Design of radiolabeled gelatinase inhibitor peptide ((99m)Tc-CLP) and evaluation in rats.

In malignant tissues, MMP-9 (gelatinase B, 92 kDa type IV collagenase) and MMP-2 (gelatinase A, 72 kDa type IV collagenase) are the most prevalent matrix metalloproteinases related to the tumor aggressiveness and metastatic potential. Since elevated levels of gelatinases are associated with poor prognosis in cancer patients, these enzymes are potential targets for tumor imaging to possibly predict metastases. In the present study, a cyclic decapeptide, CLP (Cys-Leu-Pro-Gly-His-Trp-Gly-Phe-Pro-Ser-Cys), was selected as a basic peptide because of its selective inhibitory activity toward gelatinases.

Design of (99m) Tc-DTPA-CLP and preliminary evaluation in rats.

Radiopharmaceuticals are localized in (malignant) tumor tissues by different mechanisms. One of these mechanisms, gelatinase enzyme activity, is associated with poor prognosis in cancer patients and potential targets for tumor imaging. There are some gelatinases to be associated with metastatic potential for tumor imaging to possibly predict metastases.

Design and synthesis of 99mTc-citro-folate for use as a tumor-targeted radiopharmaceutical.

Folate conjugates exhibit high affinity for folate receptor (FR) positive cells and tissues, such as those in tumors, making them attractive candidates and of interest in diagnostic tumor imaging. The aim of study was to synthesize a novel radiopharmaceutical based folate conjugate, (99m)Tc-citro-folate, and to evaluate its efficiency as a targeted agent for imaging tumors that over express FR. TLC, HPLC (1)H NMR and LC-MS/MS methods were used to check and confirm the synthesized citro-folate.