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Enediynes: Exploration of microbial genomics to discover new anticancer drug leads.

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.

SUBMITTER: Shen B

PROVIDER: S-EPMC4480864 | biostudies-other | 2015 Jan

REPOSITORIES: biostudies-other

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Enediynes: Exploration of microbial genomics to discover new anticancer drug leads.

Shen Ben B Hindra Yan Xiaohui X Huang Tingting T Ge Huiming H Yang Dong D Teng Qihui Q Rudolf Jeffrey D JD Lohman Jeremy R JR

Bioorganic & medicinal chemistry letters 20141114 1

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-g ...[more]

PMID: 25434000

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