Failure of iniparib to inhibit poly(ADP-Ribose) polymerase in vitro.

ABSTRACT:

Purpose

Poly(ADP-ribose) polymerase (PARP) inhibitors are undergoing extensive clinical testing for their single-agent activity in homologous recombination (HR)-deficient tumors and ability to enhance the action of certain DNA-damaging agents. Compared with other PARP inhibitors in development, iniparib (4-iodo-3-nitrobenzamide) is notable for its simple structure and the reported ability of its intracellular metabolite 4-iodo-3-nitrosobenzamide to covalently inhibit PARP1 under cell-free conditions. The present preclinical studies were conducted to compare the actions iniparib with the more extensively characterized PARP inhibitors olaparib and veliparib.

Experimental design

The abilities of iniparib, olaparib, and veliparib to (i) selectively induce apoptosis or inhibit co

SUBMITTER: Patel AG 

PROVIDER: S-EPMC3306513 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature