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brostallicin A synthetic, alpha-bromoacrylic, second-generation minor groove binder (MGB), related to distamycin A, with potential antineoplastic activity. Brostallicin binds to DNA minor groove DNA, after having formed a highly reactive glutathione (GSH)-brostallicin complex in the presence of the enzyme glutathione S-transferase (GST), which is overexpressed in cancer cells; DNA replication and cell division are inhibited, resulting in tumor cell death. Compared to typical MGBs, this agent appears to bind covalently to DNA in a different manner and its activity does not depend on a functional DNA mismatch repair (MMR) mechanism. Accordingly, brostallicin may be effective against MMR-defective tumors that are refractory to various anticancer agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
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Code name: | ![](https://webarchive.library.unt.edu/eot2008/20090509164644im_/http://www.cancer.gov/images/spacer.gif) | PNU-166196 | | ![](https://webarchive.library.unt.edu/eot2008/20090509164644im_/http://www.cancer.gov/images/spacer.gif) |
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