Targeting of gelatinase activity with a radiolabeled cyclic HWGF peptide.
Matrix metalloproteinases (MMPs) are a family of proteinases that play an important role in cancer as well as in numerous diseases. In this article, we describe the labeling of a phage display selected cyclic decapeptide containing the HWGF (histidine-tryptophane-glycine-phenylalanine) sequence to target MMP-2 and MMP-9. To evaluate the ability of this labeled peptide to monitor non invasively MMP-2 and MMP-9 activity, in vitro studies, biodistribution, competition studies and plasma metabolites analyses in Lewis Lung cancer tumor bearing mice were performed.
Kuhnast
B
B
Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universitaet Muenchen, 81675 Munich, Germany. kuhnast@shfj.cea.fr
Bodenstein
C
C
Haubner
R
R
Wester
H J
HJ
Senekowitsch-Schmidtke
R
R
Schwaiger
M
M
Weber
W A
WA
D000818:Animals; D014408:Biomarkers, Tumor / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods; D004789:Enzyme Activation; D005260:Female; D018093:Gelatinases / Q000378:metabolism; D007457:Iodine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D007553:Isotope Labeling / Q000379:methods; D008175:Lung Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism*; D020780:Matrix Metalloproteinase 9 / Q000378:metabolism*; D008657:Metabolic Clearance Rate; D051379:Mice; D008807:Mice, Inbred BALB C; D009928:Organ Specificity; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D014018:Tissue Distribution
D014408:Biomarkers, Tumor; D007457:Iodine Radioisotopes; D010456:Peptides, Cyclic; D019275:Radiopharmaceuticals; D018093:Gelatinases; D020778:Matrix Metalloproteinase 2; D020780:Matrix Metalloproteinase 9