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Current status and progress in using radiolabelled PARP-1 inhibitors for imaging PARP-1 expression in tumours
1Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing, 100875, PR China.
Abstract:
Poly(ADP-ribose) polymerase-1 (PARP-1) is a key enzyme in the DNA repair process, and the overexpression of PARP-1 in several tumours makes this enzyme a promising molecular target. Recently, several PARP-1 inhibitors, such as olaparib, rucaparib, niraparib and talazoparib, have been clinically approved as anticancer drugs. Several of these inhibitors have been radiolabelled for noninvasive imaging of PARP-1 expression in several types of tumours. In this review, the background and progress for using various radiolabelled PARP-1 inhibitors for cancer diagnosis are discussed and future development directions are proposed.
Insights
Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors are approved anticancer drugs. Radiolabeled PARP-1 inhibitors show promise for noninvasive cancer diagnosis and imaging of PARP-1 expression in tumors.
Area of Science:
- Biochemistry
- Oncology
- Radiochemistry
Background:
- Poly(ADP-ribose) polymerase-1 (PARP-1) is crucial for DNA repair.
- PARP-1 overexpression in tumors presents a therapeutic and diagnostic target.
- Approved PARP-1 inhibitors include olaparib, rucaparib, niraparib, and talazoparib.
Purpose of the Study:
- To review the development of radiolabeled PARP-1 inhibitors for cancer diagnosis.
- To discuss current progress and future directions in this field.
Main Methods:
- Review of existing literature on PARP-1 inhibitors and their radiolabeling.
- Analysis of studies utilizing radiolabeled PARP-1 inhibitors for tumor imaging.
Main Results:
- Several PARP-1 inhibitors have been successfully radiolabeled.
- These radiolabeled compounds enable noninvasive imaging of PARP-1 expression in various cancers.
Conclusions:
- Radiolabeled PARP-1 inhibitors represent a significant advancement in cancer diagnostics.
- Further research is needed to optimize their use and expand their clinical application.
