(2S)-2-(3-(1-Carboxy-5-(4-211At-Astatobenzamido)Pentyl)Ureido)-Pentanedioic Acid for PSMA-Targeted α-Particle Radiopharmaceutical Therapy.

ABSTRACT: Alpha-particle emitters have a high linear energy transfer and short range, offering the potential for treating micrometastases while sparing normal tissues. We developed a urea-based, ²¹¹At-labeled small molecule targeting prostate-specific membrane antigen (PSMA) for the treatment of micrometastases due to prostate cancer (PC).

Methods

PSMA-targeted (2S)-2-(3-(1-carboxy-5-(4-²¹¹At-astatobenzamido)pentyl)ureido)-pentanedioic acid (²¹¹At- 6: ) was synthesized. Cellular uptake and clonogenic survival were tested in PSMA-positive (PSMA+) PC3 PIP and PSMA-negative (PSMA-) PC3 flu human PC cells after ²¹¹At- 6: treatment. The antitumor efficacy of ²¹¹At- 6: was evaluated in mice bearing PSMA+ PC3 PIP and PSMA- PC3 flu flank xenograf

SUBMITTER: Kiess AP 

PROVIDER: S-EPMC5367442 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature