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A small-molecule prodrug inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase-1 (PARP-1) with potential chemosensitizing, radiosensitizing and antineoplastic activities. In vivo, iniparib (PARP-1 inhibitor BSI-201) is converted to the active drug, which selectively binds to PARP-1 and inhibits PARP-1- mediated DNA repair. Consequently, this agent may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. In addition, iniparib may exhibit direct antineoplastic activity against cancers defective in DNA repair. PARP-1 catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
|Synonym:||PARP-1 inhibitor BSI-201|
|Chemical structures:||4-iodo-3-nitrobenzamide |