Log in



C2TN

 
RADIOLABELED LXXLL PEPTIDES FOR ESTROGEN RECEPTOR TARGETING: 111In- VERSUS 125I-LABELLING

 CR3

Small peptides containing the LXXLL sequence have demonstrated high affinity for the estrogen receptor (ER), an attractive target for molecular imaging and radionuclide therapy of breast cancer. Thus, we have evaluated small LXXLL peptides radiolabelled with two different radionuclides, 111In and 125I, that have potential to be used in theranostics due to the simultaneous emission of gamma radiation and Auger electrons. 111In- and 125I-labelled peptides were obtained in high radiochemical yield and purity. LXXLL based peptides retained ER binding affinity after complexation with indium or iodination at the His residue. Both radiolabelled peptides have showed rapid and high uptake in MCF-7 cells and internalize in the nucleus. Biodistribution studies in female mice demonstrated that both radiolabelled peptides are stable in vivo have a rapid blood clearance and high uptake in ER rich

 

Contact PersonLurdes Gano

 

More details in:

Vultos, F. et al. (2017) A Multifunctional Radiotheranostic Agent for Dual Targeting of Breast Cancer Cells, ChemMedChem, 12, 1103 –1107, DOI:10.1002/cmdc. 201700 287