume61
Issue number11
Publication statusPublished - Jun 1 2001

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Oxytocin Receptors
Vasotocin
Acids
Glioblastoma
Breast Neoplasms
Neoplasms
Oxytocin
Endometrial Neoplasms
Chelating Agents
Neuroblastoma
Ligands
Cell Line
cyclen
human OXTR protein

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

111In-labeled 1,4,7,10-tetraazacyclododecane- N,N′,N″,N‴-tetraacetic acid-Lys8-vasotocin : A new powerful radioligand for oxytocin receptor-expressing tumors. / Bussolati, G.; Chinol, M.; Chini, B.; Nacca, A.; Cassoni, P.; Paganelli, G.

In: Cancer Research, Vol. 61, No. 11, 01.06.2001, p. 4393-4397.

Research output: Contribution to journalArticle

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abstract = "We developed a radioactive ligand for tumors expressing oxytocin receptors (OTRs) by linking the chelating agent 1,4,7,10-tetraazacyclododecane. N,N′,N″,N‴-tetraacetic acid (DOTA) to Lys8-vasotocin (LVT), an analogue of oxytocin with high affinity for OTRs. The new reagent (DOTA-LVT) retained high affinity for human OTRs, as proved by in vitro affinity binding to cells endogenously expressing OTRs, such as MCF7 breast carcinoma and MOG-U-V-W glioblastoma cells lines, as well as to transiently transfected COS7 cells. In in vivo experiments, DOTA-LVT carrying 111In showed specific binding activity to OTR-positive TS/A mouse mammary tumors. The present study opens new perspectives for imaging and, possibly, therapy of OTR-positive human tumors such as breast and endometrial carcinomas, neuroblastomas, and glioblastomas.",
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AU - Paganelli, G.

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