Add time:09/02/2019         Source:sciencedirect.com

Publisher SummaryThis chapter presents nomenclature of actinomycins (AMs) based on the peptide structure, which uses International Union of Pure and Applied Chemistry–International Union of Biochemistry (IUPAC–IUB) rules for naming peptide analogs. AMs are well-known as specific inhibitors of DNA-primed RNA synthesis and are used as a biochemical tool in numerous investigations on cellular events, especially macromolecular biosynthesis and virus replication. The clinical use of actinomycin is in the treatment of Wilms' tumor, gestational choriocarcinoma, and mixed metastatic embryonal carcinoma of the testis. The chapter has compiled microbiological procedures for actinomycin preparation and chemical methods for modification of AM and for total synthesis. Analogs and derivatives of known structure have been listed. The chapter also describes structure-activity relationships in the AMs that can at present be deduced from approximately 30 peptide analogs that have been isolated from natural sources or produced by directed biosynthesis or by chemical synthesis. The crystal structure of AM and solution conformations from nuclear magnetic resonance (NMR) and circular dichorism (CD) studies have been discussed.

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