distamycin

Distamycin 是可以从 Streptomyces distallicus 菌中分离出的天然抗生素，对某些病毒、革兰氏阳性菌和原生动物有活性。

Distamycin A (NSC-82150)为一种寡肽抗生素及小沟结合剂，其结合B型DNA，并倾向于A T富集区。Distamycin A能调节烯二炔诱导DNA切割位点并促进细胞凋亡。

Tallimustine (FCE 24517)，一种 distamycin-A 衍生物，是一种抗癌剂。

Brostallicin is 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.