Development of a Tetrathioether (S4) Bifunctional Chelate System for Rh-105
Abstract
We have previously, in the first year of this award, synthesized a new rhodium tetrathioether bombesin analogue, [Rh-S4-8Aoc-BBN(7-14)NH2]+. During the current period of investigation the molecule was tested for receptor binding affinity to the BB2 receptor on human prostate cancer PC-3 cells. Rhodium-105 radiolabeling studies were carried out with the S4-8Aoc-BBN(7-14)NH2 ligand system and also with other known chelate systems 3,3,3,3-S4-Diol, 3,3,3-S4-(COOH)2. The [Rh-S4-8Aoc-BBN(7-14)NH2]+ was found to exhibit a high affinity for the BB2 receptor (IC50 = 2.2 0.3 nM) however high yields of the radiolabeled [105Rh-S4-8Aoc-BBN(7-14)NH2]+ complex were not achieved under any conditions tested. To better understand these results, the 3,3,3,3-S4-Diol and 3,3,3-S4-(COOH)2 were investigated. It was revealed that traditional radiolabeling techniques for 105Rh are not compatible with systems that contain a carboxylic acid group.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jul 01, 2013
- Accession Number
- ADA581448
Entities
People
- Don Wycoff
- Fabio Gallizzi
- Gary Sieckman
- Silvia Jurisson
- Timothy Hoffman
- Valerie Carroll
Organizations
- University of Missouri