Current status and progress in using radiolabelled PARP-1 inhibitors for imaging PARP-1 expression in tumours.

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.