4930547N16Rik Inhibitors

The class of chemicals known as Parpbp Inhibitors consists primarily of compounds that target the enzymatic activity of Poly (ADP-ribose) polymerase 1 (PARP1). While these inhibitors do not directly bind to PARPB, their mechanism of action involves the inhibition of PARP1, which can indirectly disrupt the functional interplay between PARP1 and PARBP. The inhibition of PARP1 by these chemicals results in the reduction of poly(ADP-ribosyl)ation, a post-translational modification that PARP1 catalyzes in response to DNA damage. By suppressing this activity, these inhibitors can alter the DNA repair functions in which PARBP is implicated through its association with PARP1.

Compounds such as olaparib, rucaparib, and niraparib are structurally diverse but share the common feature of mimicking nicotinamide, the end product of the PARP reaction, thereby acting as competitive inhibitors of PARP1. The binding of these inhibitors to the nicotinamide pocket of PARP1 leads to the prevention of PARP1's adenosine diphosphate (ADP)-ribosyl transferase activity, which is crucial for signaling and recruiting DNA repair proteins to sites of damage. This inhibition of PARP1's activity by these compounds can, therefore, influence the cellular processes in which PARBP takes part.