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 journalArticlepeer-review

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

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

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