Radiolabeled PARP Inhibitors for Imaging and Targeted Radiotherapy of Prostate Cancer
Abstract
The objective of this grant was to investigate a 77Br-labeled poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor for Auger radiation targeted radiotherapy of mCRPC. PARP-1 is a nuclear enzyme which initiates DNA repair by binding to the sites of single- or double-strand breaks (SSB/DSB). The major goals of this project were to 1.) determine the therapeutic efficacy of [77Br]WC-DZ-Br in PC-3 and IGR-CaP1 cells, 2.) determine the therapeutic efficacy of [77Br]WC-DZ-Br in mice bearing subcutaneous PC-3 and IGR-CaP1 tumors, 3.) determine the therapeutic efficacy of [77Br]WC-DZ-Br in the IGR-CaP1 metastatic model. The significant results of this project were that [77Br]WC-DZ-Br induced significant cell killing and DNA damage in cells, it demonstrated significant tumor growth delay in mice bearing subcutaneous PC-3 and IGR-CaP1 tumors, and that near significance was reached when evaluating this therapy in the metastatic model.
Document Details
- Document Type
- Technical Report
- Publication Date
- Dec 01, 2023
- Accession Number
- AD1225081
Entities
People
- Buck Rogers
Organizations
- Washington University in St. Louis