MUC1-Targeted Radiopharmaceuticals in Cancer Imaging and Therapy.

Mucin 1 (MUC1) is a large, transmembrane mucin glycoprotein overexpressed in most adenocarcinomas and plays an important role in tumor progression. Regarding its cellular distribution, biochemical features, and function, tumor-related MUC1 varies from the MUC1 expressed in normal cells. Therefore, targeting MUC1 for cancer immunotherapy and imaging can exploit the difference between cancerous and normal cells.

Evaluation of a New Tc-labeled GnRH Analogue as a Possible Imaging Agent for Prostate Cancer Detection.

Introduction: Prostate cancer is a serious threat to men's health so it is necessary to develop technics for early detection of this malignancy. The purpose of this research was the evaluation of a newTc-labeled GnRH analogue as an imaging probe for tumor targeting of prostate cancer.

Methods: Tc-labeled-DLys6-GnRH analogue was prepared based on HYNIC as a chelating agent and tricine/ EDDA as coligands for labeling with Tc.

Preparation and evaluation of Tc-HYNIC- (TPPE) as a new targeted imaging probe for detection of colon cancer: Preclinical comparison with Tc-HYNIC-EPPT.

The aim of this study was to prepare radiolabeled peptide-based agents for imaging of colon cancer. According to the incorporation of HYNIC for radiolabeling with technetium-99m, two analogs were designed and compared: an antitumor-antibody-derived peptide based on the EPPT sequence and a novel retro-inverso peptidomimetic derivative (TPPE) structurally modified by replacing the L-amino acids with D-amino acids and reversing the primary amino acid sequence of EPPT. The HYNIC-conjugated peptides were labeled with Tc using tricine/EDDA coligand with more than 98% radiochemical yield and showed high metabolic stability.

In vitro/in vivo assessment of the targeting ability of [Tc] Tc-labeled an aptide specific to the extra domain B of fibronectin (APT) for colorectal cancer.

Objective: The APT is an aptide specific to the extra domain B (EDB) of fibronectin with high affinity for EDB, which is expressed in malignant tumors including brain cancer (U87MG) and colorectal cancer (HT-29). Aim of this study was to evaluate the [Tc] Tc-APT potential as an imaging probe for colorectal cancer.

Methods: Radiochemical purity was evaluated by HPLC and radio-isotope TLC scanner.

Structural modifications of amino acid sequences of radiolabeled peptides for targeted tumor imaging.

Molecular imaging techniques are increasingly being used in localization, staging and therapy control of cancer. Due to their unique target specificity for the endogenous receptors, radiopeptides have been used widely for the development of radiopharmaceuticals for targeted tumor imaging in nuclear oncology. It is necessary to modify radiolabeled peptides in order to achieve more effective agents.

Tc-(EDDA/tricine)-HYNIC-GnRH analogue as a potential imaging probe for diagnosis of prostate cancer.

Prostate cancer is a serious threat to men's health, so it is necessary to develop the techniques for early detection of this malignancy. Radiolabeled peptides are the useful tools for diagnosis of prostate cancer. In this research, we designed a new HYNIC-conjugated GnRH analogue and labeled it by Tc with tricine/EDDA as coligands.

The Influence of Different Spacers on Biological Profile of Peptide Radiopharmaceuticals for Diagnosis and Therapy of Human Cancers.

Background: Cancer is the leading cause of death worldwide. Early detection can reduce the disadvantageous effects of diseases and the mortality in cancer. Nuclear medicine is a powerful tool that has the ability to diagnose malignancy without harming normal tissues.

99mTc-D(RGD): molecular imaging probe for diagnosis of αvβ3-positive tumors.

Objective: Arginine-glycine-aspartic acid (RGD) peptide with its specific binding affinity to integrin αvβ3, is widely investigated for the development of molecular imaging probes for diagnosis of αvβ3-positive tumors. The aim of this work was to evaluate the ability of Tc- HYNIC-D(RGD), a novel retro-inverso peptidomimetic derivative for U87MG tumor (αvβ3-positive) imaging.

Methods: HYNIC-D(RGD) labeled with Tc using tricine/EDDA as an exchange coligands.