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Bioorg Med Chem Lett ; 25(1): 9-15, 2015 Jan 01.
Article in English | MEDLINE | ID: mdl-25434000

ABSTRACT

The enediyne natural products have been explored for their phenomenal cytotoxicity. The development of enediynes into anticancer drugs has been successfully achieved through the utilization of polymer- and antibody-drug conjugates (ADCs) as drug delivery systems. An increasing inventory of enediynes would benefit current application of ADCs in many oncology programs. Innovations in expanding the enediyne inventory should take advantage of the current knowledge of enediyne biosynthesis and post-genomics technologies. Bioinformatics analysis of microbial genomes reveals that enediynes are underexplored, in particular from Actinomycetales. This digest highlights the emerging opportunities to explore microbial genomics for the discovery of novel enediyne natural products.


Subject(s)
Antineoplastic Agents/chemistry , Drug Discovery/trends , Enediynes/chemistry , Genome, Microbial/genetics , Genomics/trends , Animals , Antineoplastic Agents/pharmacology , Enediynes/pharmacology , Genome, Microbial/drug effects , Humans
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