INHIBITORS AND ACTIVATORS OF ADP-RIBOSYLATION REACTIONS

ADP-ribosylation reaction, that is the transfer of the ADP-ribose moie ty of NAD(+) to acceptor protein, is catalyzed by two classes of ADP-r ibosyltransferases, i.e., poly(ADP-ribose) synthetase and mono(ADP-rib osyl)transferases. These two types differ not only in the number of tr ansferring ADP-ribose units but also in the acceptor amino acid(s) and protein. Their inhibitors, particularly those of poly(ADP-ribose) syn thetase, have been successfully employed in studies on biological func tions of the enzymes and other related fields of research. Recently, w e found many potent and specific inhibitors of poly(ADP-ribose) synthe tase, and broadened their chemical as well as biochemical variety. Mor e recently, we found several potent inhibitors of arginine-specific mo no(ADP-ribosyl)transferases and activators of poly(ADP-ribose) synthet ase.