title: 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.
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA; Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, FL 33458, USA; Natural Products Library Initiative, The Scripps Research Institute, Jupiter, FL 33458, USA. Electronic address: shenb@scripps.edu.
authors.forename: Ben
authors.initials: B
authors.lastname: Shen
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.lastname: Hindra
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Yan
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Tingting
authors.initials: T
authors.lastname: Huang
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Huiming
authors.initials: H
authors.lastname: Ge
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Dong
authors.initials: D
authors.lastname: Yang
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Qihui
authors.initials: Q
authors.lastname: Teng
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Jeffrey D
authors.initials: JD
authors.lastname: Rudolf
authors.affiliation: Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.
authors.forename: Jeremy R
authors.initials: JR
authors.lastname: Lohman
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D055808:Drug Discovery / Q000639:trends*; D053281:Enediynes / Q000737:chemistry* / Q000494:pharmacology; D064349:Genome, Microbial / Q000187:drug effects / Q000235:genetics*; D023281:Genomics / Q000639:trends*; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D053281:Enediynes
keywords: ADC payload; Biosynthetic gene cluster; Enediyne polyketide synthase; Genome mining; Natural products