The design and synthesis of a series of highly selective hydroxamate inhibitors of stromelysin-1 (MMP-3) is described.
Among them , we identified the 5-benzoyloxyisoquinolin-1 (2 H) - one derivative as the most selective PARP-2 inhibitor reported so far , with a PARP-2 / PARP-1 selectivity index greater than 60.
We propose to call this enzyme poly (ADP-ribose) polymerase 2 (PARP-2).
A good correlation between poly (ADP-ribose) polymerase activity and the level of the transcript of the gene coding for the enzyme was observed in many tissues.
An active poly (ADP-ribose) synthetase has been found to be associated to mitochondria of frog oocytes and of testis from various species.