Evaluation of laminin peptide fragments labeled with indium-111 for the potential imaging of malignant tumors.
The laminin peptide fragments GYIGSR-NH2 and CDPGYIGSR-NH2 are known to bind to a 67-kDa laminin receptor. This receptors is understood to be expressed at higher than normal levels in malignant tumor cells, particularly those of breast and colon carcinomas. Peptides DTPA-GYIGSR-NH2 (1), DTPA-(GYIGSR-NH2)2 (2), DTPA-CDPGYIGSR-NH2 (3), DTPA-(CDPGYIGSR-NH2)2 (4), and negative control DTPA-GAGAGA-NH2 (5) were prepared by solid-phase peptide synthesis. All five DTPA-conjugated peptides were subsequently radiolabeled with 111In and their tissue distribution evaluated in mice bearing C3H tumors. 111In-3 and 111In-4 showed the highest specific tumor localization. These preliminary data support further study of radiolabeled petide fragments for the potential detection of malignant tumors of the breast and other organs.
Mokotoff
M
M
Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pennsylvania, USA. mokotoff@druginfonet.pharm-epid.pitt.edu
Swanson
D P
DP
Jonnalagadda
S S
SS
Epperly
M W
MW
Brown
M L
ML
D000595:Amino Acid Sequence; D000818:Animals; D004195:Disease Models, Animal; D005260:Female; D007205:Indium Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D007797:Laminin / Q000737:chemistry*; D008325:Mammary Neoplasms, Experimental / Q000000981:diagnostic imaging*; D051379:Mice; D008809:Mice, Inbred C3H; D010446:Peptide Fragments / Q000737:chemistry / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D014018:Tissue Distribution
D007205:Indium Radioisotopes; D007797:Laminin; D010446:Peptide Fragments