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 language | English |
|---|---|
| Pages (from-to) | 4393-4397 |
| Number of pages | 5 |
| Journal | Cancer Research |
| Volume | 61 |
| Issue number | 11 |
| Publication status | Published - Jun 1 2001 |
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ASJC Scopus subject areas
- Cancer Research
- Oncology
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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 journal › Article
}
TY - JOUR
T1 - 111In-labeled 1,4,7,10-tetraazacyclododecane- N,N′,N″,N‴-tetraacetic acid-Lys8-vasotocin
T2 - A new powerful radioligand for oxytocin receptor-expressing tumors
AU - Bussolati, G.
AU - Chinol, M.
AU - Chini, B.
AU - Nacca, A.
AU - Cassoni, P.
AU - Paganelli, G.
PY - 2001/6/1
Y1 - 2001/6/1
N2 - 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.
AB - 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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UR - http://www.scopus.com/inward/citedby.url?scp=0035354185&partnerID=8YFLogxK
M3 - Article
VL - 61
SP - 4393
EP - 4397
JO - Journal of Cancer Research
JF - Journal of Cancer Research
SN - 0008-5472
IS - 11
ER -